Histamine H1 Receptors Identified in Mammalian Brain Membranes With [3H]mepyramine

Proc Natl Acad Sci U S A. 1978 Dec;75(12):6290-4. doi: 10.1073/pnas.75.12.6290.


The antihistamine [3H]mepyramine binds to H1 histamine receptors in mammalian brain membranes. Potencies of H1 antihistamines at the binding sites correlate with their pharmacological antihistamine effects in the guinea pig ileum. Specific [3H]mepyramine binding is saturable with a dissociation constant of about 4 nM in both equilibrium and kinetic experiments and a density of 10 pmol per gram of whole kinetic experiments and a density of 10 pmol per gram of whole brain. Some tricyclic antidepressants are potent inhibitors of specific [3H]mepyramine binding. Regional variations of [3H]mepyramine binding do not correlate with variations in endogeneous histamine and histidine decarboxylase activity.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amines / metabolism
  • Animals
  • Binding, Competitive
  • Brain / anatomy & histology
  • Brain / metabolism*
  • Cattle
  • Guinea Pigs
  • Kinetics
  • Male
  • Pyrilamine / metabolism
  • Rats
  • Receptors, Histamine / metabolism*
  • Receptors, Histamine H1 / metabolism*
  • Structure-Activity Relationship
  • Synaptic Membranes / metabolism


  • Amines
  • Receptors, Histamine
  • Receptors, Histamine H1
  • Pyrilamine