Literature DB >> 1407396

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

F G Boess1, M I Sepúlveda, S C Lummis, I L Martin.   

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.

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Year:  1992        PMID： 1407396     DOI： 10.1016/0028-3908(92)90188-u

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN： 0028-3908            Impact factor:   5.250


  7 in total

1.  Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.

Authors:  A G Hope; J A Peters; A M Brown; J J Lambert; T P Blackburn
Journal:  Br J Pharmacol       Date:  1996-07       Impact factor: 8.739

2.  Potentiation of chloride responses to glycine by three 5-HT3 antagonists in rat spinal neurones.

Authors:  D Chesnoy-Marchais
Journal:  Br J Pharmacol       Date:  1996-08       Impact factor: 8.739

3.  Characterization of 5-HT3 receptors of N1E-115 neuroblastoma cells by use of the influx of the organic cation [14C]-guanidinium.

Authors:  H Bönisch; M Barann; J Graupner; M Göthert
Journal:  Br J Pharmacol       Date:  1993-02       Impact factor: 8.739

4.  The interaction of trichloroethanol with murine recombinant 5-HT3 receptors.

Authors:  D L Downie; A G Hope; D Belelli; J J Lambert; J A Peters; K R Bentley; L J Steward; C Y Chen; N M Barnes
Journal:  Br J Pharmacol       Date:  1995-04       Impact factor: 8.739

5.  Selection of distinct conformational states of the 5-HT3 receptor by full and partial agonists.

Authors:  J A van Hooft; H P Vijverberg
Journal:  Br J Pharmacol       Date:  1996-03       Impact factor: 8.739

6.  An electrophysiological investigation of the properties of 5-HT3 receptors of rabbit nodose ganglion neurones in culture.

Authors:  J A Peters; H M Malone; J J Lambert
Journal:  Br J Pharmacol       Date:  1993-10       Impact factor: 8.739

7.  Electrophysiological consequences of ligand binding to the desensitized 5-HT3 receptor in mammalian NG108-15 cells.

Authors:  J T Bartrup; N R Newberry
Journal:  J Physiol       Date:  1996-02-01       Impact factor: 5.182
  7 in total

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