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Synthesis and evaluation in primates of (N‐[ 11 C]methyl)‐benperidol as a pet tracer of cerebral D2 receptor binding
Author(s) -
Moerlein S. M.,
Welch M. J.,
Perlmutter J. S.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580440174
Subject(s) - radioligand , chemistry , receptor , ligand (biochemistry) , specific activity , pet imaging , radiochemistry , tracer , positron emission tomography , nuclear medicine , pharmacology , biochemistry , medicine , enzyme , physics , nuclear physics
The routine production of the D2 receptor‐binding radioligand [ 11 C]NMB has been optimized. Uncorrected batch yields of 62–105 mCi of [ 11 C]NMB are obtained within 35 minutes EOB, with a specific activity exceeding 500 Ci/mmol and a radiochemical purity exceeding 95%. PET imaging of baboons shows rapid, specific localization of [ 11 C]NMB to cerebral D2 receptor‐rich tissue of primate brain. The specific localization of the radioligand is altered by drug challenge or pathological conditions, indicating utility of the ligand for human application.