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Pyrazole-type cannabinoid ligands conjugated with fluoro-deoxy-carbohydrates as potential PET-imaging agents: synthesis and CB1/CB2 receptor affinity evaluation

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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DOI: 10.1016/j.jfluchem.2013.03.006

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.

Item Type:Article
ID Code:9844
Status:Published
Refereed:Yes
Uncontrolled Keywords:Fluoro-carbohydrates, PET imaging, cannabinoids
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier
ISSN:0022-1139
eISSN:1873-3328
Additional Information:Special issue: Valencia Fluorine Days, 2012.
Deposited On:04 Jun 2014 11:31

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