MPEP

製品コードS2809 バッチS280901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H11N
分子量 193.24 CAS No. 96206-92-7
Solubility (25°C)* 体外 DMSO 39 mg/mL (201.82 mM)
Ethanol 39 mg/mL (201.82 mM)
Water 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.
in vitro MPEP has no appreciable agonist or antagonist activity at the closely related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a purinoreceptor endogenously expressed in L(tk-) cells up to concentrations of 100 μM. Furthermore, MPEP shows no appreciable agonist or antagonist activity in cAMP accumulation or [35S]-GTPγS binding assays at the recombinant human group II and III metabotropic receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6) receptor subtypes. In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. [1] MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist L-AP4. [3]
in vivo When microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, MPEP produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of MPEP also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. [1] MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. MPEP (1-20 mg/kg) shortens the immobility time in a tail suspension test in mice, but it is inactive in the behavioural despair test in rats. MPEP has no effect on locomotor activity or motor coordination. [2] MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. [4]
特徴 Inactive against other group I/II/III metabotropic glutamate receptors.

プロトコル(参考用のみ)

キナーゼアッセイ PI hydrolysis assay
MPEP is tested for antagonist activity at cloned human mGlu5a receptors expressed in L(tk-) cells. Clonal cell lines expressing human mGluR5 receptors are seeded in 24-well tissue culture plates. Cells are labeled to equilibrium with 2 μCi/ml myo-[3H]inositol for 20 hours in Dulbecco's modified Eagle's medium, washed twice in Krebs-Henseleit buffer, and incubated for 30 minutes at room temperature. Subsequently, cells are washed in buffer containing 10 mM LiCl and incubated in the same medium for 20 minutes at 37 °C. After aspiration of medium, increasing concentration of MPEP is added to triplicate wells. For test of antagonist activity, a submaximal concentration of quisqualate (0.3 μM) is added immediately after application of MPEP. The reaction is stopped after an incubation of 20 minutes at 37 °C by aspiration of the medium and lysis of the cells with 0.75 mL of ice-cold 10 mM formic acid (pH 3). After 30 minutes the extract is diluted into 2 mL of 5 mM NH3solution (yielding a final pH of 8-9) and applied to a column containing DOWEX-1 × 8. After flow-through of the extract, columns are washed with 10 mL of H2O and 6 mL of 5 mM sodium tetraborate, 60 mM sodium formate, respectively. Inositol monophosphates are eluted with 6 mL of 100 mM formic acid, 200 mM ammonium formate. The eluted samples are counted 7 hours after addition of 15 mL Irgasave Plus scintillation cocktail in a Tricarb 2700tr counter.
動物実験 動物モデル Male Wistar rats, male Albino Swiss mice, or male C57BL/6J mice subjected to various tests
投薬量 ~30 mg/kg
投与方法 Administered intraperitoneally (i.p.) or perorally (p.o.) at 60 minutes before the tests

カスタマーフィードバック

Data from [Data independently produced by , , Mol Neurobiol, 2017, 54(7):5286-5299]

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：

Pu-erh Tea Protects the Nervous System by Inhibiting the Expression of Metabotropic Glutamate Receptor 5. [Li C, et al. Mol Neurobiol, 2017, 54(7):5286-5299] PubMed: 27578019

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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