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MPEP Hydrochloride Sale

(Synonyms: 2-甲基-6-(苯基乙炔基)吡啶盐酸盐) 目录号 : GC16172

MPEP Hydrochloride是一种非竞争性、选择性的、强效、有口服活性和系统活性的mGlu5受体拮抗剂,其完全抑制quisqualate 刺激的磷酸肌醇水解的IC50为36nM。

MPEP Hydrochloride Chemical Structure

Cas No.:219911-35-0

规格 价格 库存 购买数量
10mM (in 1mL Water)
¥297.00
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5mg
¥270.00
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10mg
¥450.00
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25mg
¥855.00
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50mg
¥1,530.00
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100mg
¥2,430.00
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Sample solution is provided at 25 µL, 10mM.

Description

MPEP Hydrochloride 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 Hydrochloride 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 Hydrochloride 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 Hydrochloride(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 Hydrochloride (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.

MPEP Hydrochloride是一种非竞争性、选择性的、强效、有口服活性和系统活性的mGlu5受体拮抗剂,其完全抑制quisqualate 刺激的磷酸肌醇水解的IC50为36nM[1]。MPEP Hydrochloride具有抗焦虑或抗抑郁样作用[2],通常用于神经系统疾病的研究,如脆性X综合征[3]和癫痫[4]

在体外,鱼藤酮处理前30min用10μM MPEP Hydrochloride预处理MN9D细胞,逆转了鱼藤酮处理诱导的p-PERK和γ -H2AX表达水平的升高,并减轻了酪氨酸羟化酶的降低[5]

在体内,腹腔注射MPEP Hydrochloride(30mg/kg; 3days)降低了在暗中饮酒(DID)期间雄性和雌性C57BL/6小鼠的酒精摄入量,而没有改变Homer2/Erk2表达[6]。在对照小鼠和多巴胺损伤小鼠中,腹腔注射MPEP Hydrochloride(3mg /kg, 30min)促进安非他命诱导的行为学效应,且不依赖于具体测量行为[7]

实验参考方法

Cell experiment [1]:

Cell lines

MN9D cells

Preparation Method

MN9D cells were pretreated with 10μM MPEP Hydrochloride 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 Hydrochloride 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 Hydrochloride was dissolved in saline and injected i.p. at 10 ml/kg body weight. A range of doses from 0–30mg/kg MPEP Hydrochloride 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 Hydrochloride lowered alcohol consumption during DID in male and female C57BL/6 mice without changes in Homer2/Erk2 expression.

References:
[1] 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.
[2] 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.

化学性质

Cas No. 219911-35-0 SDF
别名 2-甲基-6-(苯基乙炔基)吡啶盐酸盐
化学名 2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride
Canonical SMILES CC1=CC=CC(=N1)C#CC2=CC=CC=C2.Cl
分子式 C14H12ClN 分子量 229.7
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 5 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 4.3535 mL 21.7675 mL 43.535 mL
5 mM 0.8707 mL 4.3535 mL 8.707 mL
10 mM 0.4354 mL 2.1768 mL 4.3535 mL
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