A β1-AR antagonist (Ki = 14.79 nM in rat cortical membranes); selective for β1- over β2-ARs (Ki = 588.84 nM)

Bevantolol (hydrochloride) – 500 mg

Brand:
Cayman
CAS:
42864-78-8
Storage:
-20
UN-No:
Non-Hazardous - /

Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}  

 

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Description

A β1-AR antagonist (Ki = 14.79 nM in rat cortical membranes); selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM); inhibits LVA-ICa in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM); inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induce relaxation of isolated guinea pig trachea (pA2 = 6.69); prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension at 250 mg/kg per day

Formal name: 1-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-3-(3-methylphenoxy)-2-propanol, monohydrochloride

Synonyms:  CI-755|DL-Bevantolol|NC-1400

Molecular weight: 381.9

CAS: 42864-78-8

Purity: ≥98%

Formulation: A crystalline solid

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