Zaleplon and triazolam: Drug discrimination, plasma levels, and self-administration in baboons

Research output: Contribution to journalArticle

Abstract

Zaleplon is a chemically novel hypnotic that preferentially binds α1-subunit containing subtypes of the αβγ configuration of the γ-aminobutyric acid (GABA)(A) receptor. Zaleplon and the non-subtype-selective hypnotic triazolam occasioned 100% drug-appropriate responding in baboons trained to discriminate lorazepam or pentobarbital from vehicle. Flumazenil shifted the zaleplon generalization gradient at least five-fold to the right. A plasma elimination half-life of 6-8 h for oral 10 mg/kg zaleplon and 0.32 mg/kg triazolam was paralleled by discriminative control for 7 h. Zaleplon maintained self-injection greater than vehicle, as did comparison doses of the similarly selective hypnotic zolpidem and triazolam. Concurrent food-maintained responding increased during self-injection of all three drugs. Preferential binding at this α1-containing GABA(A) subtype did not diminish the benzodiazepine (Bzs)-like behavioral effects of zaleplon. (C) 2000 Elsevier Science Ireland Ltd.

Original languageEnglish (US)
Pages (from-to)55-68
Number of pages14
JournalDrug and alcohol dependence
Volume61
Issue number1
DOIs
StatePublished - Dec 22 2000

Keywords

  • Abuse potential
  • CL 284,846
  • Drug discrimination
  • Feeding
  • Flumazenil
  • Pharmacokinetics
  • Self-administr ation
  • Triazolam
  • Zaleplon
  • Zolpidem

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology
  • Psychiatry and Mental health
  • Pharmacology (medical)

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