LY-320,135

Drugbox
IUPAC_name = 4- [6-methoxy-2-(4-methoxyphenyl)1-benzofuran-3-carbonyl] benzonitrile


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PubChem = 5311257
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chemical_formula = |C=24|H=17|N=1|O=4
molecular_weight = 383.395
smiles = c3cc(OC)ccc3-c2oc1cc(OC)ccc1c2C(=O)c4ccc(C#N)cc4
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LY-320,135 is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB₁. It was developed by Eli Lilly in the 1990s.

LY-320,135 displays fairly good selectivity, with a binding affinity for CB₁ around 70x stronger than for CB₂, [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] 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. [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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