Chemistry:GW-405,833
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Short description: Chemical compound
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| Formula | C23H24Cl2N2O3 |
| Molar mass | 447.36 g·mol−1 |
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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]
References
- ↑ "The search for selective ligands for the CB2 receptor". Current Pharmaceutical Design 6 (13): 1323–37. September 2000. doi:10.2174/1381612003399347. PMID 10903395.
- ↑ "Recent advances in the development of selective ligands for the cannabinoid CB(2) receptor". Current Topics in Medicinal Chemistry 8 (3): 187–204. 2008. doi:10.2174/156802608783498014. PMID 18289088.
- ↑ "CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain". Pain 96 (3): 253–60. April 2002. doi:10.1016/s0304-3959(01)00454-7. PMID 11972997.
- ↑ "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. doi:10.1016/j.neuropharm.2004.12.008. PMID 15814101.
- ↑ "CB2 receptor-mediated antihyperalgesia: possible direct involvement of neural mechanisms". The European Journal of Neuroscience 23 (6): 1530–8. March 2006. doi:10.1111/j.1460-9568.2006.04684.x. PMID 16553616.
- ↑ "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. doi:10.1007/s00210-008-0386-4. PMID 19152053.
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