依托咪酯（+）和戊巴比妥增强地西泮和γ-氨基丁酸的结合。

Enhancement of diazepam and gamma-aminobutyric acid binding by (+)etomidate and pentobarbital.

作者信息

Thyagarajan R, Ramanjaneyulu R, Ticku M K

出版信息

J Neurochem. 1983 Aug;41(2):578-85. doi: 10.1111/j.1471-4159.1983.tb04778.x.

DOI:10.1111/j.1471-4159.1983.tb04778.x

Abstract

(+)Etomidate and pentobarbital enhance [3H]diazepam and [3H]gamma-aminobutyric acid [( 3H]GABA) binding to cerebral cortex membranes. Both (+)etomidate and pentobarbital increase the affinity of [3H]diazepam for its binding sites. In contrast, they increase the Bmax of both the high- and low-affinity GABA receptor sites. The enhancement of [3H]diazepam and [3H]GABA by (+)etomidate and pentobarbital is blocked by GABA antagonists. These results indicate that hypnotic drugs such as (+)etomidate and pentobarbital, which are not structurally related, modulate diazepam and GABA binding sites via similar mechanisms.

摘要

依托咪酯（+）和戊巴比妥可增强[³H]地西泮和[³H]γ-氨基丁酸（[³H]GABA）与大脑皮层膜的结合。依托咪酯（+）和戊巴比妥均增加[³H]地西泮与其结合位点的亲和力。相比之下，它们增加了高亲和力和低亲和力GABA受体位点的最大结合容量（Bmax）。依托咪酯（+）和戊巴比妥对[³H]地西泮和[³H]GABA的增强作用被GABA拮抗剂阻断。这些结果表明，结构上不相关的催眠药物，如依托咪酯（+）和戊巴比妥，通过相似的机制调节地西泮和GABA结合位点。