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Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands. | LitMetric

Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands.

Bioorg Med Chem Lett

Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee-Memphis, TN 38163, USA.

Published: March 2009

A novel series of cannabinoid ligands with a structurally unique tri-aryl core has been designed, synthesized and assayed. Receptor binding assays show that these compounds possess CB2 receptor sub-type selectivity with binding affinities ranging from 1.07 (+/-0.05) for 7 to 4.77 (+/-0.57) nM for 6. The selectivity of the compounds was enhanced 9-600-fold for the CB2 receptor over the CB1 receptor. The results of our present study identify a novel, highly selective cannabinoid scaffold with a non-classical core.

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Source
http://dx.doi.org/10.1016/j.bmcl.2009.01.100DOI Listing

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