MPEP |
| رقم الكتالوجGC10864 |
MPEP هو مضاد لمستقبلات mGlu5 فعال وانتقائي وغير تنافسي ونشط عن طريق الفم ، مع IC 50 من 36 نانومتر لتثبيط التحلل المائي بفوسفوينوسيتيد (PI) المحفز تمامًا
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 96206-92-7
Sample solution is provided at 25 µL, 10mM.
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MPEP is a noncompetitive, selective, potent, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis[1]. MPEP has anxiolytic-or antidepressant-like effects[2] and is usually used in the study of neurological disorders, such as fragile X syndrome[3] and epilepsy[4] .
In vitro, pretreatment of MN9D cells with 10μM MPEP 30min prior to rotenone exposure reversed the increase in p-PERK and γ -H2AX expression levels and alleviated the decrease in tyrosine hydroxylase induced by rotenone treatment[5] .
In vivo, intraperitoneal injection of MPEP(30mg/kg; 3days) lowered alcohol consumption during Drinking in the Dark (DID) in male and female C57BL/6 mice without changes in Homer2/Erk2 expression[6] . Intraperitoneal injection of MPEP (3 mg/kg, 30min) facilitates amphetamine-induced effects independently on the behavior measured both in naïve and in dopamine lesioned mice[7].
References:
[1] Gasparini, F., Lingenhöhl, K., Stoehr, N., Flor, P. J., Heinrich, M., Vranesic, I., Biollaz, M., Allgeier, H., Heckendorn, R., Urwyler, S., Varney, M. A., Johnson, E. C., Hess, S. D., Rao, S. P., Sacaan, A. I., Santori, E. M., Veliçelebi, G., & Kuhn, R. (1999). 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology, 38(10), 1493–1503.
[2] Tatarczyńska, E., Klodzińska, A., Chojnacka-Wójcik, E., Palucha, A., Gasparini, F., Kuhn, R., & Pilc, A. (2001). Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. British journal of pharmacology, 132(7), 1423–1430.
[3] Castrén, M. L., & Castrén, E. (2014). BDNF in fragile X syndrome. Neuropharmacology, 76 Pt C, 729–736.
[4] Moldrich, R. X., Chapman, A. G., De Sarro, G., & Meldrum, B. S. (2003). Glutamate metabotropic receptors as targets for drug therapy in epilepsy. European journal of pharmacology, 476(1-2), 3–16.
[5] Gu, L., Luo, W. Y., Xia, N., Zhang, J. N., Fan, J. K., Yang, H. M., Wang, M. C., & Zhang, H. (2022). Upregulated mGluR5 induces ER stress and DNA damage by regulating the NMDA receptor subunit NR2B. Journal of biochemistry, 171(3), 349–359.
[6] Huang, G., Thompson, S. L., & Taylor, J. R. (2021). MPEP Lowers Binge Drinking in Male and Female C57BL/6 Mice: Relationship with mGlu5/Homer2/Erk2 Signaling. Alcoholism, clinical and experimental research, 45(4), 732–742.
[7] Managò, F., Lopez, S., Oliverio, A., Amalric, M., Mele, A., & De Leonibus, E. (2013). Interaction between the mGlu receptors 5 antagonist, MPEP, and amphetamine on memory and motor functions in mice. Psychopharmacology, 226(3), 541–550.
| Cell experiment [1]: | |
Cell lines | MN9D cells |
Preparation Method | MN9D cells were pretreated with 10μM MPEP for 30min followed by different concentration of rotenone or (RS)-2-chloro-5- hydroxyphenylglycine (CHPG) treatment for indicated time. The expression levels of p-PERK, γ -H2AX and tyrosine hydroxylase were detected by Western blot. |
Reaction Conditions | 10μM; 30min |
Applications | MPEP reversed the increase in p-PERK and γ -H2AX expression levels and alleviated the decrease in tyrosine hydroxylase induced by rotenone treatment. |
| Animal experiment [2]: | |
Animal models | C57BL/6NCrl mice |
Preparation Method | The animals used in this study were male and female C57BL/6NCrl mice purchased from Charles River Laboratories (Strain Code #027) at seven weeks of age. Upon delivery, mice were singly housed with food ad libitum. Water was provided ad libitum via a water bottle except for during the Drinking in the Dark (DID) sessions. A 20% ethanol drinking solution for the DID experiments was made with 200 proof ethanol diluted with tap water (v/v) and used within 24h. MPEP was dissolved in saline and injected i.p. at 10 ml/kg body weight. A range of doses from 0–30mg/kg MPEP were used in these studies. After the completion of the final MPEP dose the animals continued on DID for three days to test for blood ethanol concentrations. |
Dosage form | 0–30mg/kg for 3days; i.p. |
Applications | 30mg/kg MPEP lowered alcohol consumption during DID in male and female C57BL/6 mice without changes in Homer2/Erk2 expression. |
References: | |
| Cas No. | 96206-92-7 | SDF | |
| Chemical Name | 2-methyl-6-(2-phenylethynyl)pyridine | ||
| Canonical SMILES | CC1=CC=CC(=N1)C#CC2=CC=CC=C2 | ||
| Formula | C14H11N | M.Wt | 193.24 |
| الذوبان | ≥ 9.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.1749 mL | 25.8746 mL | 51.7491 mL |
| 5 mM | 1.035 mL | 5.1749 mL | 10.3498 mL |
| 10 mM | 517.5 μL | 2.5875 mL | 5.1749 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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