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Synthesis and preliminary evaluation of N 1 ‐methyl‐9‐[(1‐hydroxy‐3‐[ 18 F]fluoro‐2‐propoxy)methyl]guanine [ 18 F]MFHPG, a new substrate of HSV‐1‐thymidine kinase
Author(s) -
Noll B.,
Noll St.,
Grote M.,
Scheunemann M.,
Brust P.,
Friedrich A.,
Hauses M.,
Schackert H. K.,
Johannsen B.
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.25804401155
Subject(s) - chemistry , biodistribution , guanine , substrate (aquarium) , in vitro , labelling , stereochemistry , tritium , radiochemistry , biochemistry , gene , nucleotide , oceanography , geology , physics , nuclear physics
The labelling procedure for N 1 ‐methyl‐9‐[(1‐hydroxy‐3‐[ 18 F]fluoro‐2‐propoxy)methyl]guanine ([ 18 F]MFHPG), a novel substrate of HSV1‐TK that possess potent properties to image the gene expression, and its preliminary biodistribution in rats are reported. The biodistribution studies of [ 18 F]MFHPG in male Wistar rats show a fast blood clearance. The erythrocyte binding of the tracer was negligible and no metabolites were found. In vitro studies in HSV‐TK expressing cells reveal a lower uptake of [ 18 F]MFHPG than [ 18 F]FHPG which also correlates with the decreased octanol/water ratio.