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JWH-051 is an analgesic drug which is a cannabinoid agonist. Its chemical structure is closely related to that of the potent cannabinoid agonist HU-210, with the only difference being the removal of the hydroxyl group at position 1 of the aromatic ring. It was discovered and named after Dr. John W. Huffman.
JWH-051 retains high affinity for the CB1 receptor, but is a much stronger agonist for CB2, with a Ki value of 14nM at CB2 vs 19nM at CB1. It was one of the first CB2-selective ligands developed, although its selectivity for CB2 is modest compared to newer compounds such as HU-308.
- Huffman, JW; Yu, S; Showalter, V; Abood, ME; Wiley, JL; Compton, DR; Martin, BR; Bramblett, RD; Reggio, PH (1996). "Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor". Journal of Medical Chemistry 39 (20): 3875–7. doi:10.1021/jm960394y. PMID 8831752.
- Huffman, JW (2000). "The search for selective ligands for the CB2 receptor". Current pharmaceutical design 6 (13): 1323–37. doi:10.2174/1381612003399347. PMID 10903395.
- Klein, TW; Newton, C; Friedman, H (1998). "Cannabinoid receptors and the cytokine network". Advances in experimental medicine and biology. Advances in Experimental Medicine and Biology 437: 215–22. doi:10.1007/978-1-4615-5347-2_24. ISBN 978-0-306-45838-5. PMID 9666274.
- Griffin, G; Fernando, SR; Ross, RA; McKay, NG; Ashford, ML; Shire, D; Huffman, JW; Yu, S et al. (1997). "Evidence for the presence of CB2-like cannabinoid receptors on peripheral nerve terminals". European Journal of Pharmacology 339 (1): 53–61. doi:10.1016/S0014-2999(97)01336-8. PMID 9450616.
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