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  • Title: Enhancement of diazepam and gamma-aminobutyric acid binding by (+)etomidate and pentobarbital.
    Author: Thyagarajan R, Ramanjaneyulu R, Ticku MK.
    Journal: J Neurochem; 1983 Aug; 41(2):578-85. PubMed ID: 6308164.
    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.
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