纳摩尔浓度的普萘洛尔会抑制γ-氨基丁酸（GABA）刺激的苯二氮䓬与大鼠大脑皮层的结合。

Nanomolar concentrations of propranolol inhibit GABA-stimulated benzodiazepine binding to rat cerebral cortex.

作者信息

Morgan P F, Stone T W

出版信息

Neurosci Lett. 1982 Apr 16;29(2):159-62. doi: 10.1016/0304-3940(82)90346-9.

Abstract

The influence of propranolol on GABA-stimulated [3H]diazepam binding in the rat cerebral cortex was investigated. Maximum potentiation of GABA-stimulated binding (20.6 +/- 4.5%, P less than 0.05) was observed at 100 microM propranolol, whilst maximum inhibition (32.5 +/- 2.5%, P less than 0.01) was observed at 1 nM propranolol. Low concentrations (1 nM) of (+)-propranolol were observed to be equipotent with (+/-)-propranolol in shifting the dose-response curve of GABA-stimulated [3H]diazepam binding by approximately 1/2 log unit. The phenomenon does not therefore show the stereospecificity observed towards either beta-adrenergic receptors or 5-hydroxytryptamine receptors.

摘要

研究了普萘洛尔对大鼠大脑皮层中γ-氨基丁酸（GABA）刺激的[3H]地西泮结合的影响。在100微摩尔普萘洛尔时观察到GABA刺激结合的最大增强（20.6±4.5%，P<0.05），而在1纳摩尔普萘洛尔时观察到最大抑制（32.5±2.5%，P<0.01）。观察到低浓度（1纳摩尔）的（+）-普萘洛尔在将GABA刺激的[3H]地西泮结合的剂量反应曲线移动约1/2对数单位方面与（±）-普萘洛尔等效。因此，该现象未表现出对β-肾上腺素能受体或5-羟色胺受体所观察到的立体特异性。