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MPEP

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Chemical Structure| 96206-92-7 同义名 : -
CAS号 : 96206-92-7
货号 : A271724
分子式 : C14H11N
纯度 : 99%+
分子量 : 193.244
MDL号 : MFCD03787983
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(543.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • mGluR5

    mGluR5, IC50:36 nM
描述 MPEP 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 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[3]. MPEP at 10 mg/kg significantly attenuated ethanol withdrawal induced anxiety without any compromising effects on locomotor activities. Despite reversing several indices of ethanol withdrawal induced anxiety in both the elevated plus maze and the open field, low doses of MPEP (2.5, 5 mg/kg) significantly compromised the locomotor activities of ethanol withdrawn rats. High doses of MPEP (20 and 30 mg/kg) significantly attenuated withdrawal anxiety when tested in the elevated plus maze but not in the open field. Administration of MPEP (2.5, 5, 10, 20, 30 mg/kg) has no significant compromising effect on the locomotor activities of ethanol naïve rats[4]. MPEP (10 and 30 mg/kg) significantly enhanced both the sedative and hypnotic effects of ethanol[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01024491 Premature Ejaculation Phase 3 Completed - Mexico ... 展开 >> Asociacion Mexicana para la Salud Sexual, A.C. Mexico City, Mexico D.F., Mexico, 14000 Centro Especializado en Urología y Andrología del Hospital Star Médica Mexico City, Mexico D.F, Mexico, 06700 收起 <<
NCT03506945 Depressive Symptoms ... 展开 >> Stress, Psychological 收起 << Not Applicable Not yet recruiting July 2023 United States, California ... 展开 >> University of California San Diego La Jolla, California, United States, 92093 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.17mL

1.03mL

0.52mL

25.87mL

5.17mL

2.59mL

51.75mL

10.35mL

5.17mL
参考文献

[1]Chau P, Soderpalm B, et al. The mGluR5 antagonist MPEP elevates accumbal dopamine and glycine levels; interaction with strychnine-sensitive glycine receptors. Addict Biol. 2011 Oct;16(4):591-9.

[2]Gasparini F, Lingenhohl K, et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503.

[3]Gasparini F, Lingenhöhl K, Stoehr N, Flor PJ, Heinrich M, Vranesic I, Biollaz M, Allgeier H, Heckendorn R, Urwyler S, Varney MA, Johnson EC, Hess SD, Rao SP, Sacaan AI, Santori EM, Veliçelebi G, Kuhn R. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503

[4]Kumar J, Hapidin H, Bee YT, Ismail Z. Effects of the mGluR5 antagonist MPEP on ethanol withdrawal induced anxiety-like syndrome in rats. Behav Brain Funct. 2013 Nov 26;9:43

[5]Sharko AC, Hodge CW. Differential modulation of ethanol-induced sedation and hypnosis by metabotropic glutamate receptor antagonists in C57BL/6J mice. Alcohol Clin Exp Res. 2008 Jan;32(1):67-76