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Title of article :
Pyrazole-type cannabinoid ligands conjugated with fluoro-deoxy-carbohydrates as potential PET-imaging agents: Synthesis and CB1/CB2 receptor affinity evaluation
Author/Authors :
Frau، نويسنده , , Simona and Dall’Angelo، نويسنده , , Sergio and Baillie، نويسنده , , Gemma L. and Ross، نويسنده , , Ruth A. and Pira، نويسنده , , Marilena and Tseng، نويسنده , , Chih-Chung and Lazzari، نويسنده , , Paolo and Zanda، نويسنده , , Matteo، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2013
Pages :
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Abstract :
A novel class of cannabinoid ligands was synthesized in good overall yields by means of oxime-bio-conjugation between hydroxylamine-functionalized Rimonabant-type pyrazoles and fluoro-deoxy-carbohydrates (d-2-fluoro-deoxy-glucose, FDG, and d-5-fluoro-5-deoxy-ribose, FDR). FDR proved to be superior to FDG for bio-conjugation, as it occurred in milder conditions and at faster rate (rt, 20 min vs. 100 °C, 30 min). All of the title compounds showed relatively modest affinity for the CB1 receptor (high nanomolar range) and selectivities vs. the CB2.
Keywords :
Cannabinoids , PET imaging , Fluoro-carbohydrates
Journal title :
Journal of Fluorine Chemistry
Link To Document :