JNJ42153605是一种代谢型谷氨酸2 (mGlu2) 受体的正变构调节剂，EC50值为17 nM。

JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).

JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor. JNJ-42153605 is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 exhibits high permeability with no indication for P-glycoprotein efflux[1].

JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 exhibits reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, suggestive of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog[1].

1254977-87-1

C22H23F3N4

400.449

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years