5-Methyl-1-(3-pyridylcarbamoyl)-1, 2, 3, 5-tetrahydropyrrolo [2, 3-f] indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral …

IT Forbes, P Ham, DH Booth, RT Martin…

Index: Forbes, Ian T.; Ham, Peter; Booth, Deborah H.; Martin, Roger T.; Thompson, Mervyn; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 14 p. 2524 - 2530

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Citation Number: 72

Abstract

The preparation of a series of conformationally restricted analogues of indolylurea 1, namely tetrahydropyrroloindoles and tetrahydropyrroloquinolines, is described. The binding affinities of these compounds at 5-HTu,~-HT~ B, and 5-HT2c receptors were determined. Of these compounds, the 1, 2, 3, 5-tetrahydropyrrolo [2, 3-flindole derivative, compound 11, was found to have high affinity for the 5-HT2c (~ KI 8.0) and~-HT~ B receptors (pA2 8.51, ...