Bopindolol

Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol 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

β2 adrenoceptor

Beta-1 adrenergic receptor

Beta-3 adrenergic receptor

Bopindolol (intravenous injection; l8, 16 and 32 μg/kg) 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) reduced the diastolic blood pressure (DBP) in pithed rats. And pindolol (1.0 mg/kg) produced 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.

MOLECULAR FORMULA :

C23-H28-N2-O3

MOLECULAR WEIGHT :

380.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

17 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2635209 ** REPRODUCTIVE DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

3 gm/kg

SEX/DURATION :

female 6-15 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 26,115,1992

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

1188 mg/kg

SEX/DURATION :

female 7-17 day(s) after conception

TOXIC EFFECTS :

Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,4373,1989