A β1-AR antagonist
Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).1 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).2 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).3 Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.4
1.Takita, M., Kigoshi, S., and Muramatsu, I.Selectivity of bevantolol hydrochloride towards ɑ and β-adrenoceptor subtypes in rat cerebral cortexJpn. J. Pharmacol.58(2)193-196(1992) 2.T., O., Kobayashi, T., Nishioka, K., et al.Ca2+-antagonistic action of bevantolol on hypothalamic neurons in vitro: Its comparison with those of other β-adrenoceptor antagonists, a local anesthetic and a Ca2+-antagonistBrain Res.706(2)289-292(1996) 3.Takayanagi, I., Kizawa, Y., Iwasaki, S., et al.(+/-)-1-[[2-(3,4-dimethoxphenyl)ethyl]amino]-3-(3-methylphenoxy)-2-propanol hydrochloride (bevantolol, NC-1400) as a β1-selective adrenoceptor blocker With ɑ1-adrenoceptor Blocking ActivityGen. Pharmacol.18(1)87-90(1987) 4.Takita, M., Kigoshi, S., and Muramatsu, I.Effects of bevantolol HCl on immobilization stress-induced hypertension and central β-adrenoceptors in ratsPharmacol. Biochem. Behav.45623-627(1993)
动态评分
0.0