Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor

Biochem Biophys Res Commun. 1993 Dec 30;197(3):1601-8. doi: 10.1006/bbrc.1993.2662.

Abstract

A human histamine H1 receptor gene lacking introns was isolated by screening a human genomic library with a bovine histamine H1 receptor probe. The deduced protein of 487 amino acids showed characteristic properties of G-protein-coupled receptors. The coding region was subcloned into the expression vector pSVL (Pharmacia), and the resulting construct transfected into COS-7 cells. Binding studies with [3H]pyrilamine on membranes from transfected cells revealed saturable specific binding with a KD of 1.2 nM and a Bmax of 3400 fmol/mg protein. Binding affinities of histamine and known histamine antagonists were similar to those for histamine H1 receptors in guinea-pig cerebellum. In transfected COS-7 cells, histamine induced inositol phosphate formation, that was inhibitable by pyrilamine.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Cattle
  • Cell Line
  • Cloning, Molecular
  • DNA / chemistry
  • DNA / metabolism
  • GTP-Binding Proteins / metabolism
  • Gene Expression*
  • Genomic Library
  • Hominidae / genetics*
  • Humans
  • Introns
  • Kinetics
  • Molecular Sequence Data
  • Pyrilamine / metabolism
  • Rats
  • Receptors, Histamine H1 / biosynthesis*
  • Receptors, Histamine H1 / genetics*
  • Receptors, Histamine H1 / metabolism
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / metabolism
  • Sequence Homology, Amino Acid
  • Transfection

Substances

  • Receptors, Histamine H1
  • Recombinant Proteins
  • DNA
  • GTP-Binding Proteins
  • Pyrilamine

Associated data

  • GENBANK/D17636
  • GENBANK/D17637
  • GENBANK/D17638
  • GENBANK/D17639
  • GENBANK/D17640
  • GENBANK/D17641
  • GENBANK/D17642
  • GENBANK/X71491
  • GENBANK/X76786
  • GENBANK/Z34897