3-(4-Piperidinyl)-and 3-(8-aza-bicyclo [3.2. 1] oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT 2A antagonists

…, R Marwood, D O'Connor, R Herbert, P Hutson…

Index: Crawforth, James; Goodacre, Simon; Maxey, Robert; Bourrain, Sylvie; Patel, Smita; Marwood, Rosemarie; O'Connor, Desmond; Herbert, Richard; Hutson, Peter; Rowley, Michael Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 24 p. 2701 - 2703

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Citation Number: 13

Abstract

A series of 3-(4-piperidinyl)-and 3-(8-aza-bicyclo [3.2. l] oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT2A receptor. 3-(8-Phenethyl-8-aza- bicyclo [3.2. l] oct-3-yI)-2-phenyl-1H-indole is a high-affinity (1.2 nM), selective (> 800 fold over h5-HT2C and hD2 receptors) antagonist at the h5-HT2A receptor with oral bioavailability in rats.