Native Serotonin 5-HT3 Receptors Expressed in Xenopus Oocytes Differ from Homopentameric 5-HT3 Receptors |
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| Authors: | Johannes A van Hooft Angélique P Kreikamp Henk P M Vijverberg |
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| Institution: | Research Institute of Toxicology, Utrecht University, Utrecht, The Netherlands |
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| Abstract: | Abstract: Efficacies of the 5-hydroxytryptamine (serotonin) 5-HT3 receptor (5-HT3R) agonists 2-methyl-5-HT, dopamine, and m -chlorophenylbiguanide on 5-HT3R native to N1E-115 cells and on homopentameric 5-HT3R expressed in Xenopus oocytes were determined relative to that of 5-HT. Efficacies of 2-methyl-5-HT and dopamine on 5-HT3R native to differentiated N1E-115 cells are high (54 and 36%) as compared with their efficacies on homopentameric 5-HT3R-AL and 5-HT3R-As receptors expressed in oocytes (4–8%). m -Chlorophenylbiguanide does not distinguish between 5-HT3R in N1E-115 cells and in oocytes. The distinct pharmacological profile of 5-HT3R native to differentiated N1E-115 cells is conserved when poly(A)+ mRNA from these cells is expressed in oocytes. The results indicate that, apart from the known 5-HT3R subunits, N1E-115 cells express additional proteins involved in 5-HT3R function. |
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| Keywords: | Serotonin 5-HT3 receptor N1E-115 neuroblastoma cell Xenopus oocytes Receptor heterogeneity Full and partial agonists |
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