ChemicalBook English  Japanese  Germany

(-)-MK801MALEATE

生物活性 体外研究 体内研究

CAS号:121917-57-5
英文名称:(-)-MK-801 MALEATE
英文同义词:(-)-MK-801 MALEATE;(5S,10R)-(-)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE MALEATE;5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5R,10S)-, (2Z)-2-butenedioate (1:1)
中文名称:(-)-MK801MALEATE
中文同义词:(-)-MK801MALEATE
CBNumber:CB5407484
分子式:C20H19NO4
分子量:337.37
MOL File:121917-57-5.mol
(-)-MK801MALEATE化学性质
溶解度 : DMSO: >20 mg/mL
form : solid
color : white
安全信息
安全说明 : 22-24/25
WGK Germany : 3
RTECS号: HP1093575

(-)-MK801MALEATE 性质、用途与生产工艺

生物活性
(-)-MK 801 Maleate作用于大鼠脑组织膜，是一种有效的，选择性的，非竞争性NMDA受体拮抗剂，Kd为37.2 nM。
体外研究
[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.
体内研究
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.
(-)-MK801MALEATE 上下游产品信息
上游原料
下游产品
(-)-MK801MALEATE 生产厂家      全球有 19家供应商        (-)-MK801MALEATE国内生产厂家
供应商联系电话传真电子邮件国家产品数优势度
上海波以尔化工有限公司 Mr Qiu 86-21-50182298(Domestic Market)Miss Xu 86-21-50180596(Abroad Market)86-21-57758967sales@boylechem.com中国 5604 55
武汉易泰科技有限公司上海分公司 86-21-50328103 * 801、802、803、804 Mobile:1893055203786-21-5032810967055399@qq.com中国 15983 69
上海皓元化学科技有限公司 86-21-5899859086-21-53700326, 86-21-58998590sales@chemexpress.cn中国 10011 61
上海阿拉丁生化科技股份有限公司 021-20337333/400-620-6333021-50323701sale@aladdin-e.com中国 24330 65
MedChemexpress LLC 609-228-6898609-228-5909sales@medchemexpress.cn美国 4935 58
Clearsynth Labs Limited +91-22-26355700 +91-22-26355701info@clearsynth.com印度 9914 58
湖北巨胜科技有限公司 North:027-59599241,18871490274,QQ:1400878000 South:027-59531287,15727001360,QQ:1400878866℡ 027-83861211469501031@qq.com中国 10512 58
上海惯承化工科技有限公司 Please Email：sales@letopharm.com +86-21-5106 2861sales@letopharm.com中国 2641 58
上海东苍生物科技有限公司 +86-21-58447131+86-21-616424701724405207@qq.com中国 466 55
BOC Sciences 1-631-504-60931-631-614-7828sales@bocsci.com美国 6331 65
广州和为化工有限公司 +86-20-38056109 / 3892 1903+86-20-6261 9665sales@hwhg.com.cn中国 18473 55
 
121917-57-5, (-)-MK801MALEATE 相关搜索:
(S)-(-)-N-苄基-alpha-甲基苄胺 1-苯基-1,2,3,4-四氢异喹啉 (R)-(+)-N-苄基-1-苯乙胺
神经信号 BioChemical Cell Signaling and Neuroscience Cell Biology Ligand-Gated Ion Channels Ionotropic Glutamate Receptor Modulators Ion Channels (-)-MK801MALEATE 121917-57-5 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5R,10S)-, (2Z)-2-butenedioate (1:1) (5S,10R)-(-)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE MALEATE (-)-MK-801 MALEATE
Copyright 2016 © ChemicalBook. All rights reserved