121917-57-5
中文名稱
(-)-MK801MALEATE
英文名稱
(-)-MK-801 MALEATE
CAS
121917-57-5
分子式
C20H19NO4
分子量
337.37
MOL 文件
121917-57-5.mol
更新日期
2024/08/11 18:43:14
121917-57-5 結(jié)構(gòu)式
基本信息
中文別名
順丁烯二酸鹽 (-)-MK(-)-MK 801馬來酸
(-)-MK801 馬來酸鹽
英文別名
CS-2146(-)-MK 801
(-)-MK801MALEATE
(-)MK-801 maleate
(-)-MK-801 MALEATE
MK 801
MK801
C13737
(-)-DIZOCILPINE MALEATE
(-)-MK-801 MALEATE USP/EP/BP
(-)-Dizocilpine Maleate [(-)-MK 801 maleate
5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5R,10S)
所屬類別
生物化工：GluR 拮抗劑物理化學性質(zhì)
儲存條件-20°C儲存
溶解度DMSO: >20 mg/mL
溶解度二甲基亞砜：>20 mg/mL
形態(tài)solid
顏色white
水溶解性Soluble in water (25mM, gentle warming)
常見問題列表
生物活性
(-)-MK 801 Maleate作用于大鼠腦組織膜，是一種有效的，選擇性的，非競爭性NMDA受體拮抗劑，Kd為37.2 nM。體外研究
[3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for [3H]MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype. MK-801 inhibits N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively. MK-801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 is also effective at blocking NMDA-activated single-channel activity in outside-out patches. MK-801 (< 500 μM) prevents LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells.體內(nèi)研究
Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduced the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice. MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement.生物活性
(-)-MK-801 (Dizocilpine, C13737) 是一種有效的N-methyl-D-aspartate(NMDA)受體拮抗劑，Ki為30.5 nM。靶點
| Target | Value |
| NMDA receptor | 30.5 nM(Ki) |
體外研究
體外神經(jīng)生理學研究使用大鼠皮質(zhì)切片制劑，證明了dizocilpine對N-Me-D-Asp去極化響應具有有效的，選擇性的，非競爭性的拮抗作用，但是對紅藻氨酸或使君子氨酸無此作用。Phencyclidine，ketamine，SKF 10047，和dizocilpine的對映異構(gòu)體，作為N-Me-D-Asp拮抗劑的效能與它們作為[3H] dizocilpine結(jié)合抑制劑的效能密切相關(guān)。這表明，dizocilpine結(jié)合位點與N-Me-D-Asp受體相關(guān)，并解釋了dizocilpine作為抗痙攣劑的作用機制。
體內(nèi)研究
在脊髓缺血性損傷(ISCI)后，所有對照組大鼠患有嚴重的永久性神經(jīng)功能缺損，而dizocilpine治療的大鼠具有統(tǒng)計學上(P < .05)更好的神經(jīng)功能，并且恢復良好。組織病理學表明對照組大鼠的腰灰質(zhì)出現(xiàn)嚴重的神經(jīng)元壞死，而dizocilpine處理的大鼠僅表現(xiàn)出輕度損傷。這些結(jié)果表明，ISCI 之前，dizocilpine單劑量給藥提供顯著的神經(jīng)保護作用。