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

A1 Originalartikel i en vetenskaplig tidskrift (referentgranskad)


Interna författare/redaktörer


Publikationens författare: Savinainen, Kokkola, Salo, Poso, Järvinen, Laitinen
Publiceringsår: 2005
Tidskrift: British Journal of Pharmacology
Tidskriftsakronym: Br J Pharmacol
Volym: 145
Nummer: 5
Artikelns första sida, sidnummer: 636
Artikelns sista sida, sidnummer: 645
ISSN: 0007-1188
eISSN: 1476-5381


Abstrakt

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

Senast uppdaterad 2020-26-02 vid 04:32