REVIEW A 796260 is a synthetic selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models. A 796260 demonstrated analgesic activity across multiple preclinical pain models. AM1241 is an indole derivative that exhibits high affinity and selectivity for the CB2 binding site and broad spectrum analgesic activity in rodent models, but is not an antagonist of CB2 in vitro functional assays. Additionally, its analgesic effects are opioid receptor-dependent.
REFERENCES
[1]
Frost, Jennifer M.; Journal of Medicinal Chemistry 2010, V53(1), P295-315
[2]
B B Yao, G C Hsieh, J M Frost, Y Fan, T R Garrison, A V Daza, G K Grayson, C Z Zhu, M Pai, P Chandran, A K Salyers, E J Wensink, P Honore, J P Sullivan, M J Dart, M D Meyer, In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models, British Journal of Pharmacology (2008), 153(2), 390-401.
[3]
Jennifer M. Frost, Michael J. Dart, Karin R. Tietje, Tiffany R. Garrison, George K. Grayson, Anthony V. Daza, Odile F. El-Kouhen, Betty B. Yao, Gin C. Hsieh, Madhavi Pai, Chang Z. Zhu, Prasant Chandran and Michael D. Meyer, Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity. J. Med. Chem., 2010, 53 (1), pp 295-315.
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