A. Charalambous et al., SYNTHESIS OF (N-[C-11]METHYL)Y-29794, A COMPETITIVE INHIBITOR OF PROLYL ENDOPEPTIDASE, Journal of labelled compounds & radiopharmaceuticals, 34(6), 1994, pp. 499-503
Prolyl endopeptidase (PEP: [E.C.3.4.21.26]) is a widely distributed se
rine peptidase that cleaves a variety of oligopeptides in the brain an
d peripheral tissues. Y-29794 hylaminooctylthio)-6-isopropyl-3-pyridyl
-2-thienyl ketone) is a potent competitive reversible inhibitor of thi
s enzyme. In order to study the biodistribution of PEP in vivo we have
synthesized (N-[C-11]methyl)Y-29794, by [C-11]alkylation of the N-des
methyl precursor. The radiotracer was purified by silica gel Sep-Pak a
nd was obtained in 10-17% yields (EOB: synthesis times shorter than 45
min) with >98% radiochemical purities and specific activities >550 Ci
/mmol (EOS).