（±）-1-[[2-（3,4-二甲氧基苯基）乙基]氨基]-3-（3-甲基苯氧基）-2-丙醇盐酸盐（贝凡洛尔，NC-1400）是一种具有α1肾上腺素能受体阻断活性的β1选择性肾上腺素能受体阻滞剂。

(+/-)-1-[[2-(3,4-Dimethoxphenyl)ethyl]amino]-3-(3-methylphenoxy)-2- propanol hydrochloride (bevantolol, NC-1400) as a beta 1-selective adrenoceptor blocker with alpha 1-adrenoceptor blocking activity.

作者信息

Takayanagi I, Kizawa Y, Iwasaki S, Nakagoshi A

出版信息

Gen Pharmacol. 1987;18(1):87-9. doi: 10.1016/0306-3623(87)90175-3.

Abstract

Blocking activities of alpha- and beta-adrenoceptors by (+/-)-1-[[2-(3,4-dimethoxyphenyl)-ethyl]amino]-3-(3-methylphenoxy)-2 -propanol hydrochloride (NC-1400) were tested on the isolated muscles, comparing with those of labetalol and atenolol. In blocking the beta 1-adrenoceptor, NC-1400 was slightly more potent than labetalol and atenolol. NC-1400 was about 1/10th as potent as labetalol and about ten times as potent as atenolol in blocking the beta 2-receptor. NC-1400 was beta 1-adrenoceptor selective. NC-1400 was about 1/30th as potent as labetalol in blocking the alpha 1-receptor. NC-1400 did not interact with the alpha 2-adrenoceptor in concentrations up to 10(-5) M. The present results indicate that NC-1400 is the selective beta 1-adrenoceptor blocker with some blocking activity of alpha 1-adrenoceptors.

摘要

通过在离体肌肉上测试盐酸（±）-1-[[2-（3,4-二甲氧基苯基）-乙基]氨基]-3-（3-甲基苯氧基）-2-丙醇（NC-1400）对α和β肾上腺素能受体的阻断活性，并与拉贝洛尔和阿替洛尔进行比较。在阻断β1肾上腺素能受体方面，NC-1400的效力略高于拉贝洛尔和阿替洛尔。在阻断β2受体方面，NC-1400的效力约为拉贝洛尔的1/10，约为阿替洛尔的10倍。NC-1400具有β1肾上腺素能受体选择性。在阻断α1受体方面，NC-1400的效力约为拉贝洛尔的1/30。在浓度高达10^(-5) M时，NC-1400不与α2肾上腺素能受体相互作用。目前的结果表明，NC-1400是一种具有一定α1肾上腺素能受体阻断活性的选择性β1肾上腺素能受体阻滞剂。