(+)-Dizocilpine (MK 801) Maleate

製品コードS2876 バッチS287602

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₆H₁₅N.C₄H₄O₄
	分子量	337.37	CAS No.	77086-22-7
Solubility (25°C)*	体外	DMSO	67 mg/mL (198.59 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes.
in vitro	[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. ^[1] 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. ^[2] 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. ^[3] 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. ^[4]
in vivo	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. ^[4] 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. ^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	Cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold 0.32 M sucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1×10³ g, and the supernatant is recentrifuged at 1×10⁴ g for 20 min at 4 ℃. The pellet is suspended in assay buffer (118 mM NaCl/4.7 mM KCl/1.2mM MgSO₄/5 mM NaHCO₃/20 mM Hepes/1.2 mM KH₂PO₄/2.5 mM CaCl₂/11 mM glucose, pH 7.4) and incubated at 23℃ for 20 min prior to final centrifugation at 1×10³ g for 20 min at 4 ℃. The pellet is resuspended in assay buffer (70 ml per gram of original tissue). Binding of [³H]MK-801 is measured by incubating 750 μL duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 μL of buffer containing displacer or of buffer alone (total binding), 100 μL of 50 nM [³H]MK-801, and 50 μL of buffer for 60 min at 23 ℃. Nonspecific binding is defined by 100 μM (final concentration) unlabeled MK-801.
動物実験	動物モデル	Male Sprague-Dawley and Long-Evans Hooded rats
	投薬量	0.2 mg/kg
	投与方法	Intraperitoneal injection

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Sevoflurane upregulates neuron death process-related Ddit4 expression by NMDAR in the hippocampus [ Aging -Albany NY), 2023, 15(12):5698-5712]	PubMed: 37348034
Sevoflurane upregulates neuron death process-related Ddit4 expression by NMDAR in the hippocampus [ Aging (Albany NY), 2023, 15(12):5698-5712]	PubMed: 37348034
N-Methyl D-aspartate receptor subtype 2B/Ca2+/calmodulin-dependent protein kinase II signaling in the lateral habenula regulates orofacial allodynia and anxiety-like behaviors in a mouse model of trigeminal neuralgia [ Front Cell Neurosci, 2022, 16:981190]	PubMed: 36187288
Functionally distinct roles for eEF2K in the control of ribosome availability and p-body abundance [ Nat Commun, 2021, 12(1):6789]	PubMed: 34815424
Unraveling Autocrine Signaling Pathways through Metabolic Fingerprinting in Serous Ovarian Cancer Cells [ Biomedicines, 2021, 9(12)1927]	PubMed: 34944743
Lipid bilayers regulate allosteric signal of NMDA receptor GluN1 C-terminal domain [ Biochem Biophys Res Commun, 2021, 585:15-21]	PubMed: 34781056
Evaluation of acute and chronic nociception in subchronically administered MK-801-induced rat model of schizophrenia [ Behav Pharmacol, 2021, 32(7):571-580]	PubMed: 34494988
Bivalves are NO different: nitric oxide as negative regulator of metamorphosis in the Pacific oyster, Crassostrea gigas [ BMC Dev Biol, 2020, 20(1):23]	PubMed: 33228520
Propofol attenuates the adhesion of tumor and endothelial cells through inhibiting glycolysis in human umbilical vein endothelial cells. [ Acta Biochim Biophys Sin (Shanghai), 2019, 51(11):1114-1122]	PubMed: 31650167
Activation of the N-methyl-d-aspartate receptor is involved in glyphosate-induced renal proximal tubule cell apoptosis [ J Appl Toxicol, 2019, 39(8):1096-1107]	PubMed: 30907447

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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