拉贝洛尔和YM-09538对大鼠输精管中（3H）去甲肾上腺素神经元摄取的影响。

Effect of labetalol and YM-09538 on neuronal uptake of (3H)norepinephrine in the rat vas deferens.

作者信息

Cohen M L, Hynes L M

出版信息

Clin Exp Hypertens A. 1983;5(4):563-75. doi: 10.3109/10641968309081793.

DOI:10.3109/10641968309081793

Abstract

Labetalol and YM-09538 are combined alpha and beta receptor antagonists with demonstrated antihypertensive activity. Both compounds inhibited the uptake of (3H)norepinephrine into nerves in the rat vas deferens. However, labetalol was approximately 5 fold more potent than YM-09538 as an inhibitor of neuronal uptake. Inhibition of neuronal uptake occurred at concentrations 43 and 3800 times higher than necessary for inhibition of alpha receptors by labetalol and YM-09538, respectively. Thus YM-09538 shows a greater separation between neuronal uptake blocking properties and alpha receptor blocking properties than labetalol. This separation of activities may contribute to greater antihypertensive efficacy of YM-09538 relative to labetalol.

摘要

拉贝洛尔和YM-09538是兼具α和β受体拮抗作用的化合物，已证实具有抗高血压活性。两种化合物均抑制大鼠输精管神经对（3H）去甲肾上腺素的摄取。然而，作为神经元摄取抑制剂，拉贝洛尔的效力约为YM-09538的5倍。拉贝洛尔和YM-09538分别在高于抑制α受体所需浓度43倍和3800倍时出现神经元摄取抑制。因此，与拉贝洛尔相比，YM-09538在神经元摄取阻断特性和α受体阻断特性之间表现出更大的差异。这种活性差异可能导致YM-09538相对于拉贝洛尔具有更高的抗高血压疗效。