Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor.
We have cloned the peripheral cannabinoid receptor, mCB2, from a mouse splenocyte cDNA library. The 3.7 kb sequence contains an open reading frame encoding a protein of 347 residues sharing 82% overall identity with the only other known peripheral receptor, human CB2 (hCB2) and shorter than hCB2 by 13 amino acids at the carboxyl terminus. Binding experiments with membranes from COS-3 cells transiently expressing mCB2 showed that the synthetic cannabinoid WIN 55212-2 had a 6-fold lower affinity for mCB2 than for hCB2, whereas both receptors showed similar affinities for the agonists CP 55,940, delta(9)-THC and anandamide and almost no affinity for the central receptor- (CB1) specific antagonist SR 141716A. Both hCB2 and mCB2 mediate agonist-stimulated inhibition of forskolin-induced cAMP production in CHO cell lines permanently expressing the receptors. SR 141716A failed to antagonize this activity in either cell line, confirming its specificity for CB1.
Shire
D
D
Sanofi Recherche, Centre de Labège, France.
Calandra
B
B
Rinaldi-Carmona
M
M
Oustric
D
D
Pessègue
B
B
Bonnin-Cabanne
O
O
Le Fur
G
G
Caput
D
D
Ferrara
P
P
D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D002186:Cannabinoids / Q000378:metabolism*; D003001:Cloning, Molecular; D018076:DNA, Complementary; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000235:genetics* / Q000378:metabolism; D017386:Sequence Homology, Amino Acid
D002186:Cannabinoids; D018076:DNA, Complementary; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug