地卓亞平馬來酸鹽作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetDizocilpine maleateCat. No.: HY-15084CAS No.: 77086-22-7分式: CHNO分量: 337.37作靶點(diǎn): iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (296.41 mM; Need ultrasonic)Ethanol : 25 mg/

2、mL (74.10 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.9641 mL 14.8205 mL 29.6410 mL5 mM 0.5928 mL 2.9641 mL 5.9282 mL10 mM 0.2964 mL 1.4821 mL 2.9641 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month

3、。-80C 儲存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C 儲存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.41 mM)

4、; Clear solution此案可獲得 2.5 mg/mL (7.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.41 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/

5、mL (7.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.41 mM); Clear solution此案可獲得 2.5 mg/mL (7.41 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。4.

6、 請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.41 mM); Clear solution此案可獲得 2.5 mg/mL (7.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。5. 請依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline

7、)Solubility: 2.5 mg/mL (7.41 mM); Clear solution此案可獲得 2.5 mg/mL (7.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。6. 請依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 2.5 mg/mL (7.41 mM); Precipitated solution; Need ultrasonic此案可獲得 2.5 mg/mL (7.41 mM)以 1 mL 作

8、液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Dizocilpine maleate (MK-801 maleate)種有效，選擇性，競爭性的 NMDA 受體拮抗劑，Kd 值為 37.2 nM。IC & Target Ki: 37.2 nM (NMDA receptor, in rat brain membrane)1體外研究 3HDizocilpine maleate binds with NMDA receptor with a Kd of 37.2 2.7 nM in rat cereb

9、ral cortical membranes1.Dizocilpine maleate causes a progressive, long-lasting blockade of current induced by N-methyl-D-aspartate (N-Me-D-Asp)3.Dizocilpine maleate progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine fromblocking the N-Me-D-Asp-induced current, eve

10、n when Dizocilpine (MK-801) is applied for a long time in the presenceof NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches3.Dizocilpine maleate ( 500 M) inhibits activation of microglia induced by LPS with increased Cox-2 proteinexpression in BV-2 cells. Dizocilp

11、ine (MK-801; 500 M) reduces microglial TNF- output with an EC50 of 400 M inBV-2 cells4.體內(nèi)研究 Dizocilpine maleate (MK 801 maleate) (1 mg/kg) treatment before each METH injection reduces the extent of DAdepletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of

12、METH on microglialactivation in striatal of mice4.Dizocilpine maleate (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption inrats. Dizocilpine maleate (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppressionon subsequent coca

13、ine-primed reinstatement5.Dizocilpine maleate (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg,but not at 0.03 and 0.1 mg/kg6.Page 2 of 3 www.MedChemEPROTOCOLAnimal Animals are given saline or Dizocilpine (+)-MK 801) followed by cocaine 30 min late

14、r in the home cage instead of inAdministration 5 the CPP apparatus for the two days of “reactivation.” This is done to determine whether reactivation of the memoryfor the cocaine-associated context by cocaine in the CPP context is necessary for the ability of Dizocilpine (+)-MK801) to disrupt recons

15、olidation. Animals undergo preconditioning, conditioning, testing, and extinction but animalsare injected with saline or Dizocilpine (+)-MK 801) (0.20 mg/kg, i.p.) 30 min prior to a cocaine injection (10 mg/kg,i.p.) in the home cage. Animals remain in the home cages, and the next day, the procedure

16、from the first day ofreactivation is repeated. The following day, animals are tested for cocaine-primed reinstatement in their CPP boxwithout any prior microinjection of saline or Dizocilpine (+)-MK 801).MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶

17、使本產(chǎn)品發(fā)表的科研獻(xiàn) Front Cell Dev Biol. 2020 Feb 4;8:24. Front Cell Neurosci. 2019 Jun 25;13:276. Front Neurosci. 2019 Nov. Eur J Pharmacol. 2019 May 29:172427. Evid-Based Compl Alt. 2020 Mar.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Wong EH, et al. The anticonvulsant

18、MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.2. Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269.3. Huettner JE, et al. Block of N-methyl-D-aspartate-activated current by

19、 the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad SciU S A. 1988 Feb;85(4):1307-11.4. Thomas DM, et al. MK-801 and dextromethorphan block microglial activation and protect against methamphetamine-induced neurotoxicity. Brain Res.2005 Jul 19;1050(1-2):190-8.5. Brown TE, et al. The NMDA antagonist MK-801 disrupts reconsolidation of a cocaine-associated memory for conditioned place preference but not forself-administration in rats. Learn Mem. 2008 Dec 2;15(