α-adrenoceptor

Compound A (α2C adrenoceptor agonist 1) is an orally active, highly selective α2C-adrenoceptor agonist that does not penetrate the central nervous system. It exhibits EC50 and Ki values of 108 nM and 12 nM, respectively. This compound is utilized in research on nasal congestion [1].

Cicloprolol hydrochloride is a new potent and selective beta 1-adrenoceptor antagonist with partial agonist activity for the study of coronary heart disease.

Nicergoline (Nicergolinum) is an ergot derivative used to treat senile dementia and other disorders with vascular origins.

Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.

Dexmedetomidine hydrochloride (Precedex) is a potent, selective, orally active α2-adrenoceptor agonist with a Ki value of 1.08 nM. It shows 1620-fold selectivity over α1-adrenoceptors. Dexmedetomidine hydrochloride (Precedex) can protect against sepsis-induced acute lung injury through anti-inflammatory, anti-oxidative, and anti-apoptotic effects.

SR59230A is a potent, selective antagonist of β3-adrenergic receptor(β3, β1, and β2 receptors with IC50s of 40, 408, and 648 nM , respectively).

CL316243 is a highly potent selective agonist of β3-adrenoceptor, with a EC50 of 3 nM. CL316243 is an effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.

α1 adrenoceptor-MO-1 (S enantiomer) has affinity at alpha 1 adrenergic receptor with alphalytic activity and analgesic action. It has more active than R enantiomer.

Arbutamine (GP 21213) is a novel potent non-selective beta-adrenoceptor agonist with alpha-1-sympathomimetic activity.Arbutamine promotes cardiac stress and increases heart rate, cardiac contractility.Arbutamine can be used to study cardiac stress and coronary artery disease

Bunazosin Hydrochloride (E 1015) is an alpha(1)-adrenoceptor antagonist used as a systemic antihypertensive and an ocular hypotensive drug.

Tolnapersine is a mixed dopamine agonist and alpha-adrenoceptor antagonist.

Amibegron hydrochloride, a selective β3-adrenoceptor agonist (EC50: 3.5 nM for β-adrenoceptor in rat colon), exhibits anxiolytic and antidepressant activity.

CGP 20712 A (CGP 20712 mesylate) is a selective and potent β1-adrenergic receptor antagonist (IC50: 0.7 nM) with antihypertensive activity, capable of reversing RKT-induced gastric relaxation.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).

OPC-28326 is a specific an α2-adrenergic receptor antagonist and acts as a peripheral vasodilator. OPC-28326 inhibits α2A-, α2B- and α2C-adrenoceptors with Ki of 2040, 285, and 55 nM, respectively.

L-771688 (SNAP 6383) is a novel potent and selective α1A-adrenoceptor antagonist with a Ki value of 0.43±0.02 nM.L-771688 KE is used for the treatment of benign prostatic hyperplasia.

Azepexole hydrochloride (4H-Oxazolo[4,5-d]azepin-2-amine, 6-ethyl-5,6,7,8-tetrahydro-, hydrochloride (1:1)) is a potent α2-Adrenoceptor agonist with anaesthetic effects.

Talibegron hydrochloride (ZD2079 hydrochloride) is a β3 adrenergic receptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. It relaxes rat mesenteric artery and isolated aorta in vitro, and inhibits ob gene expression and circulating leptin levels in lean mice in vivo.

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

(±)-Prenalterol (H 80/62) is a new cardioselective positive inotropic compound that is an agonist of beta-2- and beta-1-adrenergic receptors and can be used to study chronic congestive heart failure.

ORM-10921 is an α2C-adrenoceptor antagonist that has shown antipsychotic and antidepressant activity in animal studies.

Bedoradrine (MN-221) free base is a novel, highly selective β2-adrenoceptor agonist for the treatment of asthma and chronic obstructive pulmonary disease.