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%. |
