Abstract

The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB 1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [ 35S]GTPγS binding to cell membranes was determined. WIN 55,212-2 (100 μM) stimulated basal [ 35S]GTPγS binding 77.9% with an EC 50 value of 0.36 μM. Conversely, AM630 (100 μM) inhibited basal [ 35S]GTPγS binding by 20.9% with an EC 50 value of 0.90 μM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.

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