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459836-30-7

中文名稱 [[[(1S)-1-(4-BROMOPHENYL)ETHYL]AMINO](1,2,3,4-TETRAHYDRO-2,3-DIOXO-5-QUINOXALINYL)METHYL] PHOSPHONIC ACID TETRASODIUM HYDRATE
英文名稱 PEAQX TETRASODIUM HYDRATE
CAS 459836-30-7
分子式 C34H32Br2N6Na4O11P2
分子量 1014.37
MOL 文件 459836-30-7.mol
459836-30-7 結(jié)構(gòu)式 459836-30-7 結(jié)構(gòu)式

基本信息

中文別名
化合物 PEAQX TETRASODIUM HYDRATE
英文別名
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

物理化學(xué)性質(zhì)

密度1.639±0.06 g/cm3(Predicted)
儲存條件-20°C
酸度系數(shù)(pKa)1.19±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to khaki

常見問題列表

生物活性
PEAQX (NVP-AAM077) tetrasodium hydrate 是有效的、選擇性的、口服有效的 NMDA 拮抗劑,其對 hNMDAR 1A 和 hNMDAR 2A 的 IC50 值分別為 270 nM 和 29600 nM。
體外研究

PEAQX (3 μM) produces similar caspase-3 activation, while NVP-AAM007 is approximately three-fold more potent.

體內(nèi)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).
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