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Radiosynthesis of [4‐ O‐methyl ‐ 11 C]KF18446 as a potential ligand for the central adenosine a 2A receptor and comparison with [4‐ O‐methyl ‐ 11 C]KW6002 in rats
Author(s) -
Turton D. R.,
Hirani E.,
Osman S.,
Poole K.,
Falokun G.,
Brady F.,
Karasawa A.,
Shimada J.,
Brooks D. J.,
Hume S.,
Luthra S. K.
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.2580440195
Subject(s) - chemistry , radiosynthesis , ligand (biochemistry) , adenosine , cortex (anatomy) , antagonist , stereochemistry , medicinal chemistry , receptor , biochemistry , positron emission tomography , neuroscience , psychology
The adenosine A 2A antagonist, KF18446 was labelled in the aromatic O ‐methyl position using [ 11 C]iodomethane. [4‐ O ‐ methyl ‐ 11 C]KF18446 and [4‐ O ‐ methyl ‐ 11 C]KW‐6002, an adenosine A 2A antagonist that we radiolabelled previously, were evaluated in rats. In brain, both [4‐ O ‐ methyl ‐ 11 C]KW‐6002 and [4‐ O ‐ methyl ‐ 11 C]KF18446 showed the highest uptake in striata and lowest in frontal cortex. For [4‐ O ‐ methyl ‐ 11 C]KW‐6002 maximal striata: frontal cortex ratio was 1.7 from 60 to 120 min. For [4‐ O ‐ methyl ‐ 11 C]KF18446 maximal striata: frontal cortex ratio was 2.4 from 30 to 90 min. The amount of unchanged [4‐ O ‐ methyl ‐ 11 C]KW‐6002 was > 98 % in striata and cerebellum at 75 min post‐injection.