Inhibition of sleep and benzodiazepine receptor binding by a β-carboline derivative

Joseph V. Martin, James M. Cook, Timothy J. Hagen, Wallace B. Mendelson

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

The effects of systemic injections of β-carboline-3-carboxylate-t-butyl ester (β-CCtB) were investigated with regard to normally occurring sleep and several measures of benzodiazepine receptor occupancy in rats. A dose of 30mg/kg of β-CCtB was found to have a long time-course of action as measured by an in vivo assay for benzodiazepine binding, with an 84% depletion of [3H]diazepam binding at one hour after the intraperitoneal injection. This dose of β-CCtB was shown to delay sleep onset, decrease non-REM and total sleep in the first two hours after the injection, and to delay the appearance of REM sleep after the sleep onset. The dose- and time-dependence of the effects on sleep approximated the dose- and time-dependence of inhibitory effects of an IP injection of β-CCtB on in vitro measures of benzodiazepine receptor affinity and number.

Original languageEnglish (US)
Pages (from-to)37-42
Number of pages6
JournalPharmacology, Biochemistry and Behavior
Volume34
Issue number1
DOIs
StatePublished - Sep 1989

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Toxicology
  • Pharmacology
  • Clinical Biochemistry
  • Biological Psychiatry
  • Behavioral Neuroscience

Keywords

  • Benzodiazepine
  • Inverse agonist
  • REM
  • Sleep
  • β-Carboline-3-carboxylate-t-butyl ester

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