5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl) sulfonyl] oxy] indolyl] ethylamines and their use as synthetic intermediates

…, P de Boer, H Wikström, SJ Peroutka…

Index: Barf; De Boer; Wikstrom; Peroutka; Svensson; Ennis; Ghazal; McGuire; Smith Journal of Medicinal Chemistry, 1996 , vol. 39, # 24 p. 4717 - 4726

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Citation Number: 23

Abstract

2-[5-[[(Trifluoromethyl) sulfonyl] oxy]-1 H-indol-3-yl] ethylamine (18), its N, N-di-n-propyl (12), N, N-diethyl (13), and N, N-dimethyl (14) derivatives, and 4-[3-[2-(N, N-dimethylamino) ethyl]- 1 H-indol-3-yl]-N-(p-methoxybenzyl) acrylamide (GR46611, 19) were synthesized and tested for binding affinities to cloned 5-HT1A, 5-HT1Dα, 5-HT1Dβ, and D2 receptors. In addition, the intrinsic efficacy was measured as the reduction of forskolin-stimulated cAMP in cells ...