Preparation and pharmacological evaluation of a novel series of 2-(phenylthio) benzo [b] thiophenes as selective MT 2 receptor ligands

C Mésangeau, M Fraise, P Delagrange…

文献索引：Mesangeau, Christophe; Fraise, Mikael; Delagrange, Philippe; Caignard, Daniel Henri; Boutin, Jean Albert; Berthelot, Pascal; Yous, Said European Journal of Medicinal Chemistry, 2011 , vol. 46, # 5 p. 1835 - 1840

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被引用次数: 20

摘要

A series of N-(2-(5-fluoro-2-(4-fluorophenylthio) benzo [b] thiophen-3-yl) ethyl) acylamides was synthesized and evaluated for binding affinity and intrinsic activity at melatonin receptors. The affinity of each compound for the melatonin receptors was determined by binding studies on cloned human MT1 and MT2 receptors expressed in CHO cells. Agonist and antagonist potency was measured on the [35S] GTPγS binding assay for the most ...