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Bioorg Med Chem Lett. 2009 Mar 15;19(6):1691-3. doi: 10.1016/j.bmcl.2009.01.100. Epub 2009 Feb 4.

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

Author information

1
Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee-Memphis, TN 38163, USA.

Abstract

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.

PMID:
19230659
DOI:
10.1016/j.bmcl.2009.01.100
[Indexed for MEDLINE]

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