A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin-like growth factor 1 …

M Bouaboula, S Perrachon, L Milligan, X Canat… - Journal of Biological …, 1997 - ASBMB
In the present study, we showed that Chinese hamster ovary (CHO) cells transfected with
human central cannabinoid receptor (CB1) exhibit high constitutive activity at both levels of
mitogen-activated protein kinase (MAPK) and adenylyl cyclase. These activities could be
blocked by the CB1-selective ligand, SR 141716A, that functions as an inverse agonist.
Moreover, binding studies showed that guanine nucleotides decreased the binding of the
agonist CP-55,940, an effect usually observed with agonists, whereas it enhanced the …