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CAS No.: 96206-92-7

MPEP Catalog No. CSN11477

MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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maze and the open field, low doses of MPEP (2.5, 5 mg/kg) significantly compromised the locomotor activities of ethanol withdrawn rats.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 ... more >> 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 Collapse <<
NCT03506945	Depressive Symptoms ... more >> Stress, Psychological Collapse <<	Not Applicable	Not yet recruiting	July 2023	United States, California ... more >> University of California San Diego La Jolla, California, United States, 92093 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.1748 mL
- 25.8741 mL
- 51.7481 mL
- 5 mM
- 1.0350 mL
- 5.1748 mL
- 10.3496 mL
- 10 mM
- 0.5175 mL
- 2.5874 mL
- 5.1748 mL

技术信息

CAS号

96206-92-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H11N

运输

蓝冰

分子量

193.24

别名

溶解度

DMSO	165.0 mg/mL (853.8 mM)
Water	310.0 mg/mL (1604.2 mM)

动物实验配方

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MPEP Catalog No. CSN11477

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