JNJ-42153605

Information

JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.

Targets

mGlu2 receptor 17 nM(EC50)

In vitro

JNJ-42153605 is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM (>50-fold vs mGluR2) and also shows no or negligible affinity or activity at any of the targets in the CEREP panel of receptors (>100-fold selectivity for mGlu2 receptor).

In vivo

In mice, JNJ-42153605 dose-dependently and significantly attenuates the increase in locomotor activity induced by phencyclidine (PCP, 5 mg/kg sc) with an ED50 of 5.4 mg/kg sc. 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. Volume of distribution is slightly higher than total body water, indicating distribution outside the plasma. Bioavailability is low to moderate across the species (35% in rat and 18−33% in dog).