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The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors
D S Choi1, G Birraux, J M Launay
1Laboratoire de Génétique Moléculaire des Eucaryotes du CNRS, U184 de Génétique et de Biologie Moléculaire de l'INSERM, Faculté de Médecine de Strasbourg, France.
Abstract:
The human serotonin 5-HT2B receptor, isolated from a human liver cDNA library, was transfected in COS-1 cells. Its pharmacological profile shows divergence with serotonin 5-HT2B receptors of other species. In particular, although strong correlation is observed between the human and the rat 5-HT2B receptor pharmacology, the correlation is almost as significant for the mouse 5-HT2B and the human 5-HT1D receptor agonists. The major sites of expression of its mRNA are in the human liver and kidney, with detectable expression in lung and heart. Therefore, this human 5-HT2B receptor could account for functions attributed to the peripheral 5-HT1D/5-HT2-like receptors, especially in the cardiovascular system. Thus, its detailed original pharmacology is of prime importance for therapeutic drug development.