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5-HT3 receptors in NG108-15 neuroblastoma x glioma cells: effect of the novel agonist 1-(m-chlorophenyl)-biguanide.

作者信息

Boess F G, Sepúlveda M I, Lummis S C, Martin I L

机构信息

MRC Molecular Neurobiology Unit, MRC Centre, Cambridge, U.K.

出版信息

Neuropharmacology. 1992 Jun;31(6):561-4. doi: 10.1016/0028-3908(92)90188-u.

DOI:10.1016/0028-3908(92)90188-u
PMID:1407396
Abstract

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 microM. Displacement of the selective 5-HT3 receptor antagonist [3H]GR65630 by mCPBG revealed a Ki 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.

摘要

相似文献

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5-HT3 receptors in NG108-15 neuroblastoma x glioma cells: effect of the novel agonist 1-(m-chlorophenyl)-biguanide.
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2
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对稳定表达于HEK 293细胞中的人5-羟色胺3A型受体（h5-HT3R-AS）亚基的表征。
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