Characterization and tissue distribution of H3 histamine receptors in guinea pigs by N alpha-methylhistamine

Biochem Biophys Res Commun. 1990 May 16;168(3):979-86. doi: 10.1016/0006-291x(90)91125-c.


We have used [3H]N alpha-methylhistamine to characterize H3-binding in the guinea pig brain and to study its tissue distribution. Kinetic and equilibrium binding experiments indicate a single class of high affinity sites in membranes isolated from guinea pig brain tissue (Kd = 0.4 nM, Bmax = 41 fmol/mg of protein). Competition binding experiments have confirmed that this ligand associates with H3-receptors and, under the conditions used in these experiments, does not bind to H1- or H2-receptors. Although there was some binding in the ileum and large intestine, H3-binding was found primarily in the central nervous system.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Binding, Competitive
  • Brain / metabolism
  • Guinea Pigs
  • Kinetics
  • Methylhistamines / metabolism*
  • Receptors, Histamine / metabolism*
  • Receptors, Histamine H1 / metabolism
  • Receptors, Histamine H2 / metabolism
  • Receptors, Histamine H3


  • Methylhistamines
  • Receptors, Histamine
  • Receptors, Histamine H1
  • Receptors, Histamine H2
  • Receptors, Histamine H3