Production of fluorine-18 labeled (3-N-methyl)benperidol for PET investigation of cerebral dopaminergic receptor binding.
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.
Moerlein
S M
SM
Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110.
Banks
W R
WR
Parkinson
D
D
D000818:Animals; D001544:Benperidol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D001921:Brain / Q000000981:diagnostic imaging*; D005260:Female; D005462:Fluorine Radioisotopes; D066298:In Vitro Techniques; D007553:Isotope Labeling; D008254:Macaca nemestrina; D008297:Male; D011954:Receptors, Dopamine / Q000378:metabolism*; D017448:Receptors, Dopamine D2; D014055:Tomography, Emission-Computed
D005462:Fluorine Radioisotopes; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; C066786:N-methylbenperidol; D001544:Benperidol