THE HUMAN SEROTONIN 5-HT2B RECEPTOR - PHARMACOLOGICAL LINK BETWEEN 5-HT2 AND 5-HT1D RECEPTORS

The human serotonin 5-HT2B receptor, isolated from a human liver cDNA library, was transfected in COS-1 cells. Its pharmacological profile s hows divergence with serotonin 5-HT2B receptors of other species. In p articular, although strong correlation is observed between the human a nd the rat 5-HT2B receptor pharmacology, the correlation is almost as significant for the mouse 5-HT2B and the human 5-HT1D receptor agonist s. The major sites of expression of its mRNA are in the human liver an d kidney, with detectable expression in lung and heart. Therefore, thi s human 5-HT2B receptor could account for functions attributed to the peripheral 5-HT1D/5-HT2-like receptors, especially in the cardiovascul ar system. Thus, its detailed original pharmacology is of prime import ance for therapeutic drug development.