Bopindolol Malonate

Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a prodrug of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research[1][2][3][4].

Research Areas >> Cardiovascular Disease

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

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> Metabolic Enzyme/Protease >> Renin

Adrenergic receptor, Renin, 5-HT receptors[1][4]

Bopindolol (intravenous injection; 8, 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 (0.3, 1 and 3 mg/kg; IP; single dosage) produces dose dependent decreases in diastolic blood pressure and in heart rate[2]. Animal Model: Male Wistar rats (260-300 g)[2] Dosage: 0.3, 1 and 3 mg/kg Administration: IP; single dosage Result: Produced dose dependent decreases in diastolic blood pressure, and the decrease of about 8 mmHg at 3 mg/kg. Decreased the heart rate in a dose-dependent manner.

[1]. Harron DW, et al. Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs. 1991 Jan;41(1):130-49.

[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.

[4]. Nagatomo T, et al. Bopindolol: pharmacological basis and clinical implications. Cardiovasc Drug Rev. 2001 Spring;19(1):9-24.

MOLECULAR WEIGHT :

484.60

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

824 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Gastrointestinal - ulceration or bleeding from stomach

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: 23,4369,1989

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

481 mg/kg

TOXIC EFFECTS :

Behavioral - ataxia Lungs, Thorax, or Respiration - cyanosis Skin and Appendages - hair

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: 23,4369,1989

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

9200 ug/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

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: 23,4369,1989