Psychopharmacology

, Volume 86, Issue 4, pp 464–467

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

  • T. Mennini
  • D. Barone
  • M. Gobbi
Original Investigations

DOI: 10.1007/BF00427909

Cite this article as:
Mennini, T., Barone, D. & Gobbi, M. Psychopharmacology (1985) 86: 464. doi:10.1007/BF00427909

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.

Key words

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

Copyright information

© Springer-Verlag 1985

Authors and Affiliations

  • T. Mennini
    • 1
  • D. Barone
    • 2
  • M. Gobbi
    • 1
  1. 1.Istituto di Ricerche Farmacologiche “Mario Negri”MilanItaly
  2. 2.Lepetit Research LaboratoriesMilanItaly

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