Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor

Savinainen, Kokkola, Outi Salo-Ahen, Poso, Järvinen, Laitinen

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    Abstract

    1. Several G protein-coupled receptors (GPCRs), including cannabinoid CB(1) and CB(2) receptors, show constitutive activity under heterologous expression. Such a tonic response is generated in the absence of an activating ligand, and can be inhibited by inverse agonists. Neutral antagonists, however, are silent at such receptors, but can reverse both agonist and inverse agonist responses. To date, no neutral antagonist for the CB(2) receptor has been reported. 2. Here, by monitoring receptor-dependent G protein activation, we demonstrate that WIN55212-3 acts as a neutral antagonist at the human CB(2) (hCB(2)) receptor. WIN55212-3 alone, at concentrations
    Original languageUndefined/Unknown
    Pages (from-to)636–645
    JournalBritish Journal of Pharmacology
    Volume145
    Issue number5
    DOIs
    Publication statusPublished - 2005
    MoE publication typeA1 Journal article-refereed

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