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The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: saturable and reversible binding to
F P Jansen1, B Rademaker, A Bast
1Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, Netherlands.
European Journal of Pharmacology
|July 7, 1992
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.