TY - JOUR
T1 - Production of fluorine-18 labeled (3-N-methyl)benperidol for PET investigation of cerebral dopaminergic receptor binding
AU - Moerlein, Stephen M.
AU - Banks, William R.
AU - Parkinson, David
N1 - Funding Information:
Acknowledgements-The authors are grateful to W. Marge-nau and J. Robison for radioisotope production, and to T. L. Duckett for manuscript preparation. This work was supported in part by NIH FIRST Award NS-26788 (S.M.M.), NIH Grant HL-13851, and by the Animal Resources Program, University of Washington Regional Primate Center Grant RR00166.
PY - 1992/7
Y1 - 1992/7
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0026642617&partnerID=8YFLogxK
U2 - 10.1016/0883-2889(92)90155-8
DO - 10.1016/0883-2889(92)90155-8
M3 - Article
C2 - 1321101
AN - SCOPUS:0026642617
SN - 0883-2889
VL - 43
SP - 913
EP - 917
JO - International Journal of Radiation Applications and Instrumentation. Part
JF - International Journal of Radiation Applications and Instrumentation. Part
IS - 7
ER -