The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors

FEBS Lett. 1994 Oct 3;352(3):393-9. doi: 10.1016/0014-5793(94)00968-6.

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

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Amphetamines / metabolism
  • Animals
  • Base Sequence
  • Cell Line
  • Chlorocebus aethiops
  • DNA, Complementary / metabolism
  • Humans
  • Kidney
  • Kinetics
  • Liver / metabolism*
  • Molecular Sequence Data
  • Polymerase Chain Reaction
  • Receptors, Serotonin / biosynthesis
  • Receptors, Serotonin / chemistry
  • Receptors, Serotonin / metabolism*
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Serotonin Antagonists / pharmacology
  • Serotonin Receptor Agonists / metabolism
  • Serotonin Receptor Agonists / pharmacology
  • Transfection

Substances

  • Amphetamines
  • DNA, Complementary
  • Receptors, Serotonin
  • Recombinant Proteins
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • 4-iodo-2,5-dimethoxyphenylisopropylamine

Associated data

  • GENBANK/Z36748