Pf 3845 Case Study

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PF-3845

Description:
Target: fatty acid amide hydrolase (FAAH)
IC50: NA
Ki: 230 nM

PF-3845 is a selective, potent, and irreversible FAAH inhibitor with Ki value of 230 nM [1]. Anandamide (AEA) is the primary FAAH substrate decreasing tactile allodynia-induced by LPS. The FAAH/AEA signaling pathways regulate a discrete subset of the behavioral processes affected by direct CB1 agonists. Inhibition of the catabolic enzyme fatty acid amide hydrolase (FAAH) elevates anandamide (AEA) levels and displays antinociceptive, analgesia, anti-inflammation, anxiolysis, and antidepression effects, without disruptions in cognition, motility, or body temperature [2].

In vitro: PF-3845 showed negligible activity against FAAH variant (IC50 > 10 μM) [1].

In

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