. sigma. Ligands with Subnanomolar Affinity and Preference for the. sigma. 2 Binding Site. 1. 3-(. omega.-Aminoalkyl)-1H-indoles

J Perregaard, EK Moltzen, E Meier…

Index: Perregaard; Moltzen; Meier; Sanchez Journal of Medicinal Chemistry, 1995 ,  vol. 38,  # 11  p. 1998 - 2008

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Citation Number: 102

Abstract

29-253). This compound had the following binding affinities: IC50 (01)= 16 nM, IC50 (02)= 0.27 nM, IC50 (5-lIT. 1~)= 22 000 nM, IC50 (~-HT~ A)= 270 nM, IC50 (D2)= 4200 nM, IC50 (ad= 220 nM. Spiro-joining of the phenyl and the piperidine rings into a spiro [isobenzofkran- l (3H), 4'-piperidine1 ring system resulted in even more selective compounds. Variations of the l-substituent at the indole and of the chain length of the alkylene spacer group were ...