JTP-4819 (1 and 3 mg/kg 1 hr before acquisition or at 3 and 10 mg/kg 1 hr before; p.o.) significantly prolonged the retention time in the one-trial passive avoidance test in rats with Scopolamine (HY-N2096)-induced amnesia[1].
JTP-4819 (1 mg/kg and 3 mg/kg; p.o.; single dose) causes a significant increase in ACh release in the frontal cortex and hippocampus of young rats, as well as in both brain regions of aged rats at higher dose[1].
JTP-4819 combinded with substance P, arginine-vasopressin or thyrotropin-releasing hormone, improves the retention time of rats with scopolamine-induced amnesia[1].
Brain pharmacokinetics in rats[2]
| AUC0-300 min (μg·min) | Cmax (μM) | Brain/blood ratio | t1/2β (min) |
| Unblound concentrations | | | | |
| Blood | 1947 | 16.7 | | 84 |
| Cortex | 206 | 1.78 | 0.13 | 77 |
| Hippocampus | 128 | 1.05 | 0.09 | 105 |
| Striatum | 178 | 1.26 | 0.10 | 128 |
| Total tissue concentrations | | | | |
| Plasma | 4230 | 78.6 | | 130 |
| Brain | 145 | 1.47 | 0.034 | 120 |