Interaction of clozapine with the histamine H3 receptor in rat brain

Br J Pharmacol. 1995 Apr;114(8):1523-4. doi: 10.1111/j.1476-5381.1995.tb14934.x.

Abstract

We examined possible interactions between neuroleptics and the histamine H3 receptor and found an interaction of clozapine with this receptor. In competition binding experiments, using the H3 antagonist, [125I]-iodophenpropit, we observed a Ki of 236 +/- 87 nM. Functionally, clozapine was studied on the H3-mediated inhibition of [3H]-5-hydroxytryptamine ([3H]-5-HT) release from rat brain cortex slices. Clozapine acts as an antagonist with an apparent KB value of 79.5 nM.

MeSH terms

  • Animals
  • Binding, Competitive
  • Cerebral Cortex / drug effects*
  • Cerebral Cortex / metabolism
  • Clozapine / pharmacology*
  • Haloperidol / pharmacology
  • Histamine Antagonists
  • Histamine Release / drug effects
  • Imidazoles / pharmacology
  • Isothiuronium / analogs & derivatives
  • Isothiuronium / pharmacology
  • Methylhistamines / pharmacology
  • Piperidines / pharmacology
  • Rats
  • Receptors, Histamine H3 / drug effects*
  • Receptors, Histamine H3 / metabolism

Substances

  • Histamine Antagonists
  • Imidazoles
  • Methylhistamines
  • Piperidines
  • Receptors, Histamine H3
  • Isothiuronium
  • iodophenpropit
  • alpha-methylhistamine
  • thioperamide
  • Clozapine
  • Haloperidol