MPEP (Hydrochloride)
Based on 10 publication(s) in Google Scholar
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects. MPEP (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.82%
- CAS 番号: 219911-35-0
- 分子式: C14H12ClN
- 分子量:229.70
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 MPEP Hydrochloride
More- Nat Commun. 2026 Jul 17;17(1):8774.
- Brain Behav Immun. 2026 Jul:135:106529. [Abstract]
- Int J Mol Sci. 2026 Apr 6;27(7):3306. [Abstract]
- Pharmacol Biochem Behav. 2023 Jun:227-228:173588. [Abstract]
- Epilepsy Res. 2021 Sep:175:106677. [Abstract]
- Neurosci Lett. 2025 Mar 15:852:138193. [Abstract]
- bioRxiv. 2026 Jan 28.
- SSRN. 2025 Aug 27.
- bioRxiv. 2024 November 03.
- SSRN. 2023 Apr 26.
生物活性
製品説明
IC50 & Target
[1]|
mGluR5 36 nM (IC50) |
体外実験
MPEP does not show agonist or antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μM on the human mGlu6 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MPEP (1-20 mg/kg) does shorten the immobility time in a tail suspension test in mice, however it is inactive in the behavioural despair test in rats[2].
MPEP (30 mg/kg i.p.) slightly but significantly increases (by 39%) the number of punished crossings in the four-plate test, lower doses of the compound (3 and 10 mg/kg) does not affect the number of punished crossings in that test (F (3,36)=3.240, P<0.05)[2].
MPEP (1, 10 and 20 mg/kg) significantly (by 55% after the highest dose), (F(3,28)=15.47, P<0.001) decreases the immobility time of mice in the tail suspension test. Its efficacy is similar to that of imipramine (20 mg/kg), used as the positive standard[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (200 ± 250 g)[2].
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Dosage:IP or PO.
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Administration:0.3, 1 and 10 mg/kg, i.p. (Conflict drinking test).
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Result:At a dose of 0.3 mg/kg was not ffective, at doses of 1 and 10 mg/kg i.p. significantly (F (3,30)=11.193, P<0.001), increased the number of shocks (by 330 and 507%, respectively) accepted during the experimental session in the Vogel test.
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Animal Model:Male Wistar rats (200 ± 250 g)[2].
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Dosage:IP or PO.
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Administration:1, 3 and 10 mg/kg, i.p. or 10 and 30 mg/kg, p.o.(Elevated plus-maze test).
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Result:Administered at a dose of 1 mg kg71 i.p. did not change the entries into and time spent in the open arms. At doses of 3 and 10 mg/kg i.p. significantly (F (3,24)=22.978, P<0.001) dose-dependently increased the time spent in the open arms (up to 45 and 74%, respectively), and the percentage of entries into the open arms (up to 48 and 68%, respectively, F(3,24)=5.678, P<.01). At doses of 3 and 10 mg/kg i.p. significantly increased (by 64%) the total number of entries and reduced (by about 25%) the total time spent (data not shown) in the arms (either type).
At the dose of 30 mg/kg (po, but not 10 mg/kg) significantly (up to 64%, F (2,16)=14.249, P<0.001) increased the percentage of the time spent in the open arms and the percentage of entries into the open arms (up to 63%, F (2,16)=7.295, P<0.01). MPEP given p.o. in both doses used did not change the total number of entries nor the total time spent in the arms (either type).
化学情報
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CAS 番号 219911-35-0
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性状 Solid
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分子量 229.70
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分子式 C14H12ClN
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Color White to off-white
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SMILES
CC1=NC(C#CC2=CC=CC=C2)=CC=C1.[H]Cl
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別名
MPEP 塩酸塩
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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Brain Behav Immun
NR2B-CaMKII signaling in the dentate gyrus driven by astrocytic P2Y1Rs mediates the antidepressant effect of low-dose LPS. [Abstract]2026 Jul:135:106529. PMID: 41796645 -
Int J Mol Sci
Neurogranin Promotes Neuronal Maturation and Network Activity Through Ca2+/Calmodulin Signaling. [Abstract]2026 Apr 6;27(7):3306. PMID: 41977485 -
Pharmacol Biochem Behav
Anxiolytic-like effects of an mGluR 5 antagonist and a mGluR 2/3 agonist, and antidepressant-like effects of an mGluR 7 agonist in the chick social separation stress test, a dual-drug screening model of treatment-resistant depression. [Abstract]2023 Jun:227-228:173588. PMID: 37348610 -
Epilepsy Res
2021 Sep:175:106677. PMID: 34130255 -
Neurosci Lett
Intracellular metabotropic glutamate receptor 5 in spinal dorsal horn neurons contributes to pain in a mouse model of vincristine-induced neuropathic pain. [Abstract]2025 Mar 15:852:138193. PMID: 40074023 -
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溶剤 & 溶解度
体外:
H2O : 25 mg/mL (108.84 mM; ultrasonic and warming and heat to 80°C)
DMSO : 17.5 mg/mL (76.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Saline
Solubility: 100 mg/mL (435.35 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. F Gasparini, et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a Potent, Selective and Systemically Active mGlu5 Receptor Antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503. [Content Brief]
[2]. E Tatarczyńska, et al. Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. Br J Pharmacol. 2001 Apr;132(7):1423-30. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.3535 mL | 21.7675 mL | 43.5350 mL | 108.8376 mL |
| 5 mM | 0.8707 mL | 4.3535 mL | 8.7070 mL | 21.7675 mL | |
| 10 mM | 0.4354 mL | 2.1768 mL | 4.3535 mL | 10.8838 mL | |
| 15 mM | 0.2902 mL | 1.4512 mL | 2.9023 mL | 7.2558 mL | |
| 20 mM | 0.2177 mL | 1.0884 mL | 2.1768 mL | 5.4419 mL | |
| 25 mM | 0.1741 mL | 0.8707 mL | 1.7414 mL | 4.3535 mL | |
| 30 mM | 0.1451 mL | 0.7256 mL | 1.4512 mL | 3.6279 mL | |
| 40 mM | 0.1088 mL | 0.5442 mL | 1.0884 mL | 2.7209 mL | |
| 50 mM | 0.0871 mL | 0.4354 mL | 0.8707 mL | 2.1768 mL | |
| 60 mM | 0.0726 mL | 0.3628 mL | 0.7256 mL | 1.8140 mL | |
| H2O | 80 mM | 0.0544 mL | 0.2721 mL | 0.5442 mL | 1.3605 mL |
| 100 mM | 0.0435 mL | 0.2177 mL | 0.4354 mL | 1.0884 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.