L-759,656

L-759,656 is an analgesic drug which is a cannabinoid agonist. It is a highly selective agonist for the CB₂ receptor, with selectivity of 414x for CB₂ over CB₁,^[1] although it is still not as selective as newer agents such as HU-308.

It produces some similar effects to other cannabinoid agonists such as analgesia, but with little or no sedative or psychoactive effects due to its weak CB₁ activity, and a relatively strong antiinflammatory effect due to its strong activity at CB₂.^[2]^[3]

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References

↑ Ross RA, Brockie HC, Stevenson LA, Murphy VL, Templeton F, Makriyannis A, Pertwee RG. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630. British Journal of Pharmacology. 1999 Feb;126(3):665-72. PMID 10188977
↑ Huffman JW. The search for selective ligands for the CB2 receptor. Current Pharmaceutical Design. 2000 Sep;6(13):1323-37. PMID 10903395
↑ Huffman JW. CB2 receptor ligands. Mini Reviews in Medicinal Chemistry. 2005 Jul;5(7):641-9. PMID 16026310

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[1] Ross RA, Brockie HC, Stevenson LA, Murphy VL, Templeton F, Makriyannis A, Pertwee RG. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630. British Journal of Pharmacology. 1999 Feb;126(3):665-72. PMID 10188977

[2] Huffman JW. The search for selective ligands for the CB2 receptor. Current Pharmaceutical Design. 2000 Sep;6(13):1323-37. PMID 10903395

[3] Huffman JW. CB2 receptor ligands. Mini Reviews in Medicinal Chemistry. 2005 Jul;5(7):641-9. PMID 16026310

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