Enhancement of diazepam and gamma-aminobutyric acid binding by (+)etomidate and pentobarbital期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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

Authors:	R Thyagarajan R Ramanjaneyulu M K Ticku

Affiliation:	Division of Molecular Pharmacology, Department of Pharmacology, The University of Texas Health Science Center at San Antonio, San Antonio, Texas, U.S.A.

Abstract:	Abstract: (+) Etomidate and pentobarbital enhance [³H]diazepam and [³H]γ-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 B _max 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.

Keywords:	Hypnotics Benzodiazepines Etomidate GABA receptor Pentobarbital Picrotoxinin sites
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