1. ¹Department of Pharmaceutical Chemistry, University of Kuopio, Kuopio, Finland
2. ²Howard L Hunter Laboratory, Clemson University, Clemson, SC, USA

Correspondence: Professor A Poso, Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, Kuopio FI-70211, Finland. E-mail: antti.poso@uku.fi

Received 25 June 2007; Revised 12 September 2007; Accepted 15 October 2007; Published online 5 November 2007.

Abstract

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.