SR 48692抑制神经降压素诱导的大鼠纹状体切片和中脑培养物中[3H]多巴胺的释放。

SR 48692 inhibits neurotensin-induced [3H]dopamine release in rat striatal slices and mesencephalic cultures.

作者信息

Brouard A, Heaulme M, Leyris R, Pelaprat D, Gully D, Kitabgi P, Le Fur G, Rostene W

机构信息

Institut National de la Santé et de la Recherche Médicale, Unité 339, Hôpital Saint Antoine, Paris, France.

出版信息

Eur J Pharmacol. 1994 Mar 3;253(3):289-91. doi: 10.1016/0014-2999(94)90204-6.

DOI:10.1016/0014-2999(94)90204-6

PMID:8200423

Abstract

In rat striatal slices, the increase (114 +/- 11%) in K(+)-evoked [3H]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 [3H]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.

摘要

在大鼠纹状体切片中，神经降压素（10 nM）诱导的K⁺诱发的[³H]多巴胺释放增加（114±11%）被2-[(1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)吡唑-3-基)羧基氨基]三环(3.3.1.1.3.7)癸烷-2-羧酸（SR 48692，IC50 = 1.2±0.11 nM）拮抗。SR 48692（100 nM）还抑制了神经降压素（10 nM）诱导的胎鼠中脑细胞原代培养物中K⁺诱发的[³H]多巴胺释放增加（47%）。这些结果进一步将SR 48692表征为大鼠中神经降压素受体的强效拮抗剂。