Production of fluorine-18 labeled (3-N-methyl)benperidol for PET investigation of cerebral dopaminergic receptor binding

Stephen M. Moerlein, William R. Banks, David Parkinson

Research output: Contribution to journalArticlepeer-review

19 Scopus citations

Abstract

The multi-millicurie synthesis of the D-2 receptor ligand [18F](3-N-methyl)benperidol (NMB; 1-[3-(4′-[18F]fluorobenzoyl)propyl]-4-(2-keto-3-methyl- 1-benzimidazolinyl)piperidine) is described. [18F]NMB was produced via a 3-step reaction sequence with an overall radiochemical yield of 5-10% and a specific activity > 3000 Ci/mmol within 100 min. In vitro binding assays indicated that NMB has high affinity for D-2 receptors in primate brain (Ki = 3.6 nM), with a receptor specificity exceeding that of spiperone. The technique described here permits the routine production of 10-20 mCi of this promising radiopharmaceutical for PET study of D-2 receptor binding in vivo.

Original languageEnglish
Pages (from-to)913-917
Number of pages5
JournalInternational Journal of Radiation Applications and Instrumentation. Part
Volume43
Issue number7
DOIs
StatePublished - Jul 1992

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