Cloning and pharmacological characterization of the monkey histamine H3 receptor

Eur J Pharmacol. 2003 Dec 15;482(1-3):49-60. doi: 10.1016/j.ejphar.2003.09.072.

Abstract

Species differences have been described previously for histamine H(3) receptor pharmacology. Rat selective histamine H(3) receptor ligands such as ciproxifan and A-304121 (2-amino-1-[4-[3-(4-cyclopropanecarbonyl-phenoxy)-propyl]-piperazin-1-yl]-propan-1-one) show over 100-fold selectivity for the rat receptor compared to the human receptor. To date, however, the pharmacology of the cloned monkey histamine H(3) receptor has not been examined. In this study, we cloned the monkey histamine H(3) receptor gene (H(3)R) and evaluated the receptor pharmacology in binding and functional assays. The monkey histamine H(3) receptor is highly homologous to the human receptor with 438 identities in their 445 amino acid sequences, but less homologous to the rat receptor. However, unlike the human or rat, we found no evidence for additional splicing for the monkey H(3)R. Pharmacological analysis indicated that the monkey receptor exhibited similar pharmacological profiles to those of the human receptor, providing critical information for characterizing histamine H(3) receptor ligands in monkey behavioral models.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence / genetics
  • Animals
  • Cell Line
  • Cloning, Molecular / methods
  • Dose-Response Relationship, Drug
  • Histamine Agonists / metabolism
  • Histamine Agonists / pharmacology*
  • Histamine Antagonists / metabolism
  • Histamine Antagonists / pharmacology*
  • Humans
  • Macaca mulatta / genetics*
  • Macaca mulatta / metabolism*
  • Molecular Sequence Data
  • Protein Binding / drug effects
  • Protein Binding / physiology
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism
  • Rats
  • Receptors, Histamine H3 / genetics*
  • Receptors, Histamine H3 / metabolism*
  • Sequence Homology, Amino Acid

Substances

  • Histamine Agonists
  • Histamine Antagonists
  • Protein Isoforms
  • Receptors, Histamine H3

Associated data

  • GENBANK/AY231164