拉贝洛尔对α和β肾上腺素能受体双重作用的生化证据。
Biochemical evidence for the dual action of labetalol on alpha- and beta-adrenoceptors.
作者信息
Aggerbeck M, Guellaen G, Hanoune J
出版信息
Br J Pharmacol. 1978 Apr;62(4):543-8. doi: 10.1111/j.1476-5381.1978.tb07759.x.
Abstract
1 Labetalol (AH 5158A) inhibited the adrenaline-stimulated adenylate cyclase activity of rat liver and heart. This drug had no effect on basal or guanosine triphosphate (GTP)-activated adenylate cyclase activities. 2 Labetalol displaced the binding of the specific ligands [3H]-dihydroergocryptine and (-)-[3H]-dihydroalprenolol from their respective alpha and beta-adrenoceptors in rat heart and liver. The affinity of labetalol was 10 fold higher for the beta- than for the alpha-adrenoceptor. It appeared to be 10 to 100 times less potent than phentolamine in blocking alpha-adrenoceptors and 5 to 10 times less potent than propranolol in blocking beta-receptors. 3 It is concluded that labetalol exerts its dual alpha- and beta-antagonism by acting directly on the plasma membranes, where it binds competitively to alpha- and beta-adrenoceptors.
摘要
- 拉贝洛尔（AH 5158A）抑制了肾上腺素刺激的大鼠肝脏和心脏的腺苷酸环化酶活性。该药物对基础或鸟苷三磷酸（GTP）激活的腺苷酸环化酶活性无影响。2. 拉贝洛尔使大鼠心脏和肝脏中特异性配体[3H] - 二氢麦角隐亭和（ - ） - [3H] - 二氢阿普洛尔与其各自的α和β肾上腺素受体的结合发生位移。拉贝洛尔对β肾上腺素受体的亲和力比对α肾上腺素受体高10倍。在阻断α肾上腺素受体方面，它的效力似乎比酚妥拉明低10至100倍，在阻断β受体方面，比普萘洛尔低5至10倍。3. 得出的结论是，拉贝洛尔通过直接作用于质膜发挥其双重α和β拮抗作用，在质膜上它与α和β肾上腺素受体竞争性结合。
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