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Preclinical Characterization of the FAAH Inhibitor JNJ-42165279
The pre-clinical characterization
of the aryl piperazinyl urea
inhibitor of fatty acid amide hydrolase (FAAH) <b>JNJ-42165279</b> is described. <b>JNJ-42165279</b> covalently inactivates the
FAAH enzyme, but is highly selective with regard to other enzymes,
ion channels, transporters, and receptors. <b>JNJ-42165279</b> 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),
oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound
was also efficacious in the spinal nerve ligation (SNL) model of neuropathic
pain. The combination of good physical, ADME, and PD properties of <b>JNJ-42165279</b> supported it entering the clinical portfolio