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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Amphetamines / metabolism
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Animals
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Base Sequence
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Cell Line
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Chlorocebus aethiops
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DNA, Complementary / metabolism
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Humans
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Kidney
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Kinetics
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Liver / metabolism*
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Molecular Sequence Data
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Polymerase Chain Reaction
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Receptors, Serotonin / biosynthesis
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Receptors, Serotonin / chemistry
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Receptors, Serotonin / metabolism*
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Recombinant Proteins / biosynthesis
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Recombinant Proteins / chemistry
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Recombinant Proteins / metabolism
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Serotonin Antagonists / pharmacology
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Serotonin Receptor Agonists / metabolism
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Serotonin Receptor Agonists / pharmacology
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Transfection
Substances
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Amphetamines
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DNA, Complementary
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Receptors, Serotonin
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Recombinant Proteins
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Serotonin Antagonists
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Serotonin Receptor Agonists
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4-iodo-2,5-dimethoxyphenylisopropylamine