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  • Title: AM630 is an inverse agonist at the human cannabinoid CB1 receptor.
    Author: Landsman RS, Makriyannis A, Deng H, Consroe P, Roeske WR, Yamamura HI.
    Journal: Life Sci; 1998; 62(9):PL109-13. PubMed ID: 9496703.
    Abstract:
    The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPgammaS binding to cell membranes was determined. WIN 55,212-2 (100 microM) stimulated basal [35S]GTPgammaS binding 77.9% with an EC50 value of 0.36 microM. Conversely, AM630 (100 microM) inhibited basal [35S]GTPgammaS binding by 20.9% with an EC50 value of 0.90 microM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.
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