-
β2-AR agonist
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries.- Ana Rubio, .et al. , Drug Test Anal, 2023, Jul 31 PMID: 37525530
- Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
- Antonia Donat, .et al. , iScience, 2023, Aug 29;26(10):107761 PMID: 37720081
-
Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
- Nebivolol hydrochloride is t a highly selective antagonist of the β1-adrenoceptor (Ki = 0.88 nM, β2-adrenoceptor Ki = 48 nM).
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14 PMID: 33330842
-
β3 adrenergic receptor activator
Mirabegron is a potent bladder relaxant and reagent for diabetes remedy.- Havard Fjelltveit, .et al. , Auton Neurosci, 2025, Apr:258:103253 PMID: 39977963
- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
- Bhavik Patel, .et al. , Pharmacol Res Perspect, 2020, 8 (1), e00564 PMID: 32030913
-
β-adrenergic blocker
S(-)-Propranolol Hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
-
β1-selective adrenergic receptor agonist
Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
-
α1-adrenergic receptor agonist
Phenylephrine is a selective α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
-
β adrenoceptor agonist
Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
-
α2C antagonist
JP 1302 2HCl is a potent and selective α2C antagonist.- Junya Maruoka, .et al. , Int J Neuropsychopharmacol, 2026, Apr 6;29(4):pyag007 PMID: 41717785
-
H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150 PMID: 34334499
- Doxazosin mesylate, a quinazoline compound, is an α1-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
- L Klem, .et al. , Psychopharmacology (Berl), 2023, Aug;240(8):1629-1650 PMID: 37329343
-
β2 adrenergic receptor antagonist
ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.- Moon Jain, .et al. , Tropical Journal of Pharmaceutical Research, 2020, Vol. 19 No. 4
- Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
-
alpha1/beta adrenergic receptors antagonist
Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Clenbuterol Hydrochloride is a sympathomimetic β2-adrenoceptor agonist that has been used as a bronchodilator in the treatment of pulmonary diseases such as asthma. At higher doses, clenbuterol acts as an anabolic steroid, favoring skeletal muscle protein synthesis at the expense of fat deposition.
- Younian Xu, .et al. , J Inflamm Res, 2022, Jan 14;15:295-309 PMID: 35058704
-
alpha-1A/alpha-1B-adrenoceptor antagonist
Tamsulosin is an alpha1a-selective alpha blocker used in the symptomatic treatment of benign prostatic hyperplasia (BPH). -
β3-adrenergic receptor agonist
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold). -
beta2-adrenergic agonist
Arformoterol tartrate is a beta2-adrenergic agonist -
α2 adrenergic agonist
AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively. -
Adrenergic Receptor agonist
Tetrahydrozoline Hydrochloride is an alpha agonist which causes constriction of conjunctival blood vessels. -
ultra-long-acting β??? adrenoreceptor agonist
Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05. -
β2 adrenergic antagonist
ICI 118551 hydrochloride is a selective β2 adrenergic antagonist. - Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
-
α2-adrenoceptor agonist
Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). - Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
- DL-Adrenaline is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands. DL-Adrenaline is found in small amounts in the body and is essential for maintaining cardiovascular homeostasis because of its ability to divert blood to tissues under stress.
- Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
-
Beta1 receptor blocker
Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. - Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and glaucoma. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may. Betaxolol also shows greater affininty for beta1 receptors than metoprolol.
- Formoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD).
- Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
- Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).
-
beta2-adrenergic receptor agonist
Salmeterol is a long-acting beta2-adrenergic receptor agonist -
adrenergic agonist
Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors. -
β2-adrenergic receptor
Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties. -
alpha2-adrenoceptor agonist
Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist. - Procaterol is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
-
AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. -
Adrenoceptors antagonist
BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration. - 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.
-
Adrenergic α1 Receptor Antagonist
HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes. -
α2- adrenoceptor antagonist / I2 imidazoline receptor agonist
Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively). -
5-HT1A receptor antagonist
NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. - Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
-
α-Adrenergic blocker
Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker.

