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LY-320,135 displays fairly good selectivity, with a binding affinity for CB1 around 70x stronger than for CB2, but both its potency and selectivity are modest compared to newer agents, and at higher doses it also binds to a range of non-cannabinoid receptors. However LY-320,135 is still fairly widely used in research, particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses.
- Felder CC, Joyce KE, Briley EM, Glass M, Mackie KP, Fahey KJ, Cullinan GJ, Hunden DC, Johnson DW, Chaney MO, Koppel GA, Brownstein M. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. Journal of Pharmacology and Experimental Therapeutics. 1998 Jan;284(1):291-7. PMID 9435190
- Pertwee RG. Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sciences. 2005 Feb 4;76(12):1307-24. PMID 15670612
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