Characterization of 5-HT2A receptor desensitization and the effect of cycloheximide on it in C6 cells

被引：5

作者：

Miyoshi, I

Kagaya, A

Kohchi, C

Morinobu, S

Yamawaki, S ^{[1
]}

机构：

[1] Hiroshima Univ, Sch Med, Dept Psychiat & Neurosci, Hiroshima, Japan

[2] Japan Sci & Technol Corp, Core Res & Evaluat Sci & Technol, Tokyo, Japan

[3] Hiroshima Univ, Radioisotope Ctr, Hiroshima, Japan

来源：

JOURNAL OF NEURAL TRANSMISSION | 2001年 / 108卷 / 03期

关键词：

5-MT2A receptor; desensitization; Ca; cycloheximide; C6 glioma cells;

D O I：

10.1007/s007020170070

中图分类号：

R74 [神经病学与精神病学];

学科分类号：

摘要：

Effect of prolonged pretreatment with serotonin (5-HT) on 5-HT2A receptor desensitization was examined by the measurement of intracellular calcium ([Ca2+](i)) mobilization in C6 cells. 5-HT-induced desensitization of [Ca2+](i) mobilization was in a time and dose dependent manner and reached a plateau after 3 hr. After 1 and 3 hr 5-HT pretreatment, 5-HT concentration in the medium little changed. 5-HT pretreatment with cycloheximide, a protein synthesis inhibitor, produced an enhancement of the desensitization for 3 and 6 hr pretreatment. However, 5-HT pretreatment for 3 and 6 hr caused no marked change in the 5-HT2A receptor mRNA level or G alphaq/11 protein in this study, suggesting that 5-HT may decrease 5-HT-induced [Ca2+](i) mobilization independent of 5-HT2A receptor mRNA or G-proteins. Endothelin-l-induced [Ca2+](i) mobilization did not alter after 5-HT and/or cycloheximide pretreatment. These results showed that activation of the 5-HT2A receptor induced homologous desensitization and pretreatment with 5-HT and/or cycloheximide did not change the efficacy of the second messenger pathway from Gq to a [Ca2+](i) rise.

引用

页码：249 / 260

页数：12

共 36 条

[1]

AKIYOSHI J, 1993, MOL PHARMACOL, V43, P349

[2]

APRISON MH, 1978, NEUROPHARMACOLOGY BE, P23

[3] PHARMACOLOGICAL CHARACTERIZATION OF REGULATION OF PHOSPHOINOSITIDE METABOLISM BY RECOMBINANT 5-HT2 RECEPTORS OF THE RAT [J].