Enhancement of Diazepam and γ‐Aminobutyric Acid Binding by (+) Etomidate and Pentobarbital

R. Thyagarajan, R. Ramanjaneyulu, M. K. Ticku

Research output: Contribution to journalArticlepeer-review

54 Scopus citations

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 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.

Original languageEnglish (US)
Pages (from-to)578-585
Number of pages8
JournalJournal of neurochemistry
Volume41
Issue number2
DOIs
StatePublished - Feb 1983
Externally publishedYes

Keywords

  • Benzodiazepines
  • Etomidate
  • GABA receptor
  • Hypnotics
  • Pentobarbital
  • Picrotoxinin sites

ASJC Scopus subject areas

  • Biochemistry
  • Cellular and Molecular Neuroscience

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