Discovery of PF-04457845: a highly potent, orally bioavailable, and selective urea FAAH inhibitor

…, DT Dudley, N Sadagopan, SN Bhattachar…

文献索引：Johnson, Douglas S.; Stiff, Cory; Lazerwith, Scott E.; Kesten, Suzanne R.; Fay, Lorraine K.; Morris, Mark; Beidler, David; Liimatta, Marya B.; Smith, Sarah E.; Dudley, David T.; Sadagopan, Nalini; Bhattachar, Shobha N.; Kesten, Stephen J.; Nomanbhoy, Tyzoon K.; Cravatt, Benjamin F.; Ahn, Kay ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 2 p. 91 - 96

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被引用次数: 89

摘要

Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without showing the undesirable side effects observed with direct cannabinoid receptor agonists, indicating that FAAH may represent an attractive ...