ADX71743
| 中文名称 | ADX71743 |
|---|---|
| 中文同义词 | 化合物 T26570;化合物 ADX71743 |
| 英文名称 | ADX71743 |
| 英文同义词 | ADX71743;ADX71743 >=98% (HPLC);ADX-71743,ADX71743;4(5H)-Benzoxazolone, 6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydro-, (+)- |
| CAS号 | 1431641-29-0 |
| 分子式 | C17H19NO2 |
| 分子量 | 269.34 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1431641-29-0.mol |
| 结构式 |  |
ADX71743 性质
| 沸点 | 405.1±24.0 °C(Predicted) |
|---|---|
| 密度 | 1.130±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | -0.05±0.40(Predicted) |
|
mGlu7
|
ADX71743 has an IC
50
of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction.
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal.
ADX71743 can against an EC
80
of glutamate (IC
50
of 22 nM) as well as against an EC
80
of L-AP4 (IC
50
of 125 nM).
ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T
1/2
of 0.68, 0.40 hours, a C
max
of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
| Animal Model: | Adult male C57Bl6/J mice (24-30 g) |
| Dosage: | 50, 100, 150 mg/kg |
| Administration: | SC |
| Result: | Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg). |
| Animal Model: | Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g) |
| Dosage: | 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis) |
| Administration: | SC |
| Result: |
Had a T
1/2
of 0.68, 0.40 hours, a C
max
of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T 1/2 of 1.5 hours, a C max of 16800 ng/ml of 100 mg/kg in rat. |