HOMOLOGOUS DESENSITIZATION OF SEROTONIN-5-HT(2) RECEPTOR-STIMULATED INTRACELLULAR CALCIUM MOBILIZATION IN C6BU-1 GLIOMA-CELLS VIA A MECHANISM INVOLVING A CALMODULIN PATHWAY

被引：38

作者：

KAGAYA, A ^{[1
]}

MIKUNI, M ^{[1
]}

MURAOKA, S ^{[1
]}

SAITOH, K ^{[1
]}

OGAWA, T ^{[1
]}

SHINNO, H ^{[1
]}

YAMAWAKI, S ^{[1
]}

TAKAHASHI, K ^{[1
]}

机构：

[1] HIROSHIMA UNIV,SCH MED,DEPT PSYCHIAT & NEUROSCI,HIROSHIMA 730,JAPAN

来源：

JOURNAL OF NEUROCHEMISTRY | 1993年 / 61卷 / 03期

关键词：

SEROTONIN-5-HT(2) RECEPTORS; INTRACELLULAR CALCIUM MOBILIZATION; HOMOLOGOUS DESENSITIZATION; RAT GLIOMA C6BU-1 CELLS; W-7; CALMODULIN ANTAGONIST;

D O I：

10.1111/j.1471-4159.1993.tb03619.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Serotonin 5-HT2 receptor-mediated intracellular Ca2+ mobilization was investigated in rat glioma C6BU-1 cells. The receptors became desensitized after previous exposure to 5-HT in a time- and concentration-dependent manner. The desensitization of 5-HT2 receptor-mediated intracellular signaling appeared to be homologous because previous exposure to 5-HT did not alter the response to other transmitters such as thrombin or isoproterenol and because previous exposure to thrombin or isoproterenol did not diminish the response to 5-HT. The desensitization induced by pretreatment with 5-HT was potently prevented by the naphthalenesulfonamide derivative W-7, a calmodulin antagonist, when it was cosupplied with 5-HT. Furthermore, the preventive effect of W-7 was greater than that of W-5, a weak analogue of W-7, and than that of H-7, a nonselective inhibitor of protein kinases. These results suggest that 5-HT2 receptor-mediated Ca2+ mobilization can be desensitized homologously after prolonged exposure to 5-HT in a calmodulin-dependent manner in rat glioma C6BU-1 cells.

引用

页码：1050 / 1056

页数：7

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