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In vitro: JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux.
In vivo: 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 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative 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.
| Cell Experiment | |
|---|---|
| Cell lines | Chinese Hamster Ovary (CHO) cells |
| Preparation method | Final assay mixtures contained 7 (human mGluR2) or 10 (rat mGluR2) μg of membrane protein were pre-incubated with JNJ-42153605 alone (determination of agonist effects) or together with an EC20 concentration (4 μM) of glutamate (determination of PAM effects) for 30 min at 30°C. [35S]GTPγS was added at a concentration of 0.1 nM and Filter-bound radioactivity according to an earlier protocol. |
| Concentrations | 30 mM |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | Sprague Dawley rats |
| Formulation | |
| Dosages | 3, 10 and 30 mg/kg |
| Administration | Oral |
| Molecular Weight | 400.44 |
| Formula | C22H23F3N4 |
| CAS Number | 1254977-87-1 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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