The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: saturable and reversible binding to rat cortex membranes.
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.
Jansen
F P
FP
Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, Netherlands.
Rademaker
B
B
Bast
A
A
Timmerman
H
H
D000818:Animals; D001665:Binding Sites; D002540:Cerebral Cortex / Q000378:metabolism*; D006633:Histamine Antagonists; D007093:Imidazoles / Q000378:metabolism*; D007457:Iodine Radioisotopes; D007550:Isothiuronium / Q000031:analogs & derivatives* / Q000378:metabolism; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D011968:Receptors, Histamine / Q000378:metabolism*; D018100:Receptors, Histamine H3
D006633:Histamine Antagonists; D007093:Imidazoles; D007457:Iodine Radioisotopes; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; D007550:Isothiuronium; C077791:iodophenpropit