Home Endocrinology & Hormones Adrenergic Receptor

Adrenergic Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Gastroenterology, 2024, 167(5):993-1007
J Immunother Cancer, 2024, 12(11)e009805
Antioxidants (Basel), 2023, 12(8)1585
S8114 Zenidolol (ICI-118551) Hydrochloride Zenidolol (ICI-118551) Hydrochloride 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.
Immunity, 2025, S1074-7613(25)00226-2
J Immunother Cancer, 2025, 13(6)e011611
Biomedicines, 2022, 10(2)487
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.
Pharmaceuticals (Basel), 2025, 18(2)181
Drug Metab Dispos, 2025, 53(4):100049
BMC Pharmacol Toxicol, 2024, 25(1):25
S1549 Nebivolol hydrochloride (R-65824) Nebivolol HCl (R-65824) selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
J Biol Chem, 2025, 301(7):110305
J Immunother Cancer, 2024, 12(11)e009805
Oncogenesis, 2022, 11(1):24
S2509 Sotalol HCl Sotalol(MJ-1999) is a non-selective beta blocker and a potassium channel blocker with an IC50 of 43 μM.
Circulation, 2024, 150(7):563-576
J Immunother Cancer, 2024, 12(11)e009805
EBioMedicine, 2023, 95:104741
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.
Front Pharmacol, 2024, 15:1431758
Anesth Analg, 2023, 137(2):426-39
Mol Pain, 2022, 18:17448069221107810
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.
J Immunother Cancer, 2024, 12(11)e009805
Int J Mol Sci, 2024, 25(18)10162
Sci Rep, 2024, 14(1):4178
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.
Biomed Pharmacother, 2024, 177:117038
Exp Mol Med, 2020, 10.1038/s12276-020-0461-6
Nitric Oxide, 2019, 85:1-9
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.
Pharmaceuticals (Basel), 2025, 18(2)181
Drug Metab Dispos, 2025, 53(4):100049
Int J Mol Sci, 2022, 23(21)12948
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.
J Physiol Sci, 2025, 75(2):100016
J Immunother Cancer, 2024, 12(11)e009805
BMC Pharmacol Toxicol, 2020, 21(1):61
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.
bioRxiv, 2025, 2025.04.03.647018
J Immunother Cancer, 2024, 12(11)e009805
J Biomed Sci, 2021, 28(1):8
S1409 Alfuzosin HCl Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
J Immunother Cancer, 2024, 12(11)e009805
Prostate, 2016, 76(8):757-66
Verified customer review of Alfuzosin HCl
S2059 Terazosin HCl Dihydrate Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
J Physiol Sci, 2025, 75(2):100016
J Biomed Sci, 2021, 28(1):8
S2517 Maprotiline HCl Maprotiline HCl is a selective noradrenalin re-uptake inhibitor, used in the treatment of depression.
Ann Hematol, 2025, 10.1007/s00277-025-06571-z
Front Pharmacol, 2021, 12:689767
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.
J Physiol Sci, 2025, 75(2):100016
Cell Syst, 2019, 8(2):97-108
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 Immunother Cancer, 2024, 12(11)e009805
J Dermatolog Treat, 2020, 24:1-7
S1827 Betaxolol HCl Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM.
J Immunother Cancer, 2024, 12(11)e009805
Chirality, 2018, 30(11):1195-1205
S4124 Tolazoline HCl Tolazoline(Imidaline hydrochloride,NSC35110 hydrochloride) is a non-selective competitive α-adrenergic receptor antagonist.
J Immunother Cancer, 2024, 12(11)e009805
Insect Biochem Mol Biol, 2017, 90:61-70
S5023 Nadolol Nadolol (Corgard, Solgol, Anabet, SQ11725) is a non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities.
J Chromatogr A, 2024, 1734:465286
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
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
S1613 Silodosin Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.
J Immunother Cancer, 2024, 12(11)e009805
S1856 Metoprolol Tartrate Metoprolol Tartrate (CGP 2175E) is a selective β1 receptor blocker medication, used to treat hypertension and heart failure.
J Immunother Cancer, 2024, 12(11)e009805
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
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.
J Immunother Cancer, 2024, 12(11)e009805
S5666 Moxisylyte hydrochloride Moxisylyte hydrochloride (thymoxamine) is an alpha-adrenergic blocking agent used for the treatment of Raynaud's disease.
J Immunother Cancer, 2024, 12(11)e009805
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.
J Pathol, 2022, 10.1002/path.6020
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
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.
Heliyon, 2024, 10(11):e31865
E2901 (-)-Isoproterenol hydrochloride (-)-Isoproterenol hydrochloride is an agonist of the beta-adrenergic receptor. This compound is also used in the treatment of bradycardia; bronchodilator.
Stem Cell Res Ther, 2022, 13(1):287
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
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.
J Immunother Cancer, 2024, 12(11)e009805
E5827 Propranolol Propranolol is a non-selective antagonist of β-adrenergic receptors (βAR), with Ki values of 1.8 nM for β1AR and 0.8 nM for β2AR, effectively lowering cAMP levels and activating the MAPK pathway downstream of βARs. It is an effective treatment for infantile hemangiomas (IHs), where it induces antiproliferative and antisurvival effects on hemangioma stem cells (HemSCs).
Pharmaceuticals (Basel), 2025, 18(2)181
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.
UNIVERSITY OF PÉCS, 2023,
S4100 Esmolol HCl Esmolol (ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms.
J Immunother Cancer, 2024, 12(11)e009805
S4278 Carteolol HCl Carteolol HCl(Carteolol hydrochloride,OPC-1085 hydrochloride) is a β-adrenoceptor antagonist, used for the treatment of glaucoma.
J Immunother Cancer, 2024, 12(11)e009805
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.
J Immunother Cancer, 2024, 12(11)e009805
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.
S2499 Phenoxybenzamine HCl Phenoxybenzamine HCl (NSC 37448, NCI-c01661) is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM.
E6046 phentolamine hydrochloride Phentolamine hydrochloride is a potent, selective, and orally active antagonist of α1 and α2 adrenergic receptors , with pKi values of 8.8, 8.0, and 8.3 for the human α2A, α2B, and α2C adrenergic receptors, respectively. It also shows binding affinities for the α1-adrenoceptor subtypes, exhibiting Ki values of 6.1 nM for cloned α1A/D, 39.8 nM for α1B, and 2.8 nM for α1C.
S5540 Landiolol hydrochloride Landiolol hydrochloride (ONO-1101) is the hydrochloride salt form of Landiolol, which is an ultra-short-acting β1 selective adrenoceptor antagonist.
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.
S5766 Alfuzosin Alfuzosin(SL 77499), a quinazoline derivative, is a selective and competitive α1-adrenoceptor antagonist.
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.
E2875 Levobunolol(l-Bunolol) hydrochloride Levobunolol (l-Bunolol) hydrochloride is a potent and nonselective β-adrenergic receptor antagonist with an IC50 of 48 μM.
E6035 (R)-Propranolol hydrochloride (R)-Propranolol (hydrochloride) (Dexpropranolol hydrochloride) is a nonselective antagonist of beta-adrenergic receptor (β-adrenergic receptor (βAR) ) that competitively blocks the action of epinephrine (EPI) and norepinephrine (NE) on β1- and β2-adrenoreceptors (AR). It exhibits anti-neuroblastoma activity and is effective in combination therapies for relapsed and refractory neuroblastoma patients.
S9285 Fargesin Fargesin is a neolignan isolated from Magnolia plants. It is a potential β1AR antagonist through cAMP/PKA pathway.
S5965 Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
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.
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.
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.
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.
S1435 Tamsulosin hydrochloride Tamsulosin (Flomax) hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
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.
E0408 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. 
E4880 Labetalol Labetalol (AH5158, Sch-15719W free base) is an orally active and selective competitive antagonist of α1-adrenergic receptors and non-selective β-adrenergic receptors. This compound, an anti-hypertensive agent is used in the research of cardiovascular diseases.
E6048New (S)-Terazosin (S)-Terazosin is a potent and selective antagonist of α-adrenoceptor with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. It also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively. It may prove to be a useful probe in understanding the functional role of subtypes of adrenoceptors in various tissues.
S5782 Doxazosin Doxazosin(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
S2174 Hydroxyflutamide (Hydroxyniphtholide) Hydroxyflutamide (SCH-16423, Hydroxyniphtholide) is an androgen receptor (AR) antagonist and possesses an IC50 of 0.7 μM for the androgen receptor.
S5923 Celiprolol hydrochloride Celiprolol is a β1-adrenoceptor antagonist with partial β2 agonist activity.
S6447 Carazolol Carazolol is a non-specific β-adrenergic receptor blocking agent and binds to β receptors irreversibly.
E6056New (R)-tamsulosin (R)-Tamsulosin ((R)-(-)-YM12617 free base, LY253351 free base) is the enantiomerically pure, pharmacologically active form of tamsulosin, a selective α₁A-adrenergic receptor antagonist used in the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS). This form is synthesized using chiral N-(1-phenylethyl)aziridine-2-carboxylate derivatives, which allow for highly stereoselective processes in its production.
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.
S5432 Dibenamine Hydrochloride Dibenamine (N-(2-Chloroethyl)dibenzylamine, Sympatholytin, Dibenzylchlorethamine) is an irreversible blocker of α1 adrenoceptors.
E6004 Metipranolol hydrochloride Metipranolol hydrochloride is a non-selective antagonist of β-adrenoceptor. It also inhibits iron/ascorbate and sodium nitroprusside-induced lipid peroxidation with an IC50 of 6.9 µM and 25.1 µM respectively. It exhibits antioxidant properties and can be used in research to lower elevated intraocular pressure associated with glaucoma.
E0529 Metipranolol Metipranolol (Betamann) is a 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.
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.
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.
J Adv Res, 2024, S2090-1232(24)00079-1
Cell Commun Signal, 2024, 22(1):266
Mol Cancer, 2023, 22(1):136
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. This compound also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. It is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Mol Metab, 2025, 91:102069
Oncogenesis, 2025, 14(1):31
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S3656 Piribedil Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. This compound also has α2-adrenergic (α2A/α2C) antagonist properties.
Cell Rep Methods, 2023, 3(1):100381
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.
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.
S5789 Propafenone Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. This compound offers a broad spectrum of activity in the treatment of cardiac arrhythmias.It can be used to induce animal models of Heart Failure.