PK 8165 and PK 9084, two quinoline derivatives with anxiolytic properties, antagonize the anticonvulsant effects of diazepam

Kelvin W. Gee, Roberta E. Brinton, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

PK 8165 and PK 9084 are two quinoline derivatives reported to interact with the benzodiazepine receptor and possess selective anxiolytic properties in vivo. In the present study we demonstrate that these two compounds antagonize the anticonvulsant effects of diazepam. In addition, in vitro binding studies indicate that both PK 8165 and PK 9084 interact competitively with [3H]flunitrazepam for brain benzodiazepine receptors. Based upon these findings, we propose the hypothesis that PK 8165 and PK 9084 act as partial agonists at the benzodiazepine receptor.

Original languageEnglish (US)
Pages (from-to)168-172
Number of pages5
JournalBrain Research
Volume264
Issue number1
DOIs
StatePublished - Mar 28 1983
Externally publishedYes

Keywords

  • (+)bicuculline
  • benzodiazepine receptor
  • benzodiazepine receptor antagonist
  • diazepam
  • PK 8165
  • PK 9084
  • quinoline derivatives
  • selective anxiolytic

ASJC Scopus subject areas

  • Neuroscience(all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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