Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3, 4-dichlorophenyl) ethyl]-N-methylethylenediamines as. sigma. receptor …

…, XS He, W Williams, L Radesca, W Bowen

Index: Costa, Brian R. de; Dominguez, Celia; He, Xiao-shu; Williams, Wanda; Radesca, Lilian; Bowen, Wayne Journal of Medicinal Chemistry, 1992 , vol. 35, # 23 p. 4334 - 4343

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Citation Number: 32

Abstract

[(-)-4]. In this displacement assay,(+)-pentazocine exhibited a Ki of 3.1 nM while DTG and haloperidol showed Ki values of 27.7 and 3.7 nM, respectively. The conformationally free parent compound 1 exhibited a Ki value of 2.1 nM. Comparison of both the u receptor affinities and nitrogen atom geometry of the compounds revealed that a gauche relation of the nitrogen atoms of cis-1, 2-cyclohexanediamines is not imperative for high affinity as we ...