Bopindolol(malonate)

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CAS NO:

82857-38-3

(±)-Bopindolol (malonate)

Bopindolol ((±)-Bopindolol) malonate 是一种口服活性的 β-肾上腺素受体 (ARs) 拮抗剂，具有部分激动剂活性。Bopindolol malonate 对 β1-和 β2-ARs 无选择性，对 β3-AR 亚型亲和力低。Bopindolol malonate 具有内在拟交感神经和膜稳定作用，抑制肾素 (renin) 分泌，并与5-HT 受体相互作用。Bopindolol malonate 是 Pindolol (HY-B0982) 的前体药物，可用于原发性和肾血管性高血压的研究。

生物活性

Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist ofβ-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, inhibitsreninsecretion, and interacts with5-HT receptors. Bopindolol malonate is a prodrug ofPindolol(HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research^[1]^[2]^[3]^[4].

IC₅₀& Target

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

体内研究
(In Vivo)

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.

分子量

484.54

Formula

C₂₆H₃₂N₂O₇

CAS 号

82857-38-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.