SR-48692 INHIBITS NEUROTENSIN-INDUCED [H-3] DOPAMINE RELEASE IN RAT STRIATAL SLICES AND MESENCEPHALIC CULTURES

被引：22

作者：

BROUARD, A

HEAULME, M

LEYRIS, R

PELAPRAT, D

GULLY, D

KITABGI, P

LEFUR, G

ROSTENE, W

机构：

[1] HOP ST ANTOINE,INST NATL SANTE & RECH MED,UNITE 339,F-75571 PARIS 12,FRANCE

[2] SANOFI RECH,F-34184 MONTPELLIER,FRANCE

[3] SANOFI RECH,F-31036 TOULOUSE,FRANCE

[4] CNRS,INST PHARMACOL MOLEC & CELLULAIRE,F-06560 VALBONNE,FRANCE

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1994年 / 253卷 / 03期

关键词：

RECEPTOR ANTAGONIST; NEUROTENSIN; DOPAMINE RELEASE; STRIATUM; MESENCEPHALIC CELL;

D O I：

10.1016/0014-2999(94)90204-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In rat striatal slices, the increase (114 +/- 11%) in K+-evoked [H-3]dopamine release induced by neurotensin (10 nM) was antagonized by 2-[(1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl)carboxylamino]tricyclo(3.3.1.1.(3.7))decan-2-carboxylic acid (SR 48692, IC50 = 1.2 +/- 0.11 nM). SR 48692 (100 nM) also suppressed the neurotensin (10 nM)-induced increase (47%) in K+-evoked [H-3]dopamine release in primary cultures of fetal rat mesencephalic cells. These results further characterize SR 48692 as a potent antagonist of neurotensin receptors in the rat.

引用

页码：289 / 291

页数：3

共 7 条

[1]

BROUARD A, 1992, J NEUROSCI, V12, P1409

[2] BIOCHEMICAL AND PHARMACOLOGICAL PROFILE OF A POTENT AND SELECTIVE NONPEPTIDE ANTAGONIST OF THE NEUROTENSIN RECEPTOR [J].