5-HT(3) RECEPTORS IN NG108-15 NEUROBLASTOMA X GLIOMA-CELLS - EFFECT OF THE NOVEL AGONIST 1-(META-CHLOROPHENYL)-BIGUANIDE

被引：29

作者：

BOESS, FG

SEPULVEDA, MI

LUMMIS, SCR

MARTIN, IL

机构：

[1] MRC Molecular Neurobiology Unit, MRC Centre, Cambridge, CB2 2QH, Hills Road

来源：

NEUROPHARMACOLOGY | 1992年 / 31卷 / 06期

关键词：

5-HT3; RECEPTORS; NG108-15; CELLS; 1-(META-CHLOROPHENYL)-BIGUANIDE; RADIOLIGAND BINDING; ELECTROPHYSIOLOGICAL; PARTIAL AGONIST;

D O I：

10.1016/0028-3908(92)90188-U

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

The effect of the novel agonist, 1-(m-chlorophenyl)-biguanide (mCPBG) was examined on 5-HT3 receptors in NG108-15 mouse neuroblastoma x rat glioma hybrid cells, using whole-cell voltage-clamp and radioligand binding on intact cells. Electrophysiological studies showed that mCPBG is a partial agonist, with an EC50 of 3.1-mu-M. Displacement of the selective 5-HT3 receptor antagonist [H-3]GR65630 by mCPBG revealed a K(i) of 14.2 nM. The study suggests that mCPBG may have a high affinity for desensitized 5-HT3 receptors and also revealed some differences between 5-HT3 receptors in NG108-15 and N1E-115 cells.

引用

页码：561 / 564

页数：4

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