JNJ-1661010 681136-29-8

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Molecular Weight:

365.45 JNJ-1661010 is a potent and Selective FAAH Inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.






Biological Activity


FAAH preincubated with JNJ-1661010 suggests a slow reversibility of the
interaction between the JNJ-1661010 and the active site, which is
accelerated at higher temperatures. JNJ-1661010 is a
covalent, mechanism-based substrate inhibitor as examined by LC-ESI-MS.
JNJ-1661010 docks with the phenylthiadiazole in the hydrophobic tunnel
and the phenylurea in the hydrophilic pocket of FAAH.


JNJ-1661010 (20 mg/kg i.p.) inhibits FAAH by at least 85% for up to 4 h
after dosing, resulting accumulation of lipid ethanolamides in rat
brain. JNJ-1661010 dose-dependently reverses the tactile allodynia with a
maximum efficacy of approximately 90% at 30 min postdose in both Mild
Thermal Injury (MTI) mice and rat model. JNJ-1661010 (20 mg/kg) reverses
tactile allodynia by 60.8% at 30 min in rat spinal nerve ligation
injury model.


JNJ-1661010 (50 mg/kg i.p.) shows a significant
attenuation of the hyperalgesia at 30 min postdose in rat carrageenan
model of inflammatory pain. Rats dosed with JNJ-1661010
(20 mg/kg i.p.) has a plasma Cmax of 26.9 μM at the Tmax of 0.75 h and a
Cmax in the brain of 6.04 μM at the Tmax of 2 h. JNJ-1661010 (20 mg/kg
i.p.) inhibits brain FAAH and elevates AEA level in brain tissue in rat.

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Product Categories : Metabolism > FAAH Inhibitor