GW-405,833 explained

GW-405,833 (L-768,242) is a drug that acts as a potent and selective partial agonist for the cannabinoid receptor subtype CB2, with an EC50 of 0.65 nM and selectivity of around 1200x for CB2 over CB1 receptors.[1] [2] Animal studies have shown it to possess antiinflammatory and anti-hyperalgesic effects at low doses, followed by ataxia and analgesic effects when the dose is increased.[3] [4] Selective CB2 agonist drugs such as GW-405,833 are hoped to be particularly useful in the treatment of allodynia and neuropathic pain for which current treatment options are often inadequate.[5] [6]

Notes and References

  1. Huffman JW . The search for selective ligands for the CB2 receptor . Current Pharmaceutical Design . 6 . 13 . 1323–37 . September 2000 . 10903395 . 10.2174/1381612003399347 .
  2. Marriott KS, Huffman JW . Recent advances in the development of selective ligands for the cannabinoid CB(2) receptor . Current Topics in Medicinal Chemistry . 2008 . 8 . 3 . 187–204 . 18289088 . 10.2174/156802608783498014 .
  3. Clayton N, Marshall FH, Bountra C, O'Shaughnessy CT . CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain . Pain . 96 . 3 . 253–60 . April 2002 . 11972997 . 10.1016/s0304-3959(01)00454-7 . 24816928 .
  4. Valenzano KJ, Tafesse L, Lee G, Harrison JE, Boulet JM, Gottshall SL, Mark L, Pearson MS, Miller W, Shan S, Rabadi L, Rotshteyn Y, Chaffer SM, Turchin PI, Elsemore DA, Toth M, Koetzner L, Whiteside GT . 6 . Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy . Neuropharmacology . 48 . 5 . 658–72 . April 2005 . 15814101 . 10.1016/j.neuropharm.2004.12.008 . 10121434 .
  5. Beltramo M, Bernardini N, Bertorelli R, Campanella M, Nicolussi E, Fredduzzi S, Reggiani A . CB2 receptor-mediated antihyperalgesia: possible direct involvement of neural mechanisms . The European Journal of Neuroscience . 23 . 6 . 1530–8 . March 2006 . 16553616 . 10.1111/j.1460-9568.2006.04684.x . 19266396 .
  6. Leichsenring A, Andriske M, Bäcker I, Stichel CC, Lübbert H . Analgesic and antiinflammatory effects of cannabinoid receptor agonists in a rat model of neuropathic pain . Naunyn-Schmiedeberg's Archives of Pharmacology . 379 . 6 . 627–36 . June 2009 . 19152053 . 10.1007/s00210-008-0386-4 . 25085194 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "GW-405,833".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.