Synthesis and in vivo evaluation of 122I- and 131I-labelled iodoperidol, a potential agent for the tomographic assessment of cerebral perfusion.
Iodoperidol (IP), an iodinated analogue of the antipsychotic drug haloperiodol, was evaluated as a cerebral blood flow radiopharmaceutical for PET or SPECT. IP was labelled with 131I or 122I (76% beta +, t1/2 = 3.6 min) in greater than 75% radiochemical yield via electrophilic aromatic iododestannylation. [131I]IP showed high cerebral uptake (1.9% of injected dose after 5 min) and good brain retention for the rat, with very low blood levels (brain/blood ratio = 35 at 2 h post injection). PET imaging of a dog demonstrated that [122I]IP has high selectivity for brain localization and good retention, and indicates that this class of compounds holds promise for development as perfusion radiopharmaceuticals.
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D002560:Cerebrovascular Circulation; D004285:Dogs; D005260:Female; D006220:Haloperidol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D007457:Iodine Radioisotopes; D009682:Magnetic Resonance Spectroscopy; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; C053199:iodoperidol; D006220:Haloperidol