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Remarks
JNJ-42165279 is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibited excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoylethanolamide (OEA), and palmitoyl ethanolamide (PEA). JNJ-42165279 was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 is currently under clinical trials.