(-)-MK-801 maleate - CAS 77086-22-7
Catalog number: 77086-22-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H19NO4
Molecular Weight:
337.37
COA:
Inquire
Targets:
NMDA Receptor
Description:
(-)-MK-801 maleate is a potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM that acts at the NMDA receptor-operated ion channel as an open channel blocker. It blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. It anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions in test rats. It were used to treat hyperalgesia in the diabetic neuropathic pain (DNP). It is used in various ischemia treatments. It has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants.
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Purity:
>99 %
Appearance:
White Solid
Synonyms:
(+)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-diyldiammonium maleate;Dizocilpine maleate;(5R,10S)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate;Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK-801 hydrogen maleate
Solubility:
DMSO: > 20 mg/mL, H2O: 6 mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
(-)-MK-801 maleate blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. It were used to treat hyperalgesia in the diabetic neuropathic pain (DNP). It is used in various ischemia treatments. It has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
541°C at 760 mmHg
Melting Point:
183-185°C
InChIKey:
QLTXKCWMEZIHBJ-PJGJYSAQSA-N
InChI:
InChI=1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-,16+;/m1./s1
Canonical SMILES:
CC12C3=CC=CC=C3CC(N1)C4=CC=CC=C24.C(=CC(=O)O)C(=O)O
1.NMDA receptors are expressed in human ovarian cancer tissues and human ovarian cancer cell lines.
North WG1, Liu F1, Tian R1, Abbasi H1, Akerman B1. Clin Pharmacol. 2015 Oct 23;7:111-7. doi: 10.2147/CPAA.S90367. eCollection 2015.
We have earlier demonstrated that breast cancer and small-cell lung cancer express functional NMDA receptors that can be targeted to promote cancer cell death. Human ovarian cancer tissues and human ovarian cancer cell lines (SKOV3, A2008, and A2780) have now been shown to also express NMDA-receptor subunit 1 (GluN1) and subunit 2B (GluN2B). Seventeen ovarian cancers in two arrays were screened by immunohistochemistry using polyclonal antibodies that recognize an extracellular moiety on GluN1 and on GluN2B. These specimens comprised malignant tissue with pathology diagnoses of serous papillary cystadenocarcinoma, endometrioid adenocarcinoma, and clear-cell carcinoma. Additionally, archival tissues defined as ovarian adenocarcinoma from ten patients treated at this institute were also evaluated. All of the cancerous tissues demonstrated positive staining patterns with the NMDA-receptor antibodies, while no staining was found for tumor-adjacent normal tissues or sections of normal ovarian tissue.
2.Development of social behavior in young zebrafish.
Dreosti E1, Lopes G2, Kampff AR2, Wilson SW1. Front Neural Circuits. 2015 Aug 18;9:39. doi: 10.3389/fncir.2015.00039. eCollection 2015.
Adult zebrafish are robustly social animals whereas larva is not. We designed an assay to determine at what stage of development zebrafish begin to interact with and prefer other fish. One week old zebrafish do not show significant social preference whereas most 3 weeks old zebrafish strongly prefer to remain in a compartment where they can view conspecifics. However, for some individuals, the presence of conspecifics drives avoidance instead of attraction. Social preference is dependent on vision and requires viewing fish of a similar age/size. In addition, over the same 1-3 weeks period larval zebrafish increasingly tend to coordinate their movements, a simple form of social interaction. Finally, social preference and coupled interactions are differentially modified by an NMDAR antagonist and acute exposure to ethanol, both of which are known to alter social behavior in adult zebrafish.
3.Rewarding Effects of Optical Stimulation of Ventral Tegmental Area Glutamatergic Neurons.
Wang HL1, Qi J1, Zhang S1, Wang H1, Morales M2. J Neurosci. 2015 Dec 2;35(48):15948-54. doi: 10.1523/JNEUROSCI.3428-15.2015.
Ventral tegmental area (VTA) neurons play roles in reward and aversion. The VTA has three major neuronal phenotypes: dopaminergic, GABAergic, and glutamatergic. VTA glutamatergic neurons--expressing vesicular glutamate transporter-2 (VGluT2)--project to limbic and cortical regions, but also excite neighboring dopaminergic neurons. Here, we test whether local photoactivation of VTA VGluT2 neurons expressing Channelrhodopsin-2 (ChR2) under the VGluT2 promoter causes place preference and supports operant responding for the stimulation. By using a Cre-dependent viral vector, ChR2 (tethered to mCherry) was expressed in VTA glutamatergic neurons of VGluT2::Cre mice. The mCherry distribution was evaluated by immunolabeling. By confocal microscopy, we detected expression of mCherry in VTA cell bodies and local processes. In contrast, VGluT2 expression was restricted to varicosities, some of them coexpressing mCherry. By electron microscopy, we determined that mCherry-VGluT2 varicosities correspond to axon terminals, forming asymmetric synapses on neighboring dopaminergic neurons.
4.Effects of a dragonfly (Anax i.) homeopathic remedy on learning, memory and cell morphology in mice.
Mutlu O1, Ulak G2, Kokturk S3, Komsuoglu Celikyurt I4, Tanyeri P5, Akar F6, Erden F7. Homeopathy. 2016 Feb;105(1):96-101. doi: 10.1016/j.homp.2015.07.004. Epub 2015 Aug 24.
BACKGROUND: Homeopathy is a form of alternative medicine in which uses highly diluted preparations that are believed to cause healthy people to exhibit symptoms similar to those exhibited by patients. The aim of this study was to investigate the effects of dragonfly (Anax imperator, Anax i.) on learning and memory in naive mice using the Morris water maze (MWM) test; moreover, the effects of dragonfly on MK-801-induced cognitive dysfunction were evaluated.
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CAS 77086-22-7 (-)-MK-801 maleate

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