Adrenergic Receptor

Choose Selective Adrenergic Receptor Inhibitors

Adrenergic Receptor Signaling Pathway Map

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Products

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  • New Adrenergic Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0949New Mebicar Mebicar, a derivative of bicyclic bis-ureas, inhibits the orientation reaction in albino mice, potentiates the action of narcotic hypnotics, abolishes the conditioned reflex reaction of avoidance, displays central adrenolytic activity, interferes with the norepinephrine metabolism in the brain stem.
S0896 DSP-4 HCl DSP-4 hydrochloride (Neurotoxin DSP 4 (hydrochloride)) can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons, which exclusively affects the noradrenergic fibers from the LC (locus coeruleus).
S1206 Bisoprolol fumarate Bisoprolol fumarate (EMD33512) is a selective type β1 adrenergic receptor blocker.
Front Nutr, 2022, 9:907986
Sci Rep, 2019, 9(1):3018
J Chromatogr B Analyt Technol Biomed Life Sci, 2019, 1129:121793
S1324 Doxazosin Mesylate Doxazosin, a quinazoline-derivative, selectively antagonizes postsynaptic α1-adrenergic receptors, used in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia.
J Ocul Pharmacol Ther, 2017, 33(1):50-56
Prostate, 2016, 76(8):757-66
Antiviral Res, 2015, 120:140-6
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
S2086 Ivabradine HCl Ivabradine HCl (S 16257-2,S-18982 D6 hydrochloride), a new If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent.
Cell Rep, 2022, 38(10):110468
J Pain, 2018, 19(6):626-634
S2113 Cisatracurium Besylate Cisatracurium Besylate(51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
Biosci Trends, 2021, 15(1):50-54
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4076 Propranolol HCl Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 of 12 nM.
Cell Rep, 2022, 38(10):110468
EBioMedicine, 2022, 82:104149
Cancers (Basel), 2022, 14(9)2222
S4112 Desvenlafaxine Succinate Desvenlafaxine Succinate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.
Drug Metab Dispos, 2020, 48(10):1044-1052
S4113 Desvenlafaxine Desvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.
Drug Metab Dispos, 2020, 48(10):1044-1052
S5088 Labetalone hydrochloride Labetalone hydrochloride (Benzoic amide) is hydrochloride form of labetalone, a blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive.
S5496 Guanethidine Monosulfate Guanethidine monosulfate is an antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves.
S5703 Carvedilol Phosphate Carvedilol Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity.
Res Pharm Sci, 2016, 11(5):419-427
Res Pharm Sci, 2015, 10(5):388-96
S5723 Carvedilol EP IMpurity E Carvedilol is a nonselective beta blocker/alpha-1 blocker and used in management of congestive heart failure (CHF).
S5739 Nebivolol Nebivolol (Bystolic,R 065824) is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure.
Front Pharmacol, 2021, 12:691998
Sci Rep, 2015, 5:16406
S5787 Dronedarone Dronedarone (SR33589) is a derivative of amiodarone which is classified as a Class III antiarrhythmic agent. It shows rate-dependent inhibition of the rapid Na+ current, inhibits α and β-adrenergic receptors like Class II agents, exhibits blockade of K+ outward currents as the main mechanism of action of Class III, and effectively block slow Ca2+ inward currents (Class IV).
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
S6345 3-Nitro-L-tyrosine 3-Nitro-L-tyrosine (3-NT, N-Tyr, MNT), synthesized from L-tyrosine by peroxynitrite, is a product of nitric oxide and superoxide. 3-Nitro-L-tyrosine inhibits the hemodynamic responses to angiotensin II, possibly through the inhibition of alpha 1-adrenoceptor-mediated events.
S9470New Penbutolol Sulfate Penbutolol sulfate ((-)-Terbuclomine) is an effective beta-adrenergic receptor blocker and diuretic that is used as an antihypertensive agent.
S9560 Anisodamine Hydrobromide Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
E0785New YS-49 YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
S3764 Isoferulic Acid Isoferulic acid (Hesperetic acid, Hesperetate, Isoferulate), a major active ingredient of Cimicifuga heracleifolia, shows anti-inflammatory, antiviral, antioxidant, and antidiabetic properties. Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use.
E0408New JP1302 JP-1302(MMV006172), a novel highly selective α2C-adrenoceptor antagonist with Kb of 16 nM at the α2C-adrenoceptor subtype, also produces antidepressant and antipsychotic-like effects. 
E0529New Metipranolol Metipranolol (Betamann) is potent β-adrenergic receptor antagonist, possessing the beta-blocking potencies (pA2) of 8.3, 8.4 at guinea pig atrial β1-adrenoceptor and β2-adrenoceptor of the rat uterus, respectively, also is a potent displacer of 3H-DHA binding, ligand concentration 0.7 nM, possessing a Ki value of 39 ± 24 nM.
S0116 Piperoxan hydrochloride Piperoxan hydrochloride (Benodaine, Fourneau 933, F933, DL-Piperoxan) is an antagonist of α2 (alpha 2) adrenoceptor.
S0812 SR59230A SR59230A is a blood-brain barrier penetrating, potent and selective antagonist of β3-adrenergic receptor with IC50 of 40 nM, 408 nM, and 648 nM for β3, β1, and β2 receptors, respectively.
S0862 L-765314 L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.
S1283 Asenapine maleate Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Biochem Biophys Res Commun, 2021, 553:172-179
Anticancer Res, 2021, 41(2):687-697
Sci Rep, 2018, 8(1):15753
S1387 Naftopidil DiHCl Naftopidil DiHCl (Flivas, KT-611, Avishot,BM-15275) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.
S1409 Alfuzosin HCl Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Prostate, 2016, 76(8):757-66
S1424 Prazosin HCl Prazosin HCl (cp-12299-1) is a competitive alpha-1 adrenoceptor antagonist, used to treat high blood pressure or benign prostatic hyperplasia.
BMC Pharmacol Toxicol, 2020, 21(1):61
S1435 Tamsulosin hydrochloride Tamsulosin (Flomax) hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
S1549 Nebivolol hydrochloride (R-65824) Nebivolol HCl (R-65824) selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Oncogenesis, 2022, 11(1):24
Nat Commun, 2021, 12(1):5919
Front Pharmacol, 2021, 12:691998
S1613 Silodosin Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.
S1827 Betaxolol HCl Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM.
Chirality, 2018, 30(11):1195-1205
S1831 Carvedilol Carvedilol (BM-14190, SKF 105517) is a non-selective beta blocker/alpha-1 blocker, used to treat congestive heart failure (CHF) and high blood pressure.
PLoS Pathog, 2020, 16;16(3):e1008341
Res Pharm Sci, 2016, 11(5):419-427
Res Pharm Sci, 2015, 10(5):388-96
S1856 Metoprolol Tartrate Metoprolol Tartrate (CGP 2175E) is a selective β1 receptor blocker medication, used to treat hypertension and heart failure.
S2038 Phentolamine Mesylate Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.
Oncol Rep, 2021, 46(3)202
S2059 Terazosin HCl Dihydrate Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
J Biomed Sci, 2021, 28(1):8
S2091 Betaxolol Betaxolol (SL 75212,Dextrobetaxolol) is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
Nat Commun, 2020, 24;11(1):1990
Chirality, 2018, 30(11):1195-1205
S2126 Naftopidil Naftopidil (KT-611) is a selective α1-adrenergic receptor antagonist with Ki of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia.
Cell Syst, 2019, 8(2):97-108
S2174New Hydroxyflutamide (Hydroxyniphtholide) Hydroxyflutamide (SCH-16423, Hydroxyniphtholide) is an androgen receptor (AR) antagonist and possesses an IC50 of 0.7 μM for the androgen receptor.
S2373 Yohimbine HCl Yohimbine (Antagonil) has been used as a mydriatic and in the treatment of impotence. It is also alleged to be an aphrodisiac.
Mol Pain, 2022, 18:17448069221107810
J Med Chem, 2021, 64(18):13510-13523
J Inflamm Res, 2021, 14:1217-1233
S2499 Phenoxybenzamine HCl Phenoxybenzamine HCl (NSC 37448, NCI-c01661) is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM.
S2509 Sotalol HCl Sotalol(MJ-1999) is a non-selective beta blocker and a potassium channel blocker with an IC50 of 43 μM.
Toxicol Appl Pharmacol, 2021, 431:115731
Gynecol Oncol, 2018, 151(3):525-532
Toxicol Appl Pharmacol, 2015, 285(1):51-60
S2517 Maprotiline HCl Maprotiline HCl is a selective noradrenalin re-uptake inhibitor, used in the treatment of depression.
Front Pharmacol, 2021, 12:689767
S2607 Buflomedil HCl Buflomedil HCl(NSC 759291) is a vasodilator used to treat claudication or the symptoms of peripheral arterial disease; A nonselective alpha adrenergic receptor inhibitor.
S2691 BMY 7378 Dihydrochloride BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
S3656 Piribedil Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.
S4010 Acebutolol HCl Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
Front Pharmacol, 2021, 12:740529
S4085 Levobetaxolol HCl Levobetaxolol (AL 1577A,(S)-Betaxolol hydrochloride) exhibits a higher affinity at cloned human β1 and β2 receptors with Ki value of 0.76 nM and 32.6 nM, respectively.
S4100 Esmolol HCl Esmolol (ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms.
S4123 Timolol Maleate Timolol Maleate (MK-950,(S)-Timolol Maleate) is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.
J Dermatolog Treat, 2020, 24:1-7
S4124 Tolazoline HCl Tolazoline(Imidaline hydrochloride,NSC35110 hydrochloride) is a non-selective competitive α-adrenergic receptor antagonist.
Insect Biochem Mol Biol, 2017, 90:61-70
S4278 Carteolol HCl Carteolol HCl(Carteolol hydrochloride,OPC-1085 hydrochloride) is a β-adrenoceptor antagonist, used for the treatment of glaucoma.
S4291 Labetalol HCl Labetalol HCl(AH-5158 hydrochloride,Labetalol hydrochloride,Sch-15719W) is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors, used in the treatment of high blood pressure.
S4358 Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S4649 Atipamezole hydrochloride Atipamezole (Antisedan, MPV1248) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride is hydrochloride form of atipamezole.
S4650 Atipamezole Atipamezole (MPV-1248, MPV1248, Antisedan) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug.
Exp Mol Med, 2020, 10.1038/s12276-020-0461-6
Nitric Oxide, 2019, 85:1-9
Front Neurol, 2019, 10:1041
S4679 Terazosin HCl Terazosin (Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin) is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
J Biomed Sci, 2021, 28(1):8
S4797 Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.
S4817 Atenolol Atenolol (Tenormin, Normiten, Blokium) is a selective β1 receptor antagonist with log Kd values of −6.66±0.05, −5.99±0.14, −4.11±0.07 for binding to the human β1-, β2- and β3-adrenoceptors.
Oncol Rep, 2021, 46(3)202
S5023 Nadolol Nadolol (Corgard, Solgol, Anabet, SQ11725) is a non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities.
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
S5042 Bevantolol hydrochloride Bevantolol hydrochloride (NC-1400) is a cardioselective, beta adrenoceptor antagonist, devoid of intrinsic β sympathomimetic activity and with weak membrane-stabilizing and local anesthetic properties.
S5281 Dapiprazole Hydrochloride Dapiprazole Hydrochloride (Glamidolo Hydrochloride, Reversil Hydrochloride) is the hydrochloride salt form of dapiprazole, an alpha-adrenergic blocker used to reverse mydriasis after eye examination.
S5337 Rauwolscine hydrochloride Rauwolscine hydrochloride (Isoyohimbine, α-Yohimbine, corynanthidine) is the hydrochloride salt form of Rauwolscine, a specific and potent α2 antagonist with Ki of 12 nM.
J Pharm Biomed Anal, 2020, 180:113019
S5341 Metroprolol succinate Metroprolol Succinate (Metoprolol succinate) is the succinate salt form of metoprolol, a cardioselective competitive beta-1 adrenergic receptor antagonist with antihypertensive properties and devoid of intrinsic sympathomimetic activity.
S5430 Metoprolol Metoprolol is a cardioselective β1-adrenergic blocking agent with log Kd values of −7.26±0.07, −6.89±0.09, −5.16±0.12 for β1, β2, and β3 adrenoceptors, respectively. It is used for acute myocardial infarction, heart failure, angina pectoris and mild to moderate hypertension.
Cell Rep, 2022, 38(10):110468
S5432 Dibenamine Hydrochloride Dibenamine (N-(2-Chloroethyl)dibenzylamine, Sympatholytin, Dibenzylchlorethamine) is an irreversible blocker of α1 adrenoceptors.
S5540 Landiolol hydrochloride Landiolol hydrochloride (ONO-1101) is the hydrochloride salt form of Landiolol, which is an ultra-short-acting β1 selective adrenoceptor antagonist.
S5666 Moxisylyte hydrochloride Moxisylyte hydrochloride (thymoxamine) is an alpha-adrenergic blocking agent used for the treatment of Raynaud's disease.
S5766 Alfuzosin Alfuzosin(SL 77499), a quinazoline derivative, is a selective and competitive α1-adrenoceptor antagonist.
S5778 Esmolol Esmolol is a cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
S5780 Prazosin Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors. It is used to treat hypertension.
BMC Pharmacol Toxicol, 2020, 21(1):61
S5782 Doxazosin Doxazosin(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
S5789 Propafenone Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias.
S5802 Alprenolol hydrochloride Alprenolol hydrochloride is the hydrochloride salt form of alprenolol, which is an beta adrenergic receptorantagonist and is used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
S5923 Celiprolol hydrochloride Celiprolol is a β1-adrenoceptor antagonist with partial β2 agonist activity.
S5942 Bisoprolol Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
S5965 Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S5981 S(-)-Propranolol hydrochloride (S)-(-)-Propranolol hydrochloride, the active enantiomer of propranolol, is a β-Adrenoceptor (β-Adrenergic Receptor) antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively.
S6447 Carazolol Carazolol is a non-specific β-adrenergic receptor blocking agent and binds to β receptors irreversibly.
S7538 RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S8114 ICI-118551 Hydrochloride ICI-118551 is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
Biomedicines, 2022, 10(2)487
Toxicol In Vitro, 2021, 77:105251
iScience, 2021, 24(12):103362
S9050 Boldine Boldine, isolated from Peumus boldus, has alpha-adrenergic antagonist activities in vascular tissue with anti-oxidant, hepatoprotective, cytoprotective, antipyretic and anti-inflammatory effects.
S9285 Fargesin Fargesin is a neolignan isolated from Magnolia plants. It is a potential β1AR antagonist through cAMP/PKA pathway.
E0450New Clenbuterol Hydrochloride

Clenbuterol (CST-103) Hydrochloride is a potent and selective adrenergic beta 2-receptor agonist.

Cell Death Dis, 2022, 13(6):571
S0032 Batefenterol  Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.
S1437 Tizanidine HCl Tizanidine HCl (DS 103-282) is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
Drug Metab Dispos, 2021, 49(8):638-647
S2020 Formoterol Hemifumarate Formoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316,Formoterol fumarate) is a potent, selective and long-acting β2-adrenoceptor agonist used in the management of asthma and chronic obstructive pulmonary disease(COPD).
S2083 Procaterol HCl Procaterol HCl (OPC-2009) is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
S2090 Dexmedetomidine HCl Dexmedetomidine HCl((+)-Medetomidine Hydrochloride) is a highly selective and potent alpha-2 adrenoceptor agonist, which reduces anesthetic requirements for patients by providing significant sedation.
Oral Dis, 2022, 10.1111/odi.14286
JHEP Rep, 2021, 3(4):100296
Sci Rep, 2021, 11(1):13345
S2092 Detomidine HCl Detomidine HCl(MPV 253AII) produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors.
Nature, 2018, 560(7718):372-376
S2304 Gramine Gramine (Donaxine) is a natural indole alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50 of 3.2 µM and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist.
S2362 Synephrine Synephrine (Oxedrine), a natural protoalkaloid in the extract of bitter orange and other citrus species, is commonly used for weight loss.
S2438 Synephrine HCl SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) agonist.
S2458 Clonidine HCl Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
Mol Pain, 2022, 18:17448069221107810
S2507 Salbutamol Sulfate Salbutamol Sulfate (Albuterol, Ventolin, Aerolin, Ventorlin, Asthalin, Asthavent) is a short-acting β2-adrenergic receptor agonist with an IC50 of 8.93 µM.
Front Physiol, 2022, 13:800055
cell, 2020, 180(1):64-78.e16
Sci Signal, 2020, 13(659)eaax0273
S2516 Xylazine HCl Xylazine(BAY 1470 hydrochloride) is an α2-Adrenergic receptor agonist, used as a sedative and muscle relaxant.
Eur J Pharmacol, 2021, 911:174522
Fitoterapia, 2021, 152:104922
STAR Protoc, 2021, 2(4):100915
S2519 Naphazoline HCl Naphazoline HCl is an ocular vasoconstrictor and imidazoline derivative sympathomimetic amine.
S2521 Epinephrine bitartrate Epinephrine bitartrate (Adrenalinium) is an alpha- and beta-adrenergic receptor stimulator.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
J Immunother Cancer, 2021, 9(1)e001466
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2522 L-Adrenaline L-Adrenaline (Epinephrine) belongs to a group of the compounds known as catecholamines.
S2523 DL-Adrenaline DL-Adrenaline(dl-Epinephrine) is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands.
S2533 Ritodrine HCl Ritodrine HCl (NSC 291565,DU 21220, Ritodrine) is a hydrochloride salt of ritodrine which is a β-2 adrenergic receptor agonist.
S2545 Scopine Scopine(6,7-Epoxytropine) is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.
S2566 Isoprenaline (NCI-C55630) HCl Isoprenaline HCl (NCI-c55630,Isoproterenol hydrochloride) is a non-selective beta-adrenergic receptor agonist, used for the treatment of bradycardia and heart block.
BMC Cancer, 2022, 22(1):213
J Dairy Sci, 2022, 105(8):6997-7010
PLoS Pathog, 2020, 16;16(3):e1008341
S2569 Phenylephrine (NCI-C55641) HCl Phenylephrine HCl (NCI-c55641,Phenylephrine hydrochloride,(R)-(-)-Phenylephrine hydrochloride, L-Phenylephrine hydrochloride) is a selective α1-adrenergic receptor agonist, used primarily as a decongestant.
Oxid Med Cell Longev, 2021, 2021:7848027
Front Pharmacol, 2019, 10:465
Sci Adv, 2019, 5(5):eaau0495
S2576 Xylometazoline HCl Xylometazoline is an α-adrenoceptor agonist commonly used as nasal decongestant, exhibits highest potency at α2B-adrenoceptor subtype with EC50 of 99 μM.
S2615 Noradrenaline bitartrate monohydrate Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
S3041 Droxidopa Droxidopa (L-DOPS) is a psychoactive drug and acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
S3060 Medetomidine HCl Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
Micromachines, 2018, 9(6)
S3061 Epinephrine HCl Epinephrine HCl (Adrenaline) is a hormone and a neurotransmitter.
J Immunother Cancer, 2021, 9(1)e001466
S3075 Dexmedetomidine Dexmedetomidine is a sedative medication used by intensive care units and anesthetists.
Neural Plast, 2022, 2022:1353778
Oral Dis, 2022, 10.1111/odi.14286
JHEP Rep, 2021, 3(4):100296
S3083 Indacaterol Maleate Indacaterol (QAB149) is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor.
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
S3185 Adrenalone HCl Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.
S3294 Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
S3640 Methoxyphenamine Hydrochloride Methoxyphenamine Hydrochloride (2-methoxy-N-methylamphetamine, OMMA) is a β-adrenergic receptor agonist of the amphetamine class used as a bronchodilator.
S3727 Vilanterol Trifenate Vilanterol trifenatate (GW642444M) is a novel inhaled long-acting beta2 adrenoceptor agonist with inherent 24-hour activity for once daily treatment of COPD and asthma.
Toxicol In Vitro, 2021, 77:105251
J Neuroimmunol, 2019, 332:37-48
S3960 Higenamine hydrochloride Higenamine (Norcoclaurine, (+-)-Demethylcoclaurine), also known as Norcoclaurine HCl, is a non-selective β2 adrenoceptor agonist which is a chemical compound naturally occurring in a number of plants.
Oncol Rep, 2021, 46(3)202
Mol Cell Biochem, 2021, 10.1007/s11010-021-04197-z
S4009 Mirabegron Mirabegron (YM 178) is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S4043 Tetrahydrozoline HCl Tetrahydrozoline (Tetryzoline) HCl is an imidazoline derivative with alpha receptor agonist activity.
S4065 Guanabenz Acetate Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.
Cell Stem Cell, 2020, 27(6):876-889.e12
Thyroid, 2019, 29(6):809-823
S4127 Terbutaline Sulfate Terbutaline Sulfate(Terbutaline hemisulfate) is a selective β2-adrenergic receptor agonist with IC50 of 53 nM.
BMC Pharmacol Toxicol, 2020, 21(1):61
Hum Reprod, 2016, 31(11):2506-2519
S4135 Clorprenaline HCl Clorprenaline HCl (NSC 334693) is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
S4266 Brimonidine Tartrate Brimonidine Tartrate(UK 1434 Tartrate) is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.
S4277 Bambuterol HCl Bambuterol HCl(Bambuterol hydrochloride,KWD-2183 hydrochloride) is a potent β-adrenoceptor agonist, used in the treatment of asthma.
S4296 Salmeterol Xinafoate Salmeterol Xinafoate(GR 33343X xinafoate,Salmetedur) is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.
ACS Pharmacol Transl Sci, 2019, 2(3):148-154
Commun Biol, 2018, 1:106
S4481 Guanabenz Guanabenz (GBZ, GA, Wytensin, Wy-8678,BR-750) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.
S4485 Olodaterol (BI 1744) Olodaterol (BI 1744) is a long-acting β2-adrenergic receptor agonist that is used as a component of an inhalation (Tiotropium/Olodaterol) for treating patients with chronic obstructive pulmonary disease (COPD).
S4693 Guanfacine Hydrochloride Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.
S5217 Arformoterol Tartrate Arformoterol Tartrate is the tartrate salt of arformoterol, a long-acting beta-2 adrenergic agonist with bronchodilator activity.
S5267 Nylidrin Hydrochloride Nylidrin Hydrochloride (Buphenine), a β-adrenergic agonist, is used therapeutically for its vasodilating effect on the peripheral circulation and possibly on the cerebral circulation as well.
S5494 Salbutamol Salbutamol (Albuterol) is a short-acting, selective beta2-adrenergic receptor agonist used to treat or prevent bronchospasm in patients with asthma, bronchitis, emphysema, and other lung diseases.
Front Physiol, 2022, 13:800055
BMC Pharmacol Toxicol, 2020, 21(1):61
S5527 Salmeterol Salmeterol (Astmerole, GR-33343X, SN408D) is a long-acting beta2-adrenergic receptor agonist with Ki value of 1.5 nM for WT β2AR and shows very high selectivity for the WT β2AR(β1Ki/β2Ki ratio of approximately 1500).
Front Pharmacol, 2022, 13:865715
Mol Syst Biol, 2021, 17(8):e10239
Drug Test Anal, 2020, 10.1002/dta.2917
S5537 Tizanidine Tizanidine is an imidazoline derivative and a centrally acting α2 adrenergic agonist used as a muscle relaxant for therapy of acute muscle spasms and chronic spasticity.
Drug Metab Dispos, 2021, 49(8):638-647
S5564 Xylazine Xylazine is a partial alpha-2 adrenergic agonist that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals.
Cell Death Differ, 2020, 10.1038
Mol Med Rep, 2017, 16(2):1911-1919
S5654 Indacaterol Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor.
Drug Test Anal, 2020, 10.1002/dta.2917
J Neuroimmunol, 2019, 332:37-48
S5669 Isoxsuprine hydrochloride Isoxsuprine hydrochloride is a beta-adrenergic agonist with vasodilator activity.
S5683 Isoproterenol sulfate dihydrate Isoproterenol Sulfate is the sulfate salt form of isoproterenol, a beta-adrenergic receptor agonist with bronchodilator activity.
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
Biochim Biophys Acta Mol Cell Res, 2021, 1868(10):119080
S5727 Tetryzoline Tetryzoline (Tetrahydrozoline) is an alpha-adrenergic agonist used in some over-the-counter eye drops and nasal sprays.
S5734 Midodrine hydrochloride Midodrine hydrochloride is the hydrochloride salt form of midodrine, an adrenergic alpha-1 agonist used as a vasopressor.
S5735 Midodrine Midodrine belongs to the class of medications known as vasopressors. It is an adrenergic alpha-1 agonist.
S5750 DL-Norepinephrine hydrochloride Norepinephrine (noradrenaline) is the neurotransmitter at most sympathetic neuroeffector junctions and has pharmacologic effects on both α1 and β1 adrenoceptors.
S5768 Fenoterol hydrobromide Fenoterol hydrobromide (Phenoterol) is the the hydrobromide salt of fenoterol, a β2 adrenoreceptor agonist with bronchodilator activity.
Toxicol In Vitro, 2021, 77:105251
S5769 Fenoterol Fenoterol (Phenoterol) is a β2 adrenoreceptor agonist with bronchodilator activity.
S5925 Olodaterol hydrochloride Olodaterol hydrochloride (BI-1744) is the hydrochloride salt form of Olodaterol, which is a long-acting beta2-adrenergic agonist.
S5954 L-(-)-α-Methyldopa hydrate L-(-)-α-Methyldopa (Methyldopa, MK-351) hydrate, a potent antihypertensive drug, is a selective agonist for α2-adrenergic receptors.
S6487 fluticasone furoate Fluticasone furoate (GW685698) is an inhaled corticosteroid/long-acting beta-agonist combination with a prolonged bronchodilator duration of action. It is used for the treatment of non-allergic and allergic rhinitis administered by a nasal spray.
S6583 Apraclonidine HCl Apraclonidine (Iopidine,ALO 2145) is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist.
S7974 L755507 L-755,507 is characterized as a potent and selective β3 adrenergic receptor partial agonist with EC50 of 0.43 nM. It is also recently identified to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs) and other cell types.
Genesis, 2022, 60(1-2):e23465
Chembiochem, 2021, 22(20):2957-2965
Hum Mutat, 2019, 10.1002/humu.23848
S9507 (−)-Norepinephrine (−)-Norepinephrine (Arterenol, Levarterenol, L-Noradrenaline) is a natural neurotransmitter and hormone. It is an agonist of adrenergic receptors with Ki values of 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively.
Commun Biol, 2022, 5(1):339
Eur J Pharmacol, 2022, 926:175040
Cardiovasc Drugs Ther, 2020, 11
S9508 Brimonidine Brimonidine (Bromoxidine, UK 1430) is an alpha adrenergic receptor agonist (primarily alpha-2) and is used for the treatment of open-angle glaucoma or ocular hypertension to lower intraocular pressure.
S3153 Levalbuterol tartrate Levalbuterol HCl(Levosalbutamol tartrate) is a relatively selective beta2-adrenergic receptor agonist used for the treatment of asthma.
S4243 Deoxycorticosterone acetate Deoxycorticosterone acetate (11-Deoxycorticosterone, DOC, Cortexone) is a steroid hormone used for intramuscular injection for replacement therapy of the adrenocortical steroid.
Nat Cancer, 2020, 1(2):235-248
E0949New Mebicar Mebicar, a derivative of bicyclic bis-ureas, inhibits the orientation reaction in albino mice, potentiates the action of narcotic hypnotics, abolishes the conditioned reflex reaction of avoidance, displays central adrenolytic activity, interferes with the norepinephrine metabolism in the brain stem.
S0896 DSP-4 HCl DSP-4 hydrochloride (Neurotoxin DSP 4 (hydrochloride)) can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons, which exclusively affects the noradrenergic fibers from the LC (locus coeruleus).
S1206 Bisoprolol fumarate Bisoprolol fumarate (EMD33512) is a selective type β1 adrenergic receptor blocker.
Front Nutr, 2022, 9:907986
Sci Rep, 2019, 9(1):3018
J Chromatogr B Analyt Technol Biomed Life Sci, 2019, 1129:121793
S1324 Doxazosin Mesylate Doxazosin, a quinazoline-derivative, selectively antagonizes postsynaptic α1-adrenergic receptors, used in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia.
J Ocul Pharmacol Ther, 2017, 33(1):50-56
Prostate, 2016, 76(8):757-66
Antiviral Res, 2015, 120:140-6
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
S2086 Ivabradine HCl Ivabradine HCl (S 16257-2,S-18982 D6 hydrochloride), a new If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent.
Cell Rep, 2022, 38(10):110468
J Pain, 2018, 19(6):626-634
S2113 Cisatracurium Besylate Cisatracurium Besylate(51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
Biosci Trends, 2021, 15(1):50-54
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4076 Propranolol HCl Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 of 12 nM.
Cell Rep, 2022, 38(10):110468
EBioMedicine, 2022, 82:104149
Cancers (Basel), 2022, 14(9)2222
S4112 Desvenlafaxine Succinate Desvenlafaxine Succinate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.
Drug Metab Dispos, 2020, 48(10):1044-1052
S4113 Desvenlafaxine Desvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.
Drug Metab Dispos, 2020, 48(10):1044-1052
S5088 Labetalone hydrochloride Labetalone hydrochloride (Benzoic amide) is hydrochloride form of labetalone, a blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive.
S5496 Guanethidine Monosulfate Guanethidine monosulfate is an antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves.
S5703 Carvedilol Phosphate Carvedilol Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity.
Res Pharm Sci, 2016, 11(5):419-427
Res Pharm Sci, 2015, 10(5):388-96
S5723 Carvedilol EP IMpurity E Carvedilol is a nonselective beta blocker/alpha-1 blocker and used in management of congestive heart failure (CHF).
S5739 Nebivolol Nebivolol (Bystolic,R 065824) is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure.
Front Pharmacol, 2021, 12:691998
Sci Rep, 2015, 5:16406
S5787 Dronedarone Dronedarone (SR33589) is a derivative of amiodarone which is classified as a Class III antiarrhythmic agent. It shows rate-dependent inhibition of the rapid Na+ current, inhibits α and β-adrenergic receptors like Class II agents, exhibits blockade of K+ outward currents as the main mechanism of action of Class III, and effectively block slow Ca2+ inward currents (Class IV).
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
S6345 3-Nitro-L-tyrosine 3-Nitro-L-tyrosine (3-NT, N-Tyr, MNT), synthesized from L-tyrosine by peroxynitrite, is a product of nitric oxide and superoxide. 3-Nitro-L-tyrosine inhibits the hemodynamic responses to angiotensin II, possibly through the inhibition of alpha 1-adrenoceptor-mediated events.
S9470New Penbutolol Sulfate Penbutolol sulfate ((-)-Terbuclomine) is an effective beta-adrenergic receptor blocker and diuretic that is used as an antihypertensive agent.
S9560 Anisodamine Hydrobromide Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
E0785New YS-49 YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
S3764 Isoferulic Acid Isoferulic acid (Hesperetic acid, Hesperetate, Isoferulate), a major active ingredient of Cimicifuga heracleifolia, shows anti-inflammatory, antiviral, antioxidant, and antidiabetic properties. Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use.
E0408New JP1302 JP-1302(MMV006172), a novel highly selective α2C-adrenoceptor antagonist with Kb of 16 nM at the α2C-adrenoceptor subtype, also produces antidepressant and antipsychotic-like effects. 
E0529New Metipranolol Metipranolol (Betamann) is potent β-adrenergic receptor antagonist, possessing the beta-blocking potencies (pA2) of 8.3, 8.4 at guinea pig atrial β1-adrenoceptor and β2-adrenoceptor of the rat uterus, respectively, also is a potent displacer of 3H-DHA binding, ligand concentration 0.7 nM, possessing a Ki value of 39 ± 24 nM.
S0116 Piperoxan hydrochloride Piperoxan hydrochloride (Benodaine, Fourneau 933, F933, DL-Piperoxan) is an antagonist of α2 (alpha 2) adrenoceptor.
S0812 SR59230A SR59230A is a blood-brain barrier penetrating, potent and selective antagonist of β3-adrenergic receptor with IC50 of 40 nM, 408 nM, and 648 nM for β3, β1, and β2 receptors, respectively.
S0862 L-765314 L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.
S1283 Asenapine maleate Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Biochem Biophys Res Commun, 2021, 553:172-179
Anticancer Res, 2021, 41(2):687-697
Sci Rep, 2018, 8(1):15753
S1387 Naftopidil DiHCl Naftopidil DiHCl (Flivas, KT-611, Avishot,BM-15275) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.
S1409 Alfuzosin HCl Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Prostate, 2016, 76(8):757-66
S1424 Prazosin HCl Prazosin HCl (cp-12299-1) is a competitive alpha-1 adrenoceptor antagonist, used to treat high blood pressure or benign prostatic hyperplasia.
BMC Pharmacol Toxicol, 2020, 21(1):61
S1435 Tamsulosin hydrochloride Tamsulosin (Flomax) hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
S1549 Nebivolol hydrochloride (R-65824) Nebivolol HCl (R-65824) selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Oncogenesis, 2022, 11(1):24
Nat Commun, 2021, 12(1):5919
Front Pharmacol, 2021, 12:691998
S1613 Silodosin Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.
S1827 Betaxolol HCl Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM.
Chirality, 2018, 30(11):1195-1205
S1831 Carvedilol Carvedilol (BM-14190, SKF 105517) is a non-selective beta blocker/alpha-1 blocker, used to treat congestive heart failure (CHF) and high blood pressure.
PLoS Pathog, 2020, 16;16(3):e1008341
Res Pharm Sci, 2016, 11(5):419-427
Res Pharm Sci, 2015, 10(5):388-96
S1856 Metoprolol Tartrate Metoprolol Tartrate (CGP 2175E) is a selective β1 receptor blocker medication, used to treat hypertension and heart failure.
S2038 Phentolamine Mesylate Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.
Oncol Rep, 2021, 46(3)202
S2059 Terazosin HCl Dihydrate Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
J Biomed Sci, 2021, 28(1):8
S2091 Betaxolol Betaxolol (SL 75212,Dextrobetaxolol) is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
Nat Commun, 2020, 24;11(1):1990
Chirality, 2018, 30(11):1195-1205
S2126 Naftopidil Naftopidil (KT-611) is a selective α1-adrenergic receptor antagonist with Ki of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia.
Cell Syst, 2019, 8(2):97-108
S2174New Hydroxyflutamide (Hydroxyniphtholide) Hydroxyflutamide (SCH-16423, Hydroxyniphtholide) is an androgen receptor (AR) antagonist and possesses an IC50 of 0.7 μM for the androgen receptor.
S2373 Yohimbine HCl Yohimbine (Antagonil) has been used as a mydriatic and in the treatment of impotence. It is also alleged to be an aphrodisiac.
Mol Pain, 2022, 18:17448069221107810
J Med Chem, 2021, 64(18):13510-13523
J Inflamm Res, 2021, 14:1217-1233
S2499 Phenoxybenzamine HCl Phenoxybenzamine HCl (NSC 37448, NCI-c01661) is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM.
S2509 Sotalol HCl Sotalol(MJ-1999) is a non-selective beta blocker and a potassium channel blocker with an IC50 of 43 μM.
Toxicol Appl Pharmacol, 2021, 431:115731
Gynecol Oncol, 2018, 151(3):525-532
Toxicol Appl Pharmacol, 2015, 285(1):51-60
S2517 Maprotiline HCl Maprotiline HCl is a selective noradrenalin re-uptake inhibitor, used in the treatment of depression.
Front Pharmacol, 2021, 12:689767
S2607 Buflomedil HCl Buflomedil HCl(NSC 759291) is a vasodilator used to treat claudication or the symptoms of peripheral arterial disease; A nonselective alpha adrenergic receptor inhibitor.
S2691 BMY 7378 Dihydrochloride BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
S3656 Piribedil Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.
S4010 Acebutolol HCl Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
Front Pharmacol, 2021, 12:740529
S4085 Levobetaxolol HCl Levobetaxolol (AL 1577A,(S)-Betaxolol hydrochloride) exhibits a higher affinity at cloned human β1 and β2 receptors with Ki value of 0.76 nM and 32.6 nM, respectively.
S4100 Esmolol HCl Esmolol (ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms.
S4123 Timolol Maleate Timolol Maleate (MK-950,(S)-Timolol Maleate) is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.
J Dermatolog Treat, 2020, 24:1-7
S4124 Tolazoline HCl Tolazoline(Imidaline hydrochloride,NSC35110 hydrochloride) is a non-selective competitive α-adrenergic receptor antagonist.
Insect Biochem Mol Biol, 2017, 90:61-70
S4278 Carteolol HCl Carteolol HCl(Carteolol hydrochloride,OPC-1085 hydrochloride) is a β-adrenoceptor antagonist, used for the treatment of glaucoma.
S4291 Labetalol HCl Labetalol HCl(AH-5158 hydrochloride,Labetalol hydrochloride,Sch-15719W) is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors, used in the treatment of high blood pressure.
S4358 Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S4649 Atipamezole hydrochloride Atipamezole (Antisedan, MPV1248) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride is hydrochloride form of atipamezole.
S4650 Atipamezole Atipamezole (MPV-1248, MPV1248, Antisedan) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug.
Exp Mol Med, 2020, 10.1038/s12276-020-0461-6
Nitric Oxide, 2019, 85:1-9
Front Neurol, 2019, 10:1041
S4679 Terazosin HCl Terazosin (Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin) is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
J Biomed Sci, 2021, 28(1):8
S4797 Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.
S4817 Atenolol Atenolol (Tenormin, Normiten, Blokium) is a selective β1 receptor antagonist with log Kd values of −6.66±0.05, −5.99±0.14, −4.11±0.07 for binding to the human β1-, β2- and β3-adrenoceptors.
Oncol Rep, 2021, 46(3)202
S5023 Nadolol Nadolol (Corgard, Solgol, Anabet, SQ11725) is a non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities.
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
S5042 Bevantolol hydrochloride Bevantolol hydrochloride (NC-1400) is a cardioselective, beta adrenoceptor antagonist, devoid of intrinsic β sympathomimetic activity and with weak membrane-stabilizing and local anesthetic properties.
S5281 Dapiprazole Hydrochloride Dapiprazole Hydrochloride (Glamidolo Hydrochloride, Reversil Hydrochloride) is the hydrochloride salt form of dapiprazole, an alpha-adrenergic blocker used to reverse mydriasis after eye examination.
S5337 Rauwolscine hydrochloride Rauwolscine hydrochloride (Isoyohimbine, α-Yohimbine, corynanthidine) is the hydrochloride salt form of Rauwolscine, a specific and potent α2 antagonist with Ki of 12 nM.
J Pharm Biomed Anal, 2020, 180:113019
S5341 Metroprolol succinate Metroprolol Succinate (Metoprolol succinate) is the succinate salt form of metoprolol, a cardioselective competitive beta-1 adrenergic receptor antagonist with antihypertensive properties and devoid of intrinsic sympathomimetic activity.
S5430 Metoprolol Metoprolol is a cardioselective β1-adrenergic blocking agent with log Kd values of −7.26±0.07, −6.89±0.09, −5.16±0.12 for β1, β2, and β3 adrenoceptors, respectively. It is used for acute myocardial infarction, heart failure, angina pectoris and mild to moderate hypertension.
Cell Rep, 2022, 38(10):110468
S5432 Dibenamine Hydrochloride Dibenamine (N-(2-Chloroethyl)dibenzylamine, Sympatholytin, Dibenzylchlorethamine) is an irreversible blocker of α1 adrenoceptors.
S5540 Landiolol hydrochloride Landiolol hydrochloride (ONO-1101) is the hydrochloride salt form of Landiolol, which is an ultra-short-acting β1 selective adrenoceptor antagonist.
S5666 Moxisylyte hydrochloride Moxisylyte hydrochloride (thymoxamine) is an alpha-adrenergic blocking agent used for the treatment of Raynaud's disease.
S5766 Alfuzosin Alfuzosin(SL 77499), a quinazoline derivative, is a selective and competitive α1-adrenoceptor antagonist.
S5778 Esmolol Esmolol is a cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
S5780 Prazosin Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors. It is used to treat hypertension.
BMC Pharmacol Toxicol, 2020, 21(1):61
S5782 Doxazosin Doxazosin(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
S5789 Propafenone Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias.
S5802 Alprenolol hydrochloride Alprenolol hydrochloride is the hydrochloride salt form of alprenolol, which is an beta adrenergic receptorantagonist and is used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
S5923 Celiprolol hydrochloride Celiprolol is a β1-adrenoceptor antagonist with partial β2 agonist activity.
S5942 Bisoprolol Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
S5965 Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S5981 S(-)-Propranolol hydrochloride (S)-(-)-Propranolol hydrochloride, the active enantiomer of propranolol, is a β-Adrenoceptor (β-Adrenergic Receptor) antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively.
S6447 Carazolol Carazolol is a non-specific β-adrenergic receptor blocking agent and binds to β receptors irreversibly.
S7538 RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S8114 ICI-118551 Hydrochloride ICI-118551 is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
Biomedicines, 2022, 10(2)487
Toxicol In Vitro, 2021, 77:105251
iScience, 2021, 24(12):103362
S9050 Boldine Boldine, isolated from Peumus boldus, has alpha-adrenergic antagonist activities in vascular tissue with anti-oxidant, hepatoprotective, cytoprotective, antipyretic and anti-inflammatory effects.
S9285 Fargesin Fargesin is a neolignan isolated from Magnolia plants. It is a potential β1AR antagonist through cAMP/PKA pathway.
E0450New Clenbuterol Hydrochloride

Clenbuterol (CST-103) Hydrochloride is a potent and selective adrenergic beta 2-receptor agonist.

Cell Death Dis, 2022, 13(6):571
S0032 Batefenterol  Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.
S1437 Tizanidine HCl Tizanidine HCl (DS 103-282) is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
Drug Metab Dispos, 2021, 49(8):638-647
S2020 Formoterol Hemifumarate Formoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316,Formoterol fumarate) is a potent, selective and long-acting β2-adrenoceptor agonist used in the management of asthma and chronic obstructive pulmonary disease(COPD).
S2083 Procaterol HCl Procaterol HCl (OPC-2009) is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
S2090 Dexmedetomidine HCl Dexmedetomidine HCl((+)-Medetomidine Hydrochloride) is a highly selective and potent alpha-2 adrenoceptor agonist, which reduces anesthetic requirements for patients by providing significant sedation.
Oral Dis, 2022, 10.1111/odi.14286
JHEP Rep, 2021, 3(4):100296
Sci Rep, 2021, 11(1):13345
S2092 Detomidine HCl Detomidine HCl(MPV 253AII) produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors.
Nature, 2018, 560(7718):372-376
S2304 Gramine Gramine (Donaxine) is a natural indole alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50 of 3.2 µM and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist.
S2362 Synephrine Synephrine (Oxedrine), a natural protoalkaloid in the extract of bitter orange and other citrus species, is commonly used for weight loss.
S2438 Synephrine HCl SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) agonist.
S2458 Clonidine HCl Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
Mol Pain, 2022, 18:17448069221107810
S2507 Salbutamol Sulfate Salbutamol Sulfate (Albuterol, Ventolin, Aerolin, Ventorlin, Asthalin, Asthavent) is a short-acting β2-adrenergic receptor agonist with an IC50 of 8.93 µM.
Front Physiol, 2022, 13:800055
cell, 2020, 180(1):64-78.e16
Sci Signal, 2020, 13(659)eaax0273
S2516 Xylazine HCl Xylazine(BAY 1470 hydrochloride) is an α2-Adrenergic receptor agonist, used as a sedative and muscle relaxant.
Eur J Pharmacol, 2021, 911:174522
Fitoterapia, 2021, 152:104922
STAR Protoc, 2021, 2(4):100915
S2519 Naphazoline HCl Naphazoline HCl is an ocular vasoconstrictor and imidazoline derivative sympathomimetic amine.
S2521 Epinephrine bitartrate Epinephrine bitartrate (Adrenalinium) is an alpha- and beta-adrenergic receptor stimulator.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
J Immunother Cancer, 2021, 9(1)e001466
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2522 L-Adrenaline L-Adrenaline (Epinephrine) belongs to a group of the compounds known as catecholamines.
S2523 DL-Adrenaline DL-Adrenaline(dl-Epinephrine) is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands.
S2533 Ritodrine HCl Ritodrine HCl (NSC 291565,DU 21220, Ritodrine) is a hydrochloride salt of ritodrine which is a β-2 adrenergic receptor agonist.
S2545 Scopine Scopine(6,7-Epoxytropine) is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.
S2566 Isoprenaline (NCI-C55630) HCl Isoprenaline HCl (NCI-c55630,Isoproterenol hydrochloride) is a non-selective beta-adrenergic receptor agonist, used for the treatment of bradycardia and heart block.
BMC Cancer, 2022, 22(1):213
J Dairy Sci, 2022, 105(8):6997-7010
PLoS Pathog, 2020, 16;16(3):e1008341
S2569 Phenylephrine (NCI-C55641) HCl Phenylephrine HCl (NCI-c55641,Phenylephrine hydrochloride,(R)-(-)-Phenylephrine hydrochloride, L-Phenylephrine hydrochloride) is a selective α1-adrenergic receptor agonist, used primarily as a decongestant.
Oxid Med Cell Longev, 2021, 2021:7848027
Front Pharmacol, 2019, 10:465
Sci Adv, 2019, 5(5):eaau0495
S2576 Xylometazoline HCl Xylometazoline is an α-adrenoceptor agonist commonly used as nasal decongestant, exhibits highest potency at α2B-adrenoceptor subtype with EC50 of 99 μM.
S2615 Noradrenaline bitartrate monohydrate Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
S3041 Droxidopa Droxidopa (L-DOPS) is a psychoactive drug and acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
S3060 Medetomidine HCl Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
Micromachines, 2018, 9(6)
S3061 Epinephrine HCl Epinephrine HCl (Adrenaline) is a hormone and a neurotransmitter.
J Immunother Cancer, 2021, 9(1)e001466
S3075 Dexmedetomidine Dexmedetomidine is a sedative medication used by intensive care units and anesthetists.
Neural Plast, 2022, 2022:1353778
Oral Dis, 2022, 10.1111/odi.14286
JHEP Rep, 2021, 3(4):100296
S3083 Indacaterol Maleate Indacaterol (QAB149) is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor.
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
S3185 Adrenalone HCl Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.
S3294 Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
S3640 Methoxyphenamine Hydrochloride Methoxyphenamine Hydrochloride (2-methoxy-N-methylamphetamine, OMMA) is a β-adrenergic receptor agonist of the amphetamine class used as a bronchodilator.
S3727 Vilanterol Trifenate Vilanterol trifenatate (GW642444M) is a novel inhaled long-acting beta2 adrenoceptor agonist with inherent 24-hour activity for once daily treatment of COPD and asthma.
Toxicol In Vitro, 2021, 77:105251
J Neuroimmunol, 2019, 332:37-48
S3960 Higenamine hydrochloride Higenamine (Norcoclaurine, (+-)-Demethylcoclaurine), also known as Norcoclaurine HCl, is a non-selective β2 adrenoceptor agonist which is a chemical compound naturally occurring in a number of plants.
Oncol Rep, 2021, 46(3)202
Mol Cell Biochem, 2021, 10.1007/s11010-021-04197-z
S4009 Mirabegron Mirabegron (YM 178) is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S4043 Tetrahydrozoline HCl Tetrahydrozoline (Tetryzoline) HCl is an imidazoline derivative with alpha receptor agonist activity.
S4065 Guanabenz Acetate Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.
Cell Stem Cell, 2020, 27(6):876-889.e12
Thyroid, 2019, 29(6):809-823
S4127 Terbutaline Sulfate Terbutaline Sulfate(Terbutaline hemisulfate) is a selective β2-adrenergic receptor agonist with IC50 of 53 nM.
BMC Pharmacol Toxicol, 2020, 21(1):61
Hum Reprod, 2016, 31(11):2506-2519
S4135 Clorprenaline HCl Clorprenaline HCl (NSC 334693) is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
S4266 Brimonidine Tartrate Brimonidine Tartrate(UK 1434 Tartrate) is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.
S4277 Bambuterol HCl Bambuterol HCl(Bambuterol hydrochloride,KWD-2183 hydrochloride) is a potent β-adrenoceptor agonist, used in the treatment of asthma.
S4296 Salmeterol Xinafoate Salmeterol Xinafoate(GR 33343X xinafoate,Salmetedur) is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.
ACS Pharmacol Transl Sci, 2019, 2(3):148-154
Commun Biol, 2018, 1:106
S4481 Guanabenz Guanabenz (GBZ, GA, Wytensin, Wy-8678,BR-750) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.
S4485 Olodaterol (BI 1744) Olodaterol (BI 1744) is a long-acting β2-adrenergic receptor agonist that is used as a component of an inhalation (Tiotropium/Olodaterol) for treating patients with chronic obstructive pulmonary disease (COPD).
S4693 Guanfacine Hydrochloride Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.
S5217 Arformoterol Tartrate Arformoterol Tartrate is the tartrate salt of arformoterol, a long-acting beta-2 adrenergic agonist with bronchodilator activity.
S5267 Nylidrin Hydrochloride Nylidrin Hydrochloride (Buphenine), a β-adrenergic agonist, is used therapeutically for its vasodilating effect on the peripheral circulation and possibly on the cerebral circulation as well.
S5494 Salbutamol Salbutamol (Albuterol) is a short-acting, selective beta2-adrenergic receptor agonist used to treat or prevent bronchospasm in patients with asthma, bronchitis, emphysema, and other lung diseases.
Front Physiol, 2022, 13:800055
BMC Pharmacol Toxicol, 2020, 21(1):61
S5527 Salmeterol Salmeterol (Astmerole, GR-33343X, SN408D) is a long-acting beta2-adrenergic receptor agonist with Ki value of 1.5 nM for WT β2AR and shows very high selectivity for the WT β2AR(β1Ki/β2Ki ratio of approximately 1500).
Front Pharmacol, 2022, 13:865715
Mol Syst Biol, 2021, 17(8):e10239
Drug Test Anal, 2020, 10.1002/dta.2917
S5537 Tizanidine Tizanidine is an imidazoline derivative and a centrally acting α2 adrenergic agonist used as a muscle relaxant for therapy of acute muscle spasms and chronic spasticity.
Drug Metab Dispos, 2021, 49(8):638-647
S5564 Xylazine Xylazine is a partial alpha-2 adrenergic agonist that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals.
Cell Death Differ, 2020, 10.1038
Mol Med Rep, 2017, 16(2):1911-1919
S5654 Indacaterol Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor.
Drug Test Anal, 2020, 10.1002/dta.2917
J Neuroimmunol, 2019, 332:37-48
S5669 Isoxsuprine hydrochloride Isoxsuprine hydrochloride is a beta-adrenergic agonist with vasodilator activity.
S5683 Isoproterenol sulfate dihydrate Isoproterenol Sulfate is the sulfate salt form of isoproterenol, a beta-adrenergic receptor agonist with bronchodilator activity.
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
Biochim Biophys Acta Mol Cell Res, 2021, 1868(10):119080
S5727 Tetryzoline Tetryzoline (Tetrahydrozoline) is an alpha-adrenergic agonist used in some over-the-counter eye drops and nasal sprays.
S5734 Midodrine hydrochloride Midodrine hydrochloride is the hydrochloride salt form of midodrine, an adrenergic alpha-1 agonist used as a vasopressor.
S5735 Midodrine Midodrine belongs to the class of medications known as vasopressors. It is an adrenergic alpha-1 agonist.
S5750 DL-Norepinephrine hydrochloride Norepinephrine (noradrenaline) is the neurotransmitter at most sympathetic neuroeffector junctions and has pharmacologic effects on both α1 and β1 adrenoceptors.
S5768 Fenoterol hydrobromide Fenoterol hydrobromide (Phenoterol) is the the hydrobromide salt of fenoterol, a β2 adrenoreceptor agonist with bronchodilator activity.
Toxicol In Vitro, 2021, 77:105251
S5769 Fenoterol Fenoterol (Phenoterol) is a β2 adrenoreceptor agonist with bronchodilator activity.
S5925 Olodaterol hydrochloride Olodaterol hydrochloride (BI-1744) is the hydrochloride salt form of Olodaterol, which is a long-acting beta2-adrenergic agonist.
S5954 L-(-)-α-Methyldopa hydrate L-(-)-α-Methyldopa (Methyldopa, MK-351) hydrate, a potent antihypertensive drug, is a selective agonist for α2-adrenergic receptors.
S6487 fluticasone furoate Fluticasone furoate (GW685698) is an inhaled corticosteroid/long-acting beta-agonist combination with a prolonged bronchodilator duration of action. It is used for the treatment of non-allergic and allergic rhinitis administered by a nasal spray.
S6583 Apraclonidine HCl Apraclonidine (Iopidine,ALO 2145) is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist.
S7974 L755507 L-755,507 is characterized as a potent and selective β3 adrenergic receptor partial agonist with EC50 of 0.43 nM. It is also recently identified to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs) and other cell types.
Genesis, 2022, 60(1-2):e23465
Chembiochem, 2021, 22(20):2957-2965
Hum Mutat, 2019, 10.1002/humu.23848
S9507 (−)-Norepinephrine (−)-Norepinephrine (Arterenol, Levarterenol, L-Noradrenaline) is a natural neurotransmitter and hormone. It is an agonist of adrenergic receptors with Ki values of 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively.
Commun Biol, 2022, 5(1):339
Eur J Pharmacol, 2022, 926:175040
Cardiovasc Drugs Ther, 2020, 11
S9508 Brimonidine Brimonidine (Bromoxidine, UK 1430) is an alpha adrenergic receptor agonist (primarily alpha-2) and is used for the treatment of open-angle glaucoma or ocular hypertension to lower intraocular pressure.
S3153 Levalbuterol tartrate Levalbuterol HCl(Levosalbutamol tartrate) is a relatively selective beta2-adrenergic receptor agonist used for the treatment of asthma.
E0949New Mebicar Mebicar, a derivative of bicyclic bis-ureas, inhibits the orientation reaction in albino mice, potentiates the action of narcotic hypnotics, abolishes the conditioned reflex reaction of avoidance, displays central adrenolytic activity, interferes with the norepinephrine metabolism in the brain stem.
S9470New Penbutolol Sulfate Penbutolol sulfate ((-)-Terbuclomine) is an effective beta-adrenergic receptor blocker and diuretic that is used as an antihypertensive agent.
E0785New YS-49 YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
E0408New JP1302 JP-1302(MMV006172), a novel highly selective α2C-adrenoceptor antagonist with Kb of 16 nM at the α2C-adrenoceptor subtype, also produces antidepressant and antipsychotic-like effects. 
E0529New Metipranolol Metipranolol (Betamann) is potent β-adrenergic receptor antagonist, possessing the beta-blocking potencies (pA2) of 8.3, 8.4 at guinea pig atrial β1-adrenoceptor and β2-adrenoceptor of the rat uterus, respectively, also is a potent displacer of 3H-DHA binding, ligand concentration 0.7 nM, possessing a Ki value of 39 ± 24 nM.
S2174New Hydroxyflutamide (Hydroxyniphtholide) Hydroxyflutamide (SCH-16423, Hydroxyniphtholide) is an androgen receptor (AR) antagonist and possesses an IC50 of 0.7 μM for the androgen receptor.
E0450New Clenbuterol Hydrochloride

Clenbuterol (CST-103) Hydrochloride is a potent and selective adrenergic beta 2-receptor agonist.

Cell Death Dis, 2022, 13(6):571
Tags: adrenergic receptor activation | adrenergic receptor types | adrenergic receptor location | adrenergic receptor drugs | adrenergic receptor signaling | adrenergic receptor pathway | beta adrenergic receptor pathway | beta adrenergic receptor activation | beta 2 adrenergic receptor activation | beta 2 adrenergic receptor pathway | alpha adrenergic receptor pathway | alpha 1 adrenergic receptor pathway | beta 1 adrenergic receptor pathway | adrenergic receptor inhibitor review