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

Int J Rad Appl Instrum A. 1992 Jul;43(7):913-7. doi: 10.1016/0883-2889(92)90155-8.

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 greater than 3000 Ci/mmol within 100 min. In vitro binding assays indicated that NMB has high affinity for D-2 receptors in primate brain (K1 = 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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Benperidol / analogs & derivatives*
  • Benperidol / chemical synthesis
  • Benperidol / metabolism
  • Brain / diagnostic imaging*
  • Female
  • Fluorine Radioisotopes*
  • In Vitro Techniques
  • Isotope Labeling
  • Macaca nemestrina
  • Male
  • Receptors, Dopamine / metabolism*
  • Receptors, Dopamine D2
  • Tomography, Emission-Computed*

Substances

  • Fluorine Radioisotopes
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • N-methylbenperidol
  • Benperidol