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

A1 Journal article (refereed)


Internal Authors/Editors


Publication Details

List of Authors: Savinainen, Kokkola, Salo, Poso, Järvinen, Laitinen
Publication year: 2005
Journal: British Journal of Pharmacology
Journal acronym: Br J Pharmacol
Volume number: 145
Issue number: 5
Start page: 636
End page: 645
ISSN: 0007-1188
eISSN: 1476-5381


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

Last updated on 2019-15-10 at 03:25