Synthesis and structure-activity relationships of N, N'-di-o-tolylguanidine analogs, high-affinity ligands for the haloperidol-sensitive. sigma. receptor

MW Scherz, M Fialeix, JB Fischer…

Index: Scherz, Michael W.; Fialeix, Michelle; Fischer, James B.; Reddy, N. Laxma; Server, Alfred C.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2421 - 2429

Full Text: HTML

Citation Number: 87

Abstract

With an eye toward the development of novel atypical antipsychotic agents, we have studied the structure-affinity relationships of N,”-di-o-tolylguanidine (DTG, 3) and its congeners at the haloperidol-sensitive u receptor. A number of DTG analogues were synthesized and evaluated in in vitro radioligand displacement experiments with guinea pig brain membrane homogenates, using the highly u-specific radioligands [3H]-3 and [3H]-(+)-3-(3-hydroxy- ...