In vivo interaction of premazepam with benzodiazepine receptors: Relation to its pharmacological effects

T. Mennini, D. Barone, M. Gobbi

Research output: Contribution to journalArticle

Abstract

The study of in vivo occupancy of benzodiazepine receptors in rat hippocampus and cerebellum indicates that premazepam reaches only about 70% and 80% occupancy respectively within the dose range used for pharmacological tests in rats. Moreover, at equiactive doses (antileptazol ED50), more brain receptors are occupied by premazepam than by other benzodiazepines, suggesting that premazepam may act as a partial agonist at benzodiazepine receptors, with intrinsic activity lower in cerebellum than in hippocampus. These results may explain the lack of sedative and ataxic properties of premazepam.

Original languageEnglish
Pages (from-to)464-467
Number of pages4
JournalPsychopharmacology
Volume86
Issue number4
DOIs
Publication statusPublished - Aug 1985

Fingerprint

GABA-A Receptors
Pharmacology
Cerebellum
Hippocampus
Hypnotics and Sedatives
Benzodiazepines
premazepam
Brain

Keywords

  • Anticonvulsant effect
  • Benzodiazepine receptors
  • Diazepam
  • In vivo occupancy e/o binding
  • Muscle relaxant effect
  • Premazepam

ASJC Scopus subject areas

  • Pharmacology

Cite this

In vivo interaction of premazepam with benzodiazepine receptors : Relation to its pharmacological effects. / Mennini, T.; Barone, D.; Gobbi, M.

In: Psychopharmacology, Vol. 86, No. 4, 08.1985, p. 464-467.

Research output: Contribution to journalArticle

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