ISOMERIC SELECTIVITY AT DOPAMINE-D(3) RECEPTORS

被引：40

作者：

BALDESSARINI, RJ

KULA, NS

MCGRATH, CR

BAKTHAVACHALAM, V

KEBABIAN, JW

NEUMEYER, JL

机构：

[1] MASSACHUSETTS GEN HOSP,MCLEAN DIV,MAILMAN RES CTR,NATICK,MA

[2] HARVARD UNIV,SCH MED,DEPT PSYCHIAT,NATICK,MA

[3] HARVARD UNIV,SCH MED,NEUROSCI PROGRAM,NATICK,MA

[4] RBI,NATICK,MA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 239卷 / 1-3期

关键词：

AMINOTETRALINS; DOPAMINE-D(3) RECEPTORS; 7-OH-DPAT; (7-HYDROXY-2-(N; N-DI-N-PROPYLAMINO)TETRALIN);

D O I：

10.1016/0014-2999(93)91011-B

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Racemic 7-hydroxy-N,N-dipropylaminotetralin (7-OH-DPAT) shows greater affinity for limbic-selective dopamine D3 receptors than for more ubiquitous dopamine D2 receptors. R(+)-7-OH-DPAT was prepared and evaluated in radioreceptor assays using membranes of fibroblasts expressing the human dopamine D3 receptor as well as rat striatal membranes containing dopamine D2. receptors. This enantiomer had 2-fold greater D3 affinity than the racemate and similarly greater D3 vs. D2 selectivity (64-fold). The results may facilitate development of D3 selective agents and evaluation of functions of these receptors.

引用

页码：269 / 270

页数：2

共 5 条

[1]

BALDESSARINI RJ, 1992, MOL PHARMACOL, V42, P856

[2] SYNTHESIS OF (R,S)-2'-TRANS-7-HYDROXY-2-[N-N-PROPYL-N-(3'-IODO-2'-PROPENYL)-AMINO]TETRALIN (TRANS-7-OH-PIPAT) - A NEW D3-DOPAMINE RECEPTOR-LIGAND [J].