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Merck

M107

(+)-MK-801 hydrogen maleate

NMDA glutamate receptor antagonist, powder

동의어(들):

(5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate, Dizocilpine hydrogen maleate

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C16H15N · C4H4O4
CAS 번호:
Molecular Weight:
337.37
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352209
EC Number:
278-614-5
MDL number:
Form:
powder
Quality level:
기술 서비스
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제품 이름

(+)-MK-801 hydrogen maleate, powder

InChI key

QLTXKCWMEZIHBJ-PJGJYSAQSA-N

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

SMILES string

[H]\C(=C(/[H])C(O)=O)C(O)=O.C[C@]12N[C@H](Cc3ccccc13)c4ccccc24

form

powder

optical activity

[α]25/D +117°, c = 1 in methanol(lit.)

color

white

solubility

DMSO: >20 mg/mL
H2O: 6 mg/mL
0.1 M HCl: soluble
ethanol: soluble

Quality Level

관련 카테고리

Application

(+)-MK-801 hydrogen maleate has been used in following experimental studies:
It is injected to mice to study the effect of systemic administration of CIQ [(3-chlorophenyl) (6, 7-dimethoxy-1-((4-methoxyphenoxy) methyl)-3, 4-dihydroisoquinolin-2(1H)-yl)methanone] on schizophrenia-like behaviours stimulated by MK-801.
It has been used to block the NMDA (N-methyl-D-aspartate) receptor-mediated rtPA (recombinant tissue plasminogen activator)-enhanced excitotoxic pathway.
It is injected in varied doses to study behavioral performance altering effects of MK-801 in zebrafish (Danio rerio).
It is used as a NMDA receptor antagonist to study 3-OH-GA-induced neuronal damage via NMDA receptors.

Biochem/physiol Actions

Experimental study shows that MK-801, influence circling behavior in a direction-specific manner, modify swimming activity and place preference in zebrafish. Acute injection of MK-801, dose dependently, enhances extracellular acetylcholine (ACh) release in the rat parietal cortex. For intracerebral hematomas, MK-801 might act as a potent supplement to reduce delayed edema after recombinant tissue plasminogen activator (rtPA) clot lysis. MK-801 functions as an antidepressant in the social defeat stress model, but it doesn’t have long-lasting effect.
Highly potent and selective non-competitive NMDA glutamate receptor antagonist that acts at the NMDA receptor-operated ion channel as an open channel blocker. Inhibits behavioral sensitization to psychostimulants and ethanol.

General description

(+)-MK-801 hydrogen maleate is a highly potent and selective non-competitive NMDA glutamate receptor antagonist that acts at the NMDA receptor-operated ion channel as an open channel blocker. Neurons are depolarized when MK-801 binds to the Glu (40 Glu) receptor (NMDA receptor- ion channel complex) at two sites. 40 Glu is the brain′s primary excitatory neurotransmitter. MK-801 attaches to the ion channel at the binding site PCP of the receptor. Receptor blockade occurs in a voltage-dependent manner. It also known as dizocilpine hydrogen maleate is an effective anticonvulsant with both anxiolytic and sympathomimetic properties.(+)-MK-801 hydrogen maleate stimulates locomotion in monoamine-depleted mice.

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

MK-801 increases endogenous acetylcholine release in the rat parietal cortex: a study using brain microdialysis.
Hasegawa M
Neuroscience Letters, 150(1), 53-56 (1993)
Effects of dizocilpine (MK-801) on circling behavior, swimming activity, and place preference in zebrafish (Danio rerio).
Swain HA
Neurotoxicology and Teratology, 26(6), 725-729 (2004)
Behavioral performance altering effects of MK-801 in zebrafish (Danio rerio).
Sison M and Gerlai R.
Behavioural Brain Research, 220(2), 331-337 (2011)
Elizabeth K Ruzzo et al.
Cell, 178(4), 850-866 (2019-08-10)
We performed a comprehensive assessment of rare inherited variation in autism spectrum disorder (ASD) by analyzing whole-genome sequences of 2,308 individuals from families with multiple affected children. We implicate 69 genes in ASD risk, including 24 passing genome-wide Bonferroni correction and
Gabrielle Girardeau et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 34(15), 5176-5183 (2014-04-11)
Hippocampal sharp wave-ripples (SPW-Rs) and associated place-cell reactivations are crucial for spatial memory consolidation during sleep and rest. However, it remains unclear how learning and consolidation requirements influence and regulate subsequent SPW-R activity. Indeed, SPW-R activity has been observed not

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