(2S, 3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor
作者： Keiko Hosohata , Thomas H Burkey , Josua Alfaro-Lopez , Victor J Hruby , William R Roeske
DOI: 10.1016/S0014-2999(99)00516-6
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摘要: We examined the pharmacologic effect of beta-methyl-2',6'-dimethyltyrosine-L-tetrahydroisoquinone-3- carboxylic acid ((2S,3R)TMT-L-Tic-OH) on G protein activation in membranes prepared from Chinese Hamster Ovary cells transfected with cDNA human delta-opioid receptor. (2S,3R)TMT-L-Tic-OH inhibited to 58% basal an EC50 0.72 nM as determined by [35S]GTPgammaS binding. These findings suggest that is a highly potent inverse agonist at
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