3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine
3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine Basic information
- Product Name:
- 3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine
- Synonyms:
-
- JNJ-42153605;JNJ42153605
- CS-2446
- 3-(Cyclopropylmethyl)-7-(4-phenyl-1-piperidinyl)-8-(trifluorometh yl)[1,2,4]triazolo[4,3-a]pyridine
- 3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine
- JNJ42153605 (on going)
- 1,2,4-Triazolo[4,3-a]pyridine, 3-(cyclopropylmethyl)-7-(4-phenyl-1-piperidinyl)-8-(trifluoromethyl)-
- Inhibitor,JNJ42153605,Metabotropic glutamate receptors,JNJ-42153605,inhibit,JNJ 42153605,mGluR
- JNJ-42153605 ，S6618
- CAS:
- 1254977-87-1
- MF:
- C22H23F3N4
- MW:
- 400.44
- Mol File:
- 1254977-87-1.mol
3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine Chemical Properties
- Density
- 1.38±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF:30.0(Max Conc. mg/mL);74.92(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.62(Max Conc. mM)
DMSO:10.34(Max Conc. mg/mL);25.81(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);24.97(Max Conc. mM) - form
- A crystalline solid
- pka
- 3.07±0.30(Predicted)
- color
- White to off-white
3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine Usage And Synthesis
Description
JNJ-42153605 is a positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2; EC50 = 17 nM in CHO cells expressing the human receptor). In vivo, JNJ-42153605 (3 mg/kg) inhibits mGluR2-mediated rapid eye movement (REM) sleep in rats. It also reverses phencyclidine-induced hyperlocomotion in mice (ED50 = 5.4 mg/kg).
Uses
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
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[1].
IC 50
mGluR2: 17 nM (EC50)
References
[1] Cid JM, et al. Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor. J Med Chem. 2012 Oct 25;55(20):8770-89. DOI:10.1021/jm3010724
3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridineSupplier
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