459836-30-7
中文名称
[[[(1S)-1-(4-BROMOPHENYL)ETHYL]AMINO](1,2,3,4-TETRAHYDRO-2,3-DIOXO-5-QUINOXALINYL)METHYL] PHOSPHONIC ACID TETRASODIUM HYDRATE
英文名称
PEAQX TETRASODIUM HYDRATE
CAS
459836-30-7
分子式
C34H32Br2N6Na4O11P2
分子量
1014.37
MOL 文件
459836-30-7.mol
结构式
基本信息
中文别名
化合物 PEAQX TETRASODIUM HYDRATE
英文别名
PEAQX TETRASODIUM HYDRATE
NVP-AAM077 tetrasodiuM hydrate
NVP-AAM 077 tetrasodiuM hydrate
[[[(1S)-1-(4-BROMOPHENYL)ETHYL]AMINO](1,2,3,4-TETRAHYDRO-2,3-DIOXO-5-QUINOXALINYL)METHYL] PHOSPHONIC ACID TETRASODIUM HYDRATE
NVP-AAM077 tetrasodiuM hydrate
NVP-AAM 077 tetrasodiuM hydrate
[[[(1S)-1-(4-BROMOPHENYL)ETHYL]AMINO](1,2,3,4-TETRAHYDRO-2,3-DIOXO-5-QUINOXALINYL)METHYL] PHOSPHONIC ACID TETRASODIUM HYDRATE
物理化学性质
| 密度 | 1.639±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 酸度系数(pKa) | 1.19±0.10(Predicted) |
| 形态 | Solid |
| 颜色 | Light yellow to khaki |
常见问题列表
生物活性
PEAQX (NVP-AAM077) tetrasodium hydrate 是有效的、选择性的、口服有效的 NMDA 拮抗剂，其对 hNMDAR 1A 和 hNMDAR 2A 的 IC50 值分别为 270 nM 和 29600 nM。
体外研究
PEAQX (3 µM) produces similar caspase-3 activation, while NVP-AAM007 is approximately three-fold more potent.
体内研究
PEAQX (10-40 mg/kg) dose-dependently increased cortical caspase-3 activity following sub-chronic administration.
PEAQX (10 and 20 mg/kg) shows enhanced locomotor activity in response to PCP challenge (4 mg/kg on PN28-35) compared to saline pretreatment (F
3, 73
=4.99).
PEAQX (10 mg/kg, ip) antagonizes the effects of PRE084 on CaMKIV-TORC1-CREB and BDNF, even for learning and memory impairment.
| Animal Model: | Timed, day 14 pregnant female Sprague-Dawley rats. |
| Dosage: | 10, 20 or 40 mg/kg. |
| Administration: | S.C. |
| Result: | Showed a sensitized locomotor response to PCP challenge on PN28-35. |
| Animal Model: | Timed, day 14 pregnant female Sprague-Dawley rats. |
| Dosage: | 4 mg/kg. |
| Administration: | I.P. |
| Result: | Did not significantly increase locomotor activity in rats treated sub-chronically with PEAQX on PN7, 9 and 11. |
| Animal Model: | 11-week old C57BL/6 mice. |
| Dosage: | 10 mg/kg. |
| Administration: | IP. |
| Result: | Reversed the effect of PRE084 (F 3,78 = 10.446, p<0.01). |