Frau, Simona and Dall'Angelo, Sergio and Baillie, Gemma L. and Ross, Ruth A. and Pira, Marilena and Tseng, Chih-Chung and Lazzari, Paolo and Zanda, Matteo (2013) Pyrazole-type cannabinoid ligands conjugated with fluoro-deoxy-carbohydrates as potential PET-imaging agents: synthesis and CB1/CB2 receptor affinity evaluation. Journal of fluorine chemistry, Vol. 152 , p. 166-172. ISSN 0022-1139. eISSN 1873-3328. Article.
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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.
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