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Preparation and characterization of (R,S)‐[ 76 Br]BrQNB: An analogue of QNB for PET
Author(s) -
Strijckmans V.,
Lee K. S.,
Loc'h C.,
Ottaviani M.,
Zeeberg B. R.,
Mazière B.
Publication year - 1997
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/(sici)1099-1344(199704)39:4<339::aid-jlcr969>3.0.co;2-c
Subject(s) - chemistry , bromine , radiochemistry , biodistribution , electrophilic substitution , oxidizing agent , metabolite , specific activity , peracetic acid , yield (engineering) , nuclear chemistry , medicinal chemistry , in vitro , organic chemistry , biochemistry , hydrogen peroxide , metallurgy , enzyme , materials science
(R,S)‐[ 76 Br]BrQNB was prepared for imaging mAChR by PET. (R,S)QNB was labelled with bromine‐76 by electrophilic substitution of the tributylstannyl precursor using peracetic acid as oxidizing agent. The exchange between bromine‐76 and the leaving group occurred in 20 min at room temperature. A chemically and radiochemically pure product was obtained with a final radiolabelling yield of 30%. Preliminary evaluation of pharmacological properties was performed in rats. In brain, biodistribution and autoradiography studies showed that the preferential localization of (R,S)‐[ 76 Br]BrQNB was m‐AChR rich structures. 6 h p.i. the radioactivity uptake in the posterior cortex was 1% ID/g and the striatum to cerebellum radioactivity ratio was 13.5. Metabolite study revealed that the radiotracer remains unchanged in brain for at least 3 h. © 1997 John Wiley & Sons, Ltd.