Bevantolol (hydrochloride)

Bevantolol is an antagonist of the beta1-adrenergic receptor (beta1-AR, Ki = 14.79 nM in rat cortical membranes). It is selective for beta1- over beta2-ARs (Ki = 588.84 nM), as well as alpha2-ARs up to 100 µM, but is an antagonist of alpha1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 µM). 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). Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.Formal Name: 1-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-3-(3-methylphenoxy)-2-propanol, monohydrochloride. CAS Number: 42864-78-8. Synonyms: CI-755, DL-Bevantolol, NC-1400. Molecular Formula: C20H27NO4 . HCl. Formula Weight: 381.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml. SMILES: CC1=CC=CC(OCC(O)CNCCC2=CC(OC)=C(OC)C=C2)=C1.Cl. InChi Code: InChI=1S/C20H27NO4.ClH/c1-15-5-4-6-18(11-15)25-14-17(22)13-21-10-9-16-7-8-19(23-2)20(12-16)24-3,/h4-8,11-12,17,21-22H,9-10,13-14H2,1-3H3,1H. InChi Key: FJTKCFSPYUMXJB-UHFFFAOYSA-N.