adrenoceptor antagonist

ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist with pKD values of 8.8, 6.7, and 6.4 at α2B, α2A, and α2D receptors respectively (pKD values are 8.8, 6.7, and 6.4 at α2B, α2A, and α2D receptors respectively).

α1A/1D-Adrenoceptor antagonist-1 is a dual-targeting adrenoceptor antagonist exhibiting exceedingly high binding affinity for both alpha 1A and alpha 1D subtypes. It significantly reduces urethral resistance by specifically blocking smooth muscle contraction in the lower urinary tract and prostate, serving as an important tool for investigating benign prostatic hyperplasia (BPH) and hypertension mechanisms.

Atipamezole is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride (MPV-1248 hydrochloride) is hydrochloride form of atipamezole.

Atipamezole (Antisedan) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug.

5-HT2 antagonist 1 is a small molecule antagonist functioning as a 5-HT2B receptor antagonist (IC50 = 33.4 nM), with oral bioactivity and weak inhibition of α1 receptors, employed in research on hepatocellular carcinoma and related diseases.

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

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.

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.

Pamatolol is a selective and potent beta-adrenoceptor antagonist that has not shown sympathomimetic activity in ex vivo experiments.

RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays.

JP1302 is a selective α2C adrenoceptor antagonist with a Kb value of 16 nM and a Ki of 28 nM for human α2C receptors.JP1302 has antidepressant activity, disrupts the FACT complex and degrades histone H1.JP1302 has been used in the study of neuropsychiatric disorders, acute renal failure, and renal injury.

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.

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

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

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

CGP-20712 is a selective β 1-adrenoceptor antagonist with an IC50 of 0.7 nM.

Neldazosin is used as a potent α1-adrenoceptor antagonist.

SM-2470 is an α1-adrenoceptor antagonist with antihypertensive activity that decreases anterior ganglionic adrenal nerve activity and aortic descending nerve activity.SM-2470 has hypocholesterolemic activity and inhibits cholesterol absorption.

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

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.

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.

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.

Fluparoxan hydrochloride is a highly selective and potent α2-adrenoceptor antagonist for the prevention, amelioration or treatment of neurodevelopmental disorders and neurodegenerative diseases.