| Identification | Back Directory | [Name]
JNJ-40411813 | [CAS]
1127498-03-6 | [Synonyms]
CS-1035
ADX 71149
JNJ-40411813
JNJ 40411813;JNJ-40411813
1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2(1H)-one
1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-2(1H)-Pyridinone
2(1H)-Pyridinone, 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)- | [Molecular Formula]
C20H25ClN2O | [MOL File]
1127498-03-6.mol | [Molecular Weight]
344.88 |
| Chemical Properties | Back Directory | [Boiling point ]
463.5±45.0 °C(Predicted) | [density ]
1.18±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:25.0(Max Conc. mg/mL);72.49(Max Conc. mM) | [form ]
Solid | [pka]
1.06±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
ADX 71149 is drug candidate; used in preparation of Bipyridinones as positive allosteric modulators of mGluR2 for treating neurological and psychiatric disorders.Also, use as a treatment for ADHD. | [in vivo]
JNJ-40411813 (ADX-71149) (5-20 mg/kg; p.o.; 6 times in 24 h) clearly potentiated glutamate response in brain regions, more specifically in the cortical regions, striatum, and the hippocampus, coaddition of Glutamate (HY-N0455B)[2].
Pharmacokinetic Analysis in SD rat[2]
| Route | Dose (mg/kg) | AUCINF_obs (ng·h/mL) | t1/2 (h) | Tmax (h) | Cmax (ng/mL) | Clobs (L·h/kg) | Vss_obs (L/kg) | | i.v. | 2.5 | 1833±90 | / | / | / | 1.4±0.1 | 2.31.4±0.10.2 | | p.o. | 10 | 2250±417 | 2.31±0.5 | 7 | 938 | / | / |
| Animal Model: | Male Wistar Rats (150 mg)[2] | | Dosage: | 5 mg/kg, 20 mg/kg | | Administration: | Oral Gavage (p.o.) | | Result: | Showed increasing in basal binding with an EC50 of 48 μM and a Combined with 10 μM glutamate, [35S]GTPγS binding with an EC50 of 7.3 μM and a maximal effect of 380%. |
| [IC 50]
mGlu2 Receptor: 147 nM (EC50) |
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