adrenoceptor

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.

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].

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

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.

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator that inhibits α1-adrenoceptor-mediated positive inotropic effects in a concentration-dependent manner, induced by contraction of isolated rabbit vascular smooth muscle.

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

Clopimozide (R-29764) acts as a calcium channel antagonist and inhibits [3H] nilandipine binding.Clopimozide is a novel and orally available long-acting antischizophrenic psychostatic compound.

Taprizosin(UK-338003) is a selective and orally active α1-adrenoceptor antagonist for vasodilatation in the treatment of benign prostatic hyperplasia.

LY377604 is a human β3-adrenergic receptor agonist (EC50: 2.4 nM) and β1 2-adrenergic receptor antagonist for the study of obesity.

T-0509 is a selective beta 1 receptor agonist that increases inotropy in canine ventricular muscle and selectively down-regulates rat cardiac beta 1-adrenoceptors.

β2AR M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

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.

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

Neldazosin is used as a potent α1-adrenoceptor antagonist.

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

Delequamine (RS 15385-197) is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.

Fipamezole is a potent alpha2 adrenergic receptor antagonist that may be useful for studying autonomic dysfunction in Parkinson's disease.

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.

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

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.

Saterinone is a potent and selective phosphodiesterase III inhibitor and a potent antagonist of the vascular α-1-adrenoceptor. Saterinone has vasodilatory properties and can be used in the acute treatment of chronic heart failure. Saterinone inhibited crude cAMP phosphodiesterase (PDE) activity in guinea pig right ventricular homogenates The ic50 value is 2.3 × 10(-5) mol l.

Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist that acts as a hypoglycemic agent by lowering blood glucose levels and increasing blood pressure in vivo.

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