The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: saturable and reversible binding to rat cortex membranes

  • Eur J Pharmacol. 1992 Jul 7;217(2-3):203-5. doi: 10.1016/0014-2999(92)90851-t.
F P Jansen  1 ,  B Rademaker ,  A Bast ,  H Timmerman
Affiliations
  • 1. Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, Netherlands.
PMID: 1330590 DOI: 10.1016/0014-2999(92)90851-t
Abstract

We describe the binding to rat cortex membranes of [125I]iodophenpropit, the first radiolabeled histamine H3 antagonist. The binding of [125I]iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM; Bmax 209 fmol/mg of protein). Specific binding at a concentration of 0.3 nM accounted for 45-55% of the total binding. [125I]Iodophenpropit seems to fulfill the criteria for a suitable ligand for histamine H3 receptor binding studies.

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