| 词条 | GR-196,429 |
| 释义 |
| IUPAC_name = N-[2-(2,3,7,8-tetrahydrofuro[2,3-g]indol-1-yl)ethyl]acetamide | image = GR-196429_structure.png | width = 200 | tradename = | pregnancy_US = | legal_US = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 1349 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 170729-12-1 | ATC_suffix = | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | PubChem = 5311134 | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4470661 | C=14 | H=18 | N=2 | O=2 | molecular_weight = 246.308 | smiles = c23c1CCOc1ccc2CCN3CCNC(=O)C | StdInChI = 1S/C14H18N2O2/c1-10(17)15-6-8-16-7-4-11-2-3-13-12(14(11)16)5-9-18-13/h2-3H,4-9H2,1H3,(H,15,17) | StdInChIKey = LTYWTNUOUBBVNZ-UHFFFAOYSA-N }}GR-196,429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. It was one of the first synthetic melatonin agonists developed and continues to be used in scientific research, though it has never been developed for medical use. Studies in mice have shown GR-196,429 to produce both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release.[1][2][3] References1. ^Beresford IJ, Browning C, Starkey SJ, Brown J, Foord SM, Coughlan J, North PC, Dubocovich ML, Hagan RM. GR196429: a nonindolic agonist at high-affinity melatonin receptors. Journal of Pharmacology and Experimental Therapeutics. 1998 Jun;285(3):1239-45. {{PMID|9618428}} {{Melatonergics}}{{sedative-stub}}2. ^Beresford IJ, Harvey FJ, Hall DA, Giles H. Pharmacological characterisation of melatonin mt1 receptor-mediated stimulation of [35S]-GTPgammaS binding. Biochemical Pharmacology. 1998 Nov 1;56(9):1167-74. {{PMID|9802327}} 3. ^Drijfhout WJ, de Vries JB, Homan EJ, Brons HF, Copinga S, Gruppen G, Beresford IJ, Hagan RM, Grol CJ, Westerink BH. Novel non-indolic melatonin receptor agonists differentially entrain endogenous melatonin rhythm and increase its amplitude. European Journal of Pharmacology. 1999 Oct 15;382(3):157-66. {{PMID|10556666}} 2 : Acetamides|Melatonin receptor agonists |
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