5-HT3 receptors in NG108-15 neuroblastoma x glioma cells: effect of the novel agonist 1-(m-chlorophenyl)-biguanide.
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.
Boess
F G
FG
MRC Molecular Neurobiology Unit, MRC Centre, Cambridge, U.K.
Sepúlveda
M I
MI
Lummis
S C
SC
Martin
I L
IL
D000818:Animals; D001645:Biguanides / Q000494:pharmacology*; D001667:Binding, Competitive; D005071:Evoked Potentials / Q000187:drug effects; D005910:Glioma; D006822:Hybrid Cells / Q000187:drug effects / Q000502:physiology; D007093:Imidazoles / Q000378:metabolism; D007211:Indoles / Q000378:metabolism; D007700:Kinetics; D051379:Mice; D009447:Neuroblastoma; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism / Q000502:physiology*; D012701:Serotonin / Q000031:analogs & derivatives / Q000494:pharmacology; D012702:Serotonin Antagonists
D001645:Biguanides; D007093:Imidazoles; D007211:Indoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C059068:GR 65630; D012701:Serotonin; C045918:2-methyl-5-HT; C065734:1-(3-chlorophenyl)biguanide