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 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.
Choi
D S
DS
Laboratoire de Génétique Moléculaire des Eucaryotes du CNRS, U184 de Génétique et de Biologie Moléculaire de l'INSERM, Faculté de Médecine de Strasbourg, France.
Birraux
G
G
Launay
J M
JM
Maroteaux
L
L
D000595:Amino Acid Sequence; D000662:Amphetamines / Q000378:metabolism; D000818:Animals; D001483:Base Sequence; D002460:Cell Line; D002522:Chlorocebus aethiops; D018076:DNA, Complementary / Q000378:metabolism; D006801:Humans; D007668:Kidney; D007700:Kinetics; D008099:Liver / Q000378:metabolism*; D008969:Molecular Sequence Data; D016133:Polymerase Chain Reaction; D011985:Receptors, Serotonin / Q000096:biosynthesis / Q000737:chemistry / Q000378:metabolism*; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000737:chemistry / Q000378:metabolism; D012702:Serotonin Antagonists / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000378:metabolism / Q000494:pharmacology; D014162:Transfection
D000662:Amphetamines; D018076:DNA, Complementary; D011985:Receptors, Serotonin; D011994:Recombinant Proteins; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; C015952:4-iodo-2,5-dimethoxyphenylisopropylamine