拉贝洛尔的α和β肾上腺素能受体阻断作用评估。
Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol.
作者信息
Richards D A, Tuckman J, Prichard B N
出版信息
Br J Clin Pharmacol. 1976 Oct;3(5):849-55. doi: 10.1111/j.1365-2125.1976.tb00637.x.
Abstract
Isoprenaline dose-response curves plotting increases in heart rate before and after labetalol are suggestive of competitive antagonism at beta-adrenoceptor sites. Phenylephrine dose-response curves using increases in systolic pressure before and after labetalol are suggestive of competitive antagonism at alpha-adrenoceptor sites. The ratio of alpha:beta-adrenoceptor antagonism induced by labetalol is approximately 1:3. Peak pharmacological responses after a single oral dose of labetalol (400 mg) occurred between 90-120 min after administration.
摘要
绘制拉贝洛尔用药前后心率增加情况的异丙肾上腺素剂量-反应曲线表明在β-肾上腺素受体部位存在竞争性拮抗作用。利用拉贝洛尔用药前后收缩压升高情况绘制的去氧肾上腺素剂量-反应曲线表明在α-肾上腺素受体部位存在竞争性拮抗作用。拉贝洛尔诱导的α:β-肾上腺素受体拮抗作用比例约为1:3。单次口服拉贝洛尔（400毫克）后的最大药理反应出现在给药后90 - 120分钟之间。
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