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A series of N4-imidoethyl derivatives of 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A receptor ligands: synthesis and structure-affinity relationships.

作者信息

van Steen B J, van Wijngaarden I, Tulp M T, Soudijn W

机构信息

Department of Medicinal Chemistry, Solvay Duphar Research Laboratories, Weesp, The Netherlands.

出版信息

J Med Chem. 1995 Oct 13;38(21):4303-8. doi: 10.1021/jm00021a020.

DOI:10.1021/jm00021a020
PMID:7473558
Abstract

A series of unsubstituted and substituted succinimido, maleimido, and glutarimidoethyl derivatives of eltoprazine (3) was synthesized and tested for affinity for the 5-HT1A receptor in rat brain homogenates. The unsubstituted compounds have a moderate affinity for the receptor, while the affinity considerably increases by substitution at or enlargement of these cyclic ring systems. A good correlation was found between the inhibition constant Ki (expressed as pKi) and the lipophilicity (clogP). No correlation was observed between the pKi or pKi+ (local inhibition constant) and the basicity of the N4-nitrogen atom.

摘要

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