TY - JOUR
T1 - The human serotonin 5-HT2B receptor
T2 - Pharmacological link between 5-HT2 and 5-HT1D receptors
AU - Choi, Doo Sup
AU - Birraux, Guillaume
AU - Launay, Jean Marie
AU - Maroteaux, Luc
N1 - Funding Information:
Acknowledgements: We wish to acknowledge P. Hickel and D. Bon-doux for excellent technical assistance, J.-M. Gamier for providing the human cDNA libraries, M. Acker for help in tissue culture, A. Staub and F. Ruffenach for oligonucleotide synthesis, S. Vicaire for DNA sequencing, and B. Boulay for help in preparing the artwork of this manuscript. We thank O. Kellerman for critical reading of this manuscript and helpful discussions. This work has been supported by funds from the Centre National de la Recherche Scientifique, the Institut National de la Sant6 et de la Recherche Mrdical, the Centre Hospitalier Universitaire R6gional, and by grants from the Ministrre de la Recherche, from Rhrne-Poulenc-Rorer, from the Fondation pour la Recherche Mrdicale, and from the Association pour la Recherche contre le Cancer to L.M. and D.-S.C.
PY - 1994/10/3
Y1 - 1994/10/3
N2 - 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.
AB - 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.
KW - Cardiovascular system
KW - DOI binding
KW - G protein-coupled receptor
KW - Polymerase chain reaction
KW - cDNA cloning
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U2 - 10.1016/0014-5793(94)00968-6
DO - 10.1016/0014-5793(94)00968-6
M3 - Article
C2 - 7926008
AN - SCOPUS:0028168066
SN - 0014-5793
VL - 352
SP - 393
EP - 399
JO - FEBS Letters
JF - FEBS Letters
IS - 3
ER -