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Br J Pharmacol. 2008 Jan;153(2):335-46. Epub 2007 Nov 5.

Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands.

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  • 1Department of Pharmaceutical Chemistry, University of Kuopio, Kuopio, Finland.


Recent developments indicate that CB2 receptor ligands have the potential to become therapeutically important. To explore this potential, it is necessary to develop compounds with high affinity for the CB2 receptor and little affinity for the CB1 receptor. This review will discuss structure-activity relations at both receptors for classical cannabinoids and cannabimimetic indoles. Examples of CB2 selective ligands from both classes of compounds are presented and the structural features leading to selectivity are described. Two approaches, receptor mutations and molecular modelling, have been employed to investigate the interaction of ligands with both cannabinoid receptors. These results obtained from these techniques are discussed.

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