The human cannabinoid CB(1) receptor stably expressed in Chinese hamster ovary cells provides a model system to predict the pharmacological effects of cannabinoids in man

摘要: Since the cloning of only known cannabinoid receptor in human brain, CB„ scientists have been trying to elucidate mechanisms action this receptor. The possibility yet unidentified receptors brain makes it important be certain that any results obtained from studies CB, are due strictly Therefore, cloned has stably expressed Chinese Hamster Ovary (CHO/CB,) cells, which do not endogenously express and receptors. Saturation binding using f H]SR1417l6Aand [^H]CP55,940 determined system expresses at approximately 1.8 pmoles receptor/mg protein expression is able differentially bind agonists (CP55,940) antagonists (SR141716A). In [^®S]GTPyS assay, CP55,940, WIN 55,212-2 HU-2I0 full agonists, methanandamide 11-OH-A'THC partial A'-THC a competitive antagonist SR141716A AM630 inverse agonists. for consistent with those reported these compounds mammalian brain. findings [^^S]GTPyS assay novel, CP55,940 were also shown by maximally inhibiting forskolin-stimulated cAMP formation CHO/CB, cells. finding an agonist was further supported its ability augment formation. Interestingly, since inhibited formation, but lesser extent