Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor.
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Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor. / Savinainen, Juha R; Kokkola, Tarja; Salo, Outi M H; Poso, Antti; Järvinen, Tomi; Laitinen, Jarmo T.
in: BRIT J PHARMACOL, Jahrgang 145, Nr. 5, 5, 2005, S. 636-645.Publikationen: SCORING: Beitrag in Fachzeitschrift/Zeitung › SCORING: Zeitschriftenaufsatz › Forschung › Begutachtung
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T1 - Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor.
AU - Savinainen, Juha R
AU - Kokkola, Tarja
AU - Salo, Outi M H
AU - Poso, Antti
AU - Järvinen, Tomi
AU - Laitinen, Jarmo T
PY - 2005
Y1 - 2005
N2 - 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
AB - 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
M3 - SCORING: Zeitschriftenaufsatz
VL - 145
SP - 636
EP - 645
JO - BRIT J PHARMACOL
JF - BRIT J PHARMACOL
SN - 0007-1188
IS - 5
M1 - 5
ER -