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Enhancement of Diazepam and γ‐Aminobutyric Acid Binding by (+) Etomidate and Pentobarbital
Author(s) -
Thyagarajan R.,
Ramanjaneyulu R.,
Ticku M. K.
Publication year - 1983
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1983.tb04778.x
Subject(s) - etomidate , pentobarbital , diazepam , aminobutyric acid , hypnotic , chemistry , pharmacology , gabaa receptor , receptor , biochemistry , medicine , propofol
(+) Etomidate and pentobarbital enhance [ 3 H]diazepam and [ 3 H]γ‐aminobutyric acid ([ 3 H]GABA) binding to cerebral cortex membranes. Both (+)etomidate and pentobarbital increase the affinity of [ 3 H]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 [ 3 H]diazepam and [ 3 H]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.