Novel (4-Phenylpiperidinyl)-and (4-Phenylpiperazinyl) alkyl-Spaced Esters of 1-Phenylcyclopentanecarboxylic Acids as Potent. sigma.-Selective Compounds

…, RB Mailman, DL DeHaven-Hudkins

Index: Hudkins, Robert L.; Mailman, Richard B.; DeHaven-Hudkins, Diane L. Journal of Medicinal Chemistry, 1994 , vol. 37, # 13 p. 1964 - 1970

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Citation Number: 16

Abstract

A series of novel 4-phenylpiperidinyl and (4-phenylpiperaziny1) alkyl l- phenylcyclopentanecar-boxylates was synthesized and evaluated for affinity at u1 and a2 sites by inhibition of L3H1-(+)-pentazocine (PENT) and PHI-1, 3-di (2-tolyl) guanidine (DTG) binding in guinea pig brain. The phenylpiperidines were more potent u ligands than the corresponding piperazines. Structural modifications varying the optimal spatial distance ...