These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol.
    Author: Bonetti EP, Burkard WP, Gabl M, Hunkeler W, Lorez HP, Martin JR, Moehler H, Osterrieder W, Pieri L, Polc P.
    Journal: Pharmacol Biochem Behav; 1988 Nov; 31(3):733-49. PubMed ID: 2855118.
    Abstract:
    The imidazobenzodiazepinone derivative Ro 15-4513 has the activity profile of a partial inverse (low efficacy) agonist at the benzodiazepine receptor (BZR). It reverses central nervous depressant effects of diazepam, and, in part, of phenobarbitone and ethanol in mice, rats and cats in behavioural, electrophysiological, and neurochemical paradigms. The interaction of Ro 15-4513 with barbiturates and ethanol is due to its inverse agonistic (negative allosteric modulatory) property at the BZR, as it was reversed by the selective BZR blocker flumazenil (Ro 15-1788). In the present experiment situations, other BZR partial inverse agonists in subconvulsant or overt convulsant doses were less effective against ethanol effects than Ro 15-4513. Possible mechanisms for this differential activity of BZR inverse agonists are discussed.
    [Abstract] [Full Text] [Related] [New Search]