Bopindolol fumarate

Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate is a prodrug of pindolol and can be used for essential and renovascular hypertension research[1][2].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

β1 adrenoceptor

β2 adrenoceptor

β3 adrenoceptor

Bopindolol (intravenous injection; l8, 16 and 32 μg/kg) fumarate causes a dose-dependent inhibition of isoprenaline-induced tachycardia, and this agent is 4 times more potent than propranolol in anaesthetised dogs[1]. Bopindolol (intraperitoneal injection; 3.0 mg/kg) fumarate reduces the diastolic blood pressure (DBP) in pithed rats. And pindolol (1.0 mg/kg) produces similar decreases in DBP of about 8 mmHg. it also produces a dose-dependent decrease in heart rate[2].

[1]. D W Harron, et al. Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs

[2]. H Tanaka, et al. Hypotensive effect of bopindolol in pithed rats. Gen Pharmacol. 1993 Mar;24(2):373-5.

[3]. Y Hosohata, et al. Bopindolol is a slowly dissociating beta 1-adrenoceptor antagonist when compared to other beta-blockers. Biol Pharm Bull. 1995 Aug;18(8):1066-71.