JNJ-42153605

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-42153605 是一种 mGlu2 受体正变构调节剂 (EC50: 17 nM)。

JNJ-42153605 is a potent and selective mGlu2 receptor PAM with an acceptable pharmacokinetic profile in rodent and nonrodent species. JNJ-42153605 showed centrally mediated in vivo effectivity in models sensitive to mGlu2 receptor modulation such as sleep?wake electroencephalogram (sw-EEG) in rats,34 showing suppressed REM sleep during the first 4 h after oral administration of a 3 mg/kg dose.

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.

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.

JNJ-42153605 | JNJ 42153605 | JNJ42153605

Chromatin/Epigenetic

COX

mGluR2 PAM

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1254977-87-1

400.45

C22H23F3N4

>98% (HPLC)

In Vitro:?DMSO : 16.67 mg/mL (41.63 mM)

c12c(c(ccn1c(nn2)CC1CC1)N1CCC(CC1)c1ccccc1)C(F)(F)F

3-(Cyclopropylmethyl)-7-(4-phenyl-1-piperidinyl)-8-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyridine

(-20℃)

With Ice Pack

≥ 2 years