| 词条 | LY-320,135 |
| 释义 |
| Watchedfields = changed | verifiedrevid = 424674882 | IUPAC_name = 4-[6-methoxy-2-(4-methoxyphenyl)1-benzofuran-3-carbonyl]benzonitrile | image = LY-320,135.png | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 176977-56-3 | ATC_prefix = | ATC_suffix = | PubChem = 5311257 | IUPHAR_ligand = 742 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID = 4470772 | ChEMBL = 411481 | UNII = CJY03984CT | 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 | StdInChI = 1S/C24H17NO4/c1-27-18-9-7-17(8-10-18)24-22(20-12-11-19(28-2)13-21(20)29-24)23(26)16-5-3-15(14-25)4-6-16/h3-13H,1-2H3 | StdInChIKey = RYNSGDFWBJWWSZ-UHFFFAOYSA-N }} 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 and Company in the 1990s. LY-320,135 displays fairly good selectivity, with a binding affinity for CB1 around 70x stronger than for CB2,[1] 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.[2] References1. ^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}} {{Cannabinoids}}{{cannabinoid-stub}}2. ^Pertwee RG. Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sciences. 2005 Feb 4;76(12):1307-24. {{PMID|15670612}} 7 : Cannabinoids|CB1 receptor antagonists|Benzofurans|Phenol ethers|Ketones|Nitriles|Eli Lilly and Company |
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