Characterization of the adrenergic activity of carbuterol (SK&F 40383-A).
Characterization of the adrenergic activity of carbuterol (SK&F 40383-A).
复制标题
卡布特罗 (SK
DOI：
10.1016/0014-2999(77)90338-7
复制
发表时间：
1977
影响因子：
5
通讯作者：
J. R. Wardell
中科院分区：
文献类型：
--
作者：
D. F. Colella;L. W. Chakrin;A. Shetzline;J. R. Wardell
Carbuterol是一种β-肾上腺素能支气管扩张剂，对包括人在内的几种动物的支气管平滑肌具有选择性，而对心脏和血管组织具有选择性。体外研究表明，卡布特罗是一种直接作用的β-肾上腺素能激动剂，不依赖于内源性儿茶酚胺释放，并且没有α-肾上腺素能激动剂活性。外消旋体的活性主要存在于L-对映体中。Carbuterol可抑制免疫诱导的被动致敏恒河猴肺组织组胺和过敏反应慢反应物质的释放，也可抑制大鼠被动皮肤过敏反应。在麻醉开胸犬中证实了卡布特罗对介导收缩速率和收缩力的β 1受体的相对较弱的兴奋活性。在麻醉猫中，卡布特罗在降低舒张压、增加心率、降低比目鱼肌不完全强直收缩的张力和融合度方面的效力明显低于异丙肾上腺素。
Carbuterol is a β-adrenergic bronchodilator with selectivity for bronchial smooth muscle relative to cardiac and vascular tissues of several species including man. The present studies were undertaken to further characterize its adrenergic profile. In vitro studies demonstrated that carbuterol was a direct acting β-adrenergic agonist, not dependent on endogenous catecholamine release, and was devoid of α-adrenergic agonist activity. The activity of the racemate was shown to reside primarily in the l-enantiomer. Carbuterol inhibited immunologically induced release of histamine and slow reacting substance of anaphylaxis from passively sensitized fragmented Rhesus monkey lung and also inhibited passive cutaneous anaphylaxis in rats. The relatively weak stimulant activity of carbuterol onβ1receptors mediating both rate and force of contraction was confirmed in anesthetized open-chest dogs. In the anesthetized cat, carbuterol was significantly less potent than isoproterenol in decreasing diastolic blood pressure, increasing heart rate, and decreasing the tension and degree of fusionof incomplete tetanic contraction of the soleus muscle.