| S1206 |
Bisoprolol fumarate
|
Bisoprolol fumarate (EMD33512) is a selective type β1 adrenergic receptor blocker.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
J Pathol, 2022, 10.1002/path.6020
-
Frontiers in Nutrition, 2022, 907986
|
|
| S2507 |
Salbutamol (Albuterol) Sulfate
|
Salbutamol (Albuterol) Sulfate is a short-acting β2-adrenergic receptor agonist with an IC50 of 8.93 µM.
|
-
Front Pharmacol, 2025, 16:1621775
-
Front Physiol, 2022, 13:800055
-
cell, 2020, 180(1):64-78.e16
|
|
| 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 Physiol Sci, 2025 Mar 28, 100016
-
J Physiol Sci, 2025, 75(2):100016
-
J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z
|
|
| S1549 |
Nebivolol hydrochloride (R-65824)
|
Nebivolol HCl (R-65824) selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
|
-
Molecular Cancer Research, 2025 Mar 3, 236-249
-
Journal of Biological Chemistry, 2025, 110305
-
J Biol Chem, 2025, 301(7):110305
|
|
| 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.
|
-
Communications Medicine, October 2025, 5(1)
-
Anticancer Research, December 2021, 6179-6190
-
Communications Medicine, 2025, 420
|
|
| 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.
|
-
Cancer Discovery, 2025, CD-24-0287
-
Drug Delivery, 2025, 2585612
-
British Journal of Anaesthesia, 2023, 142-153
|
|
| 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.
|
-
Neurotherapeutics, October 2023, 1779-1795
-
Molecular Cancer Research, March 3, 2025, 236-249
-
International Journal of Biological Sciences, March 25, 2026, 3617-3634
|
|
| 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.
|
-
Human Mutation, November 15, 2019, 2044-2056
-
Frontiers in Cell and Developmental Biology, January 25, 2024, 11:1276890
-
Frontiers in Cell and Developmental Biology, January 25, 2024, 1276890
|
|
| 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 & Disease, 2023, 318
-
Cell Death Dis, 2023, 14(5):318
-
STAR Protocols, 2021, 100915
|
|
| 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 HCl (Antagonil) is an α2-adrenergic receptor antagonist. It also produces an antidiuretic effect, and increases heart rate and blood pressure. Yohimbine HCl (Antagonil) is useful in treating erectile dysfunction.
|
-
Front Pharmacol, 2024, 15:1431758
-
Anesth Analg, 2023, 137(2):426-39
-
Mol Pain, 2022, 18:17448069221107810
|
|
| 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.
|
-
Nature Communications, October 06, 2025, 8870
-
ACS Pharmacology & Translational Science, 2024 Dec 29, 8(1):245-255
-
Front Physiol, 2022, 13:800055
|
|
| 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.
|
-
Oncology Reports, July 23, 2021, 202
-
J Immunother Cancer, 2024, 12(11)e009805
-
Int J Mol Sci, 2024, 25(18)10162
|
|
| 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.
|
-
Biomed Pharmacother, 2025, 187:118100
-
Gut, 2024, 1984-1998
-
Theranostics, 2024, 593-607
|
|
| 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.
|
-
Drug Delivery, November 26, 2025, 2585612
-
Oncology Reports, July 23, 2021, 202
-
Pharmaceuticals (Basel), 2025, 18(2)181
|
|
| 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.
|
-
American Journal of Physiology-Cell Physiology, January 2023, C133-C141
-
American Journal of Physiology-Cell Physiology, January 1, 2023, C133-C141
-
bioRxiv, 2024, nan
|
|
| S4124 |
Tolazoline HCl
|
Tolazoline(Imidaline hydrochloride,NSC35110 hydrochloride) is a non-selective competitive α-adrenergic receptor antagonist.
|
-
Cancer Biology & Medicine, January 15, 2022, 74-89
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cancer Biology & Medicine, 2022, 74-89
|
|
| 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.
|
-
Frontiers in Neurology, September 27, 2019, 1041
-
Experimental & Molecular Medicine, July 06, 2020, 1062-1074
-
Biomed Pharmacother, 2024, 177:117038
|
|
| 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.
|
-
J Cell Mol Med, 2025, 29(1):e70335
-
Journal of Allergy and Clinical Immunology, 2022 Feb, 671-684.e9
-
Drug Test Anal, 2020, 10.1002/dta.2917
|
|
| 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
-
Journal of Biomedical Science, 2021, 8
|
|
| S5780 |
Prazosin
|
Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors. It is used to treat hypertension.
|
-
Communications Medicine, 2025, 420
-
Analytical Chemistry, 2024, 1547-1555
-
Anticancer Research, 2021, 6179-6190
|
|
| 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).
|
-
Oncology Letters, 2025 Dec 15, 75
-
Korean Circ J, 2024, 54(4):172-186
-
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
|
|
| 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.
|
-
ERJ Open Research, September 2025, 00342-2025
-
Anticancer Research, December 2021, 6179-6190
-
ERJ Open Research, 2025, 00342-2025
|
|
| S1613 |
Silodosin
|
Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.
|
-
Communications Medicine, 2025, 5:1
-
J Immunother Cancer, 2024, 12(11)e009805
-
bioRxiv, 2023, 2023.07.12.548707
|
|
| S2458 |
Clonidine HCl
|
Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
|
-
J Control Release, 2025, 379:120-134
-
J Immunother Cancer, 2024, 12(11)e009805
-
Molecular Pain, 2022 Apr, 17448069221107810
|
|
| S3041 |
Droxidopa
|
Droxidopa (L-DOPS) is a psychoactive drug and acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
|
-
Nature Metabolism, 2026, 96-115
-
Science Translational Medicine, 2024, 16(738):eadg3665
-
Science Translational Medicine, 2024, eadg3665
|
|
| 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
-
Pharmaceutical Research, 2024, 557–566
-
Frontiers in Pharmacology, 2022, 1049640
|
|
| S2059 |
Terazosin HCl Dihydrate
|
Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
|
-
The Journal of Physiological Sciences, 2025, 100016
-
J Physiol Sci, 2025, 75(2):100016
-
Journal of Biomedical Science, 2021, 8
|
|
| S2517 |
Maprotiline HCl
|
Maprotiline HCl is a selective noradrenalin re-uptake inhibitor, used in the treatment of depression.
|
-
Annals of Hematology, September 2, 2025, 5841-5854
-
Annals of Hematology, September 02, 2025, 5841-5854
-
Frontiers in Pharmacology, May 20, 2021, 689767
|
|
| 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
-
British Journal of Pharmacology, 2019 Mar, 176(6):801-813
-
British Journal of Pharmacology, 2019 Mar, 801-813
|
|
| S3061 |
Epinephrine HCl
|
Epinephrine HCl (Adrenaline) is a hormone and a neurotransmitter.
|
-
Cell Rep Methods, 2023, 3(10):100599
-
J Immunother Cancer, 2021, 9(1)e001466
-
Journal for ImmunoTherapy of Cancer, 2021, e001466
|
|
| S1437 |
Tizanidine HCl
|
Tizanidine HCl (DS 103-282) is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
|
-
bioRxiv, July 13, 2023, 2023.07.12.548707
-
Communications Medicine, 2025, 420
-
Drug Metab Dispos, 2021, 49(8):638-647
|
|
| S1827 |
Betaxolol HCl
|
Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
Journal for ImmunoTherapy of Cancer, 2024, e009805
-
Nature Communications, 2020, 1990
|
|
| 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
|
|
| S4127 |
Terbutaline Sulfate
|
Terbutaline Sulfate(Terbutaline hemisulfate) is a selective β2-adrenergic receptor agonist with IC50 of 53 nM.
|
-
International Journal of Molecular Sciences, 2022, 12657
-
BMC Pharmacol Toxicol, 2020, 21(1):61
-
BMC Pharmacology and Toxicology, 2020, 61
|
|
| S5683 |
Isoproterenol sulfate dihydrate
|
Isoproterenol Sulfate is the sulfate salt form of isoproterenol, a beta-adrenergic receptor agonist with bronchodilator activity.Isoproterenol sulfate dihydrate can be used to induce animal models of Angina Pectoris.
|
-
Stem Cell Res Ther, 2022, 13(1):287
-
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
-
Biochim Biophys Acta Mol Cell Res, 2021, 1868(10):119080
|
|
| S5766 |
Alfuzosin
|
Alfuzosin(SL 77499), a quinazoline derivative, is a selective and competitive α1-adrenoceptor antagonist.
|
-
Journal of Medicinal Chemistry, December 5, 2025, nan
-
Prostate, 2016, 757-766
-
Doctoral Thesis, Bond University, 2016, 69
|
|
| 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.
|
-
Pharmaceuticals, 2025, 181
-
Heliyon, 2024, 10(11):e31865
-
Heliyon, 2024, 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 Research & Therapy, 2022, 287
-
Stem Cell Res Ther, 2022, 13(1):287
-
BMC Cancer, 2022, 213
|
|
| 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.
|
-
Doctoral Thesis, University of Pécs, 2023, nan
-
UNIVERSITY OF PÉCS, 2023,
-
Journal of Pharmacology and Experimental Therapeutics, 2016, 73-81
|
|
| 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.
|
-
bioRxiv, December 08, 2024, nan
-
Cell Rep, 2022, 38(10):110468
-
Doctoral dissertation, Boston University, 2020, nan
|
|
| S2091 |
Betaxolol
|
Betaxolol (SL 75212,Dextrobetaxolol) is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
|
-
Translational Psychiatry, 2023, 324
-
Nat Commun, 2020, 24;11(1):1990
-
Nature Communications, 2020, 1990
|
|
| 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
-
The Prostate, 2016, 757-766
|
|
| S2522 |
L-Adrenaline
|
L-Adrenaline (Epinephrine) belongs to a group of the compounds known as catecholamines.This compound can be used to induce animal models of Arrhythmias.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
Journal for ImmunoTherapy of Cancer, 2021, e001466
|
|
| 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
|
|
| S3060 |
Medetomidine HCl
|
Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
|
-
Research Square (Preprint), 2026, Preprint
-
Micromachines, 2018, 9(6)
|
|
| S2092 |
Detomidine HCl
|
Detomidine HCl(MPV 253AII) produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
Nature, 2018, 372-376
-
Nature, 2018, 560(7718):372-376
|
|
| 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.
|
-
Communications Medicine, October 09, 2025, 420
-
Communications Medicine, 2025, 420
-
Drug Metab Dispos, 2021, 49(8):638-647
|
|
| 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.
|
-
Oncology Reports, July 23, 2021, 202
-
Mol Cell Biochem, 2021, 10.1007/s11010-021-04197-z
-
Oncol Rep, 2021, 46(3)202
|
|
| 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
-
Skeletal Muscle, 2017, 16
|
|
| 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
|
|
| E8311New |
Isoprenaline
|
Isoprenaline is a synthetic, non-selective agonist of beta-adrenergic receptor and is used for the treatment of bradycardia, heart block, and congestive heart failure.
|
-
Animal Nutrition, July 12, 2025, 1-16
-
BMC Cancer, February 26, 2022, 213
-
BMC Cancer, 2022, 213
|
|
| S4693 |
Guanfacine Hydrochloride
|
Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.
|
-
bioRxiv, 2025, nan
-
J Immunother Cancer, 2024, 12(11)e009805
|
|
| E2944 |
Norepinephrine hydrochloride
|
Norepinephrine (Levarterenol; L-Noradrenaline) hydrochloride is a potent agonist of adrenergic receptor (AR). Norepinephrine activates α1, α2, β1 receptors.
|
-
Clinical Science, July 31 2020, 1957-1971
-
BMC Nephrology, August 29 2025, 498
-
BMC Nephrology, 2025, 498
|
|
| 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
|
|
| 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.
|
-
Skeletal Muscle, September 4, 2017, 16
-
ACS Omega, March 1, 2023, 9302-9316
|
|
| 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.
|
-
ACS Pharmacology & Translational Science, 2025, 245-255
-
Front Pharmacol, 2025, 16:1621775
-
Frontiers in Pharmacology, 2025, 1621775
|
|
| S3185 |
Adrenalone HCl
|
Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
Skeletal Muscle, 2017, 16
|
|
| 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.
|
-
Journal of Allergy and Clinical Immunology, 2022 Feb, 671-684.e9
-
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
|
|
| 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
|
|
| S3153 |
Levalbuterol tartrate
|
Levalbuterol tartrate(Levosalbutamol tartrate) is a relatively selective beta2-adrenergic receptor agonist used for the treatment of asthma.
|
-
J Immunother Cancer, 2024, 12(11)e009805
|
|
| 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. This compound stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
|
-
Signal Transduct Target Ther, 2024, 9(1):243
|
|
| 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
|
|
| 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.
|
-
mediaTUM (Technical University of Munich), 2020, 66
|
|
| 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
|
|
| S5734 |
Midodrine hydrochloride
|
Midodrine hydrochloride is the hydrochloride salt form of midodrine, an adrenergic alpha-1 agonist used as a vasopressor.
|
-
Anticancer Research, 2021, 6179-6190
|
|
| S9470 |
Penbutolol Sulfate
|
Penbutolol sulfate ((-)-Terbuclomine) is an effective beta-adrenergic receptor blocker and diuretic that is used as an antihypertensive agent.
|
-
Antimicrobial Agents and Chemotherapy, 2018, e00024-18
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|
| 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
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|
| 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
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| 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).
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-
Pharmaceuticals (Basel), 2025, 18(2)181
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|
| S5925 |
Olodaterol hydrochloride
|
Olodaterol hydrochloride (BI-1744) is the hydrochloride salt form of Olodaterol, which is a long-acting beta2-adrenergic agonist.
|
-
Frontiers in Pharmacology, 2025, 1621775
-
Front Pharmacol, 2025, 16:1621775
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| S6407 |
Tulobuterol hydrochloride
|
Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
|
-
Skeletal Muscle, 2017, 16
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| 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
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| E4849 |
Terbutaline
|
Terbutaline(Brican, Brethine), an active metabolite of bambuterol is an orally active agonist of β2-adrenergic receptor, that increases MKP-1 expression. This compound is used in the treatment of obstructive lung diseases as a bronchodilator remedy. It also exhibits anti-inflammatory effects.
|
-
Human Reproduction, 2016, 2506-2519
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| S4243 |
Deoxycorticosterone acetate
|
Deoxycorticosterone acetate (11-Deoxycorticosterone, DOC, Cortexone) is a steroid hormone used for intramuscular injection for replacement therapy of the adrenocortical steroid.Deoxycorticosterone acetate can be used to induce animal models of Aneurysm, Hypertension.
|
-
Nature Cancer, 2020, 235-248
-
Nat Cancer, 2020, 1(2):235-248
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| 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
|
|
| S5750 |
DL-Norepinephrine hydrochloride
|
Norepinephrine (noradrenaline) is the neurotransmitter at most sympathetic neuroeffector junctions and has pharmacologic effects on both α1 and β1 adrenoceptors.
|
-
J Ethnopharmacol, 2025, 344:119517
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Journal of Ethnopharmacology, 2025, 119517
|
|
| S2362 |
Synephrine
|
Synephrine (Oxedrine), a natural protoalkaloid in the extract of bitter orange and other citrus species, is commonly used for weight loss.
|
-
Journal of the California Dental Association, 2016 Aug, 493-498
|
|
| S2113 |
Cisatracurium Besylate
|
Cisatracurium Besylate(51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
|
-
BioScience Trends, 2021 Mar 15, 50-54
-
Biosci Trends, 2021, 15(1):50-54
-
Bioscience Trends, 2021, 50-54
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|
| 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.
|
-
British Journal of Pharmacology, 2019 Mar, 801-813
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| 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).
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|
| 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.
|
|
|
| S2519 |
Naphazoline HCl
|
Naphazoline HCl is an ocular vasoconstrictor and imidazoline derivative sympathomimetic amine.
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|
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| S2533 |
Ritodrine HCl
|
Ritodrine HCl (NSC 291565,DU 21220, Ritodrine) is a hydrochloride salt of ritodrine which is a β-2 adrenergic receptor agonist.
|
|
|
| S2438 |
Synephrine HCl
|
SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) 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.
|
|
|
| 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.
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| 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.
|
|
|
| S2523 |
DL-Adrenaline
|
DL-Adrenaline(dl-Epinephrine) is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands.
|
|
|
| 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.
|
|
|
| S5540 |
Landiolol hydrochloride
|
Landiolol hydrochloride (ONO-1101) is the hydrochloride salt form of Landiolol, which is an ultra-short-acting β1 selective adrenoceptor antagonist.
|
|
|
| S2615 |
Noradrenaline bitartrate monohydrate
|
Norepinephrine (Levarterenol; L-Noradrenaline) bitartrate monohydrate is a potent adrenergic receptor (AR) agonist that primarily targets α1, α2, and β1 adrenergic receptors, with Ki values of 330 nM for α1 and 56 nM for α2 receptors.
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|
|
| E4888 |
Guanabenz hydrochloride
|
Guanabenz hydrochloride(NE56490) is a small molecule, antihypertensive agonist of α2-adrenoceptor. It also inhibits eIF2α and GADD34, showing potential for treating cardiac hypertrophy, heart failure, atherosclerosis, and ischemic heart disease.
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|
| E4825 |
Naphazoline (nitrate)
|
Naphazoline (nitrate) is a agonist of peripheral α2-adrenergic receptor and used as a topical decongestant. It also acts as a vasoconstrictor that effectively reduces intraoperative bleeding and enhances postoperative analgesia. When used in conjunction with intranasal lidocaine, it significantly reduces both intra- and postoperative pain, thereby decreasing the need for rescue analgesics in the postoperative period following septorhinoplasty.
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|
| S5769 |
Fenoterol
|
Fenoterol (Phenoterol) is a β2 adrenoreceptor agonist with bronchodilator activity.
|
|
|
| S4135 |
Clorprenaline HCl
|
Clorprenaline HCl (NSC 334693) is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
|
|
|
| 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. This compound inhibits the hemodynamic responses to angiotensin II, possibly through the inhibition of alpha 1-adrenoceptor-mediated events.
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| S4043 |
Tetrahydrozoline HCl
|
Tetrahydrozoline (Tetryzoline) HCl is an imidazoline derivative with alpha receptor agonist activity.
|
|
|
| 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.
|
|
|
| E7904 |
Ritodrine
|
Ritodrine (DU21220) is a potent and selective agonist of β2-adrenergic. It rapidly inhibits recurrent uterine contractions and can be used in research to study the prevention of preterm labor and prolong pregnancy.
|
|
|
| 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.
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|
|
| S9285 |
Fargesin
|
Fargesin is a neolignan isolated from Magnolia plants. It is a potential β1AR antagonist through cAMP/PKA pathway.
|
|
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| S5965 |
Urapidil
|
Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
|
|
|
| E4963 |
Clonidine
|
Clonidine (Clonidin) is a direct-acting α2-adrenergic agonist. It is potentially used in the treatment of attention-deficit hyperactivity disorder (ADHD) in children and adolescents.
|
|
|
| S5217 |
Arformoterol Tartrate
|
Arformoterol Tartrate is the tartrate salt of arformoterol, a long-acting beta-2 adrenergic agonist with bronchodilator activity.
|
|
|
| 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.
|
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|
| S5735 |
Midodrine
|
Midodrine belongs to the class of medications known as vasopressors. It is an adrenergic alpha-1 agonist.
|
|
|
| S5727 |
Tetryzoline
|
Tetryzoline (Tetrahydrozoline) is an alpha-adrenergic agonist used in some over-the-counter eye drops and nasal sprays.
|
|
|
| S5954 |
L-(-)-α-Methyldopa hydrate
|
L-(-)-α-Methyldopa (Methyldopa, MK-351) hydrate, a potent antihypertensive drug, is a selective agonist for α2-adrenergic receptors.
|
|
|
| E4842 |
Vilanterol
|
Vilanterol (GW642444) is a potent and selective agonist of β2-adrenoceptor (β2-AR) with pEC50 of β2-AR, β1-AR, and β3-AR is 10.37, 6.98 and 7.36 respectively in cAMP detection assays.
|
|
|
| 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.
|
|
|
| S3640 |
Methoxyphenamine Hydrochloride
|
Methoxyphenamine Hydrochloride (2-methoxy-N-methylamphetamine, OMMA) is a β-adrenergic receptor agonist of the amphetamine class used as a bronchodilator.
|
|
|
| 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.
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|
|
| 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.
|
|
|
| S1423 |
Dobutamine HCl
|
Dobutamine(Dobutrex) hydrochloride is a selective potent agonist of β1-AR (β-1 adrenergic receptor) and exhibits weak activity at α1-AR and β2-AR. Dobutamine is a sympathomimetic compound that effectively restores blood pressure in hypotensive dogs and human patients by improving myocardial contractility and increasing cardiac output (CO).
|
|
|
| S6583 |
Apraclonidine HCl
|
Apraclonidine (Iopidine,ALO 2145) is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist.
|
|
|
| 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.
|
|
|
| S4485 |
Olodaterol
|
Olodaterol is a long-acting β2-adrenergic receptor agonist that is used as a component of an inhalation (Tiotropium/this compound) for treating patients with chronic obstructive pulmonary disease (COPD).
|
|
|
| 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.
|
|
|
| S5669 |
Isoxsuprine hydrochloride
|
Isoxsuprine hydrochloride is a beta-adrenergic agonist with vasodilator activity.
|
|
|
| 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.
|
|
|
| E0949 |
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.
|
|
|
| E1049 |
CL316243
|
CL316243 is a highly potent and selective agonist of β3-adrenoceptor with an EC50 value of 3 nM, respectively but is an extremely poor to β1/2- receptors.It effectively stimulates adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate.
|
|
|
| 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.
|
|
|
| E6494New |
ATR-258
|
ATR‑258 (Compound 15) is a specific agonist of GRK‑biased β2‑adrenergic receptor (β2AR) with a pEC50 of 6.87 that increases glucose uptake with low cAMP generation.
|
|
|
| S5496 |
Guanethidine Monosulfate
|
Guanethidine monosulfate is an antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves.
|
|
|
| E6068New |
levosalbutamol hydrochloride
|
levosalbutamol hydrochloride ((R)-Salbutamol hydrochloride, (R)-Salbutamol hydrochloride) is a short-acting agonist of the β2 adrenergic receptor used to treat asthma and chronic obstructive pulmonary disease (COPD). It is the active (R)-enantiomer of salbutamol.
|
|
|
| S5782 |
Doxazosin
|
Doxazosin(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
|
|
|
| E4892 |
Formoterol
|
Formoterol is a highly selective and potent long-acting beta2-adrenergic agonist that functions by binding to and activating beta2-adrenergic receptors on the smooth muscle cells of the airways. It is used in the treatment of patients with chronic obstructive pulmonary disease (COPD).
|
|
|
| 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.
|
|
|
| E6056 |
(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.
|
|
|
| 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
|
|
|
| S5432 |
Dibenamine Hydrochloride
|
Dibenamine (N-(2-Chloroethyl)dibenzylamine, Sympatholytin, Dibenzylchlorethamine) is an irreversible blocker of α1 adrenoceptors.
|
|
|
| E7406 |
Tulobuterol
|
Tulobuterol (C-78 free base) is a long-acting and selective agonist of β2-adrenoceptor . It can be used as a transdermal patch, increases normal diaphragm muscle strength and aids in bronchial asthma treatment, and may protect against endotoxins in inhaled house dust.
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|
|
| E2964 |
Norepinephrine tartrate
|
Norepinephrine tartrate is a potent agonist of adrenergic receptor (AR). Norepinephrine activates α1, α2, β1 receptors.
|
|
|
| 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.
|
|
|
| S4277 |
Bambuterol HCl
|
Bambuterol HCl(Bambuterol hydrochloride,KWD-2183 hydrochloride) is a potent β-adrenoceptor agonist, used in the treatment of asthma.
|
|
|
| E1746 |
Protokylol hydrochloride
|
Protokylol hydrochloride(Caytine hydrochloride, JB-251 hydrochloride) is a salt form of protokylol and is an agonist of β-adrenergic receptor. This compound is also used as a bronchodilator.
|
|
|
| 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.
|
|
|
| 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.
|
|
|
| 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).
|
|
|
| S5723 |
Carvedilol EP IMpurity E
|
Carvedilol is a nonselective beta blocker/alpha-1 blocker and used in management of congestive heart failure (CHF).
|
|
|
| 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.
|
-
Anticancer Research, February 2021, 687-697
-
Anticancer Research, February 15, 2021, 687-697
-
bioRxiv, February 07, 2026, nan
|
|
| 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.
|
-
Anticancer Research, October 15, 2018, 5685-5692
-
Acta Haematologica, January 6, 2025, 729-733
-
Mol Metab, 2025, 91:102069
|
|
| S1642 |
Methyldopa
|
Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
mBio, 2022, e02177-21
-
Scientific Reports, 2017, 8491
|
|
| 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.
|
-
Am J Cancer Res, 2024, 14(3):1087-1100
-
American Journal of Cancer Research, 2024, 1087-1100
-
Drug Metab Dispos, 2020, 48(10):1044-1052
|
|
| E0785 |
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.
|
-
Cell Signal, 2025, 131:111752
-
Signal Transduct Target Ther, 2024, 9(1):243
|
|
| 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.
|
-
Anticancer Research, December 15, 2021, 6179-6190
|
|
| 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. This compound is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist.
|
-
Journal of Cellular and Molecular Medicine, 2021 Jul 19, 7980-7992
-
Journal of Cellular and Molecular Medicine, 2021, 7980-7992
|
|
| 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.
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Cell Rep Methods, 2023, 3(1):100381
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| S4112 |
Desvenlafaxine Succinate hydrate
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Desvenlafaxine Succinate hydrate (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.
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Drug Metab Dispos, 2020, 48(10):1044-1052
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| S2691 |
BMY 7378 Dihydrochloride
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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.
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| S0032 |
Batefenterol
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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.
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| S7538 |
RS-102895 Hydrochloride
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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.
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| S3913 |
Pimethixene maleate
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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.
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| S9560 |
Anisodamine Hydrobromide
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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).
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