Phenylpiperazinylmethylheterocycle derivatives: Synthesis and dopamine receptor binding profiles

被引：8

作者：

Abadi, AH ^{[1
]}

机构：

[1] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo 11562, Egypt

来源：

ARCHIV DER PHARMAZIE | 2004年 / 337卷 / 07期

关键词：

phenylpiperazinylmethylheterocycle derivatives; dopaminergic ligands;

D O I：

10.1002/ardp.200300838

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Four series of phenylpiperazinylmethylimidazo[1,2-a]pyridine, phenylpiperazinylmethylpyrrole, phenylpiperazinylmethylbenzofuran, and phenylpiperazinylmethylbenzothiophene derivatives were synthesized and investigated for their in vitro binding profiles for the dopamine receptor subtypes D-1, D-2long, D-2short, D-3 and D-4. All tested compounds showed selectivity towards the D-4 receptor subtype. Affinity and selectivity for D-4 follows the order imidazo[1,2-a]pyridine > benzofuran > benzothiophene > pyrrole derivatives. The D-4-related affinity and selectivity pattern seems to be dependent on the presence of a region of negative molecular electrostatic potential below the heterocyclic moiety.

引用

页码：383 / 390

页数：8

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