4-（2-羟基-3-[(1-甲基-3-苯基丙基)氨基]丙氧基）苯乙酰胺（KF4317）和拉贝洛尔对α和β肾上腺素能受体的作用

Actions of 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy) benzeneacetamide (KF4317) and labetalol on alpha- and beta-adrenoceptors.

作者信息

Takayanagi I, Koike K, Konno F, Hiruta T, Kusunoki M, Sato T, Toyoda J, Kizawa Y

出版信息

Gen Pharmacol. 1986;17(6):651-3. doi: 10.1016/0306-3623(86)90295-8.

Abstract

Blocking activities of alpha- and beta-adrenoceptors by 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy)benzeneacetamide (KF4317) were tested on the isolated muscles, compared with the action of labetalol. In blocking the beta 1-adrenoceptor, KF4317 was almost as active as labetalol. KF4317 was about 1/10th as potent as labetalol in blocking the beta 2-receptor. KF4317 was beta 1-adrenoceptor selective. KF4317 was about 1/50th as potent as labetalol in blocking the alpha 1-receptor. KF4317 did not interact with the alpha 2-adrenoceptor in concentrations up to 10(-5) M. The present results indicate that KF4317 is a selective beta 1- and alpha 1-adrenoceptor blocker, though the alpha 1-adrenoceptor blocking action is weak.

摘要

与拉贝洛尔的作用相比，在离体肌肉上测试了4-(2-羟基-3-[(1-甲基-3-苯基丙基)氨基]丙氧基)苯乙酰胺（KF4317）对α和β肾上腺素能受体的阻断活性。在阻断β1肾上腺素能受体方面，KF4317的活性几乎与拉贝洛尔相同。在阻断β2受体方面，KF4317的效力约为拉贝洛尔的1/10。KF4317具有β1肾上腺素能受体选择性。在阻断α1受体方面，KF4317的效力约为拉贝洛尔的1/50。在浓度高达10(-5) M时，KF4317不与α2肾上腺素能受体相互作用。目前的结果表明，KF4317是一种选择性β1和α1肾上腺素能受体阻滞剂，尽管其α1肾上腺素能受体阻断作用较弱。