Chronic clonazepam administration induced benzodiazepine receptor subsensitivity

Jacqueline Crawley, P. J. Marangos, J. Stivers, F. K. Goodwin

Research output: Contribution to journalArticle

85 Scopus citations

Abstract

Clonazepam and chlordiazepoxide were administered chronically in increasing doses for three weeks in two different strains of mice. Forebrain [3H]diazepam binding was assayed in groups of mice sacrified at 2, 26, 50 hr and 10 days following the last dose. Scatchard and single point analyses revealed a significant decrease in the number of [3H]diazepam binding sites [Bmax] which persisted for at least two days following chronic clonazepam treatment. The Bmax changes observed following chlordiazepoxide treatment were less pronounced than those elicited by clonazepam. No significant changes in receptor binding affinity (Kd) were detected with either drug. In the clonazepam-treated animals, Bmax values returned to normal by day 10 after drug treatment. Chronic benzodiazepine administration therefore induced a decrease in the apparent number of benzodiazepine binding sites in the mouse forebrain. The magnitude and duration of the observed subsensitivity appears to depend on the potency of the administered benzodiazepine.

Original languageEnglish (US)
Pages (from-to)85-89
Number of pages5
JournalNeuropharmacology
Volume21
Issue number1
DOIs
StatePublished - 1982
Externally publishedYes

Keywords

  • benzodiazepine receptors
  • chlordiazepoxide
  • chronic administration
  • clonazepam
  • subsensitivity

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Drug Discovery
  • Pharmacology

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