Synthesis and in vivo evaluation of 122I- and 131I-labelled iodoperidol, a potential agent for the tomographic assessment of cerebral perfusion

Stephen M. Moerlein, Chester A. Mathis, Kathleen M. Brennan, Thomas F. Budinger

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

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% β+, t 1 2 = 3.6 min) in >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.

Original languageEnglish
Pages (from-to)91-93,95-98
JournalInternational Journal of Radiation Applications and Instrumentation.
Volume14
Issue number2
DOIs
StatePublished - 1987
Externally publishedYes

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