Haloperidol-succinylglycyl[125I]iodotyrosine, a novel iodinated ligand for dopamine D2 receptors.
A novel radioiodinated ligand of the butyrophenone type has been synthesized for the quantification and characterization of dopamine D2 receptors. This haloperidol-derived ligand, haloperidol-succinylglycyl[125I]iodotyrosine ([125I]HSGTI), binds rapidly (equilibrium is reached within 30 min, at 10 pM and 37 degrees C) and with high affinity (Kd = 0.3 nM) to bovine striatal membranes. Its pharmacology, determined by competitive displacement with dopaminergic and non-dopaminergic drugs, is characteristic of binding to dopamine D2 receptors.
Garrigues
A M
AM
IBCN-CNRS, Bordeaux, France.
Gehelmann
F
F
Girault
J M
JM
Delaage
M
M
Labouesse
J
J
D000609:Aminoacridines; D000818:Animals; D001667:Binding, Competitive; D002417:Cattle; D002462:Cell Membrane / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism*; D006220:Haloperidol / Q000031:analogs & derivatives*; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D007700:Kinetics; D008024:Ligands; D007470:Monoiodotyrosine / Q000031:analogs & derivatives*; D011954:Receptors, Dopamine / Q000378:metabolism*
D000609:Aminoacridines; D007457:Iodine Radioisotopes; D008024:Ligands; D011954:Receptors, Dopamine; C054505:9-aminoacridine-4-carboxamide; C054504:haloperidol-succinylglycyliodotyrosine; D007470:Monoiodotyrosine; D006220:Haloperidol