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Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands
Author(s) -
Poso A,
Huffman J W
Publication year - 2008
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0707567
Subject(s) - cannabinoid receptor type 2 , cannabinoid receptor , cannabinoid , receptor , chemistry , computational biology , pharmacology , biochemistry , biology , agonist
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. British Journal of Pharmacology (2008) 153 , 335–346; doi: 10.1038/sj.bjp.0707567 ; published online 5 November 2007