Colella D F, Chakrin L W, Shetzline A, Wardell J R
Eur J Pharmacol. 1977 Dec 1;46(3):229-41. doi: 10.1016/0014-2999(77)90338-7.
Carbuterol is a beta-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 beta-adrenergic agonist, not dependent on endogenous catecholamine release, and was devoid of alpha-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 on beta1 receptors 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 fusion of incomplete tetanic contraction of the soleus muscle.
卡布特罗是一种β-肾上腺素能支气管扩张剂，相对于包括人类在内的几种物种的心脏和血管组织，它对支气管平滑肌具有选择性。目前的研究旨在进一步描述其肾上腺素能特征。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，不依赖内源性儿茶酚胺释放，且无α-肾上腺素能激动剂活性。消旋体的活性主要存在于左旋对映体中。卡布特罗抑制免疫诱导的组胺释放以及被动致敏的恒河猴肺碎片中过敏反应迟缓反应物质的释放，并且还抑制大鼠的被动皮肤过敏反应。在麻醉的开胸犬中证实了卡布特罗对介导心率和收缩力的β1受体的刺激活性相对较弱。在麻醉的猫中，卡布特罗在降低舒张压、增加心率以及降低比目鱼肌不完全强直收缩的张力和融合程度方面的效力明显低于异丙肾上腺素。
