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CPPHA,mGlu1和mGlu5受体的正变构调节剂

CPPHA （订货以英文为准）

编号：C127791
CAS号：693288-97-0
分子式：C22H15N2O4CL
分子量：406.82
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C127791-25mg 阿拉丁 25mg ¥1812.90
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C127791-50mg 阿拉丁 50mg ¥3254.90
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C127791-10mg 阿拉丁 10mg ¥1470.90
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C127791-100mg 阿拉丁 100mg ¥5870.90
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产品名称 CPPHA
中文名称 CPPHA,mGlu1和mGlu5受体的正变构调节剂
CAS号 693288-97-0
分子式（M.F.） C22H15N2O4CL
分子量（M.W.） 406.82
储存条件 -20°C储存
溶解性25°C: DMSO
存贮条件储存温度-20°C
产品介绍CPPHA
生化机理Description:IC50 Value: N/ACPPHA is a selective positive allosteric modulator of mGluR5 receptor. It has no agonist activity alone, but reduces threshold response and shifts dose-response curves to glutamate, quisqualate, and DHPG by 4- to 7-fold to the left in recombinant CHO cells expressing human or rat mGluR5.in vitro: The selective mGlu5 receptor positive allosteric modulator, N-{4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2yl)-methyl]phenyl}-2-hydrobenzamide (CPPHA) potentiated the response to a subthreshold concentration of 3,5-dihydroxy-phenylglycine (DHPG) on extracellular signal-regulated protein kinase (ERK) and cyclic-AMP responsive element-binding protein (CREB) activity, as well as N-methyl d-aspartate (NMDA) receptor subunit NR1 phosphorylation in cortical and hippocampal slices [1]. CPPHA potentiated threshold responses to glutamate in fluorometric Ca(2+) assays 7- to 8-fold with EC(50) values in the 400 to 800 nM range, and at 10 microM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and (R,S)-3,5-dihydroxyphenylglycine (DHPG) 4- to 7-fold to the left.  CPPHA (10 microM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 microM CPPHA also potentiated mGluR5-mediated DHPG-induced depolarization of rat subthalamic nucleus neurons [2]. CPPHA induced an increase in basal mGluR5-mediated ERK1/2 phosphorylation and potentiated the effect of low concentrations of agonists. In contrast, CPPHA significantly decreased ERK1/2 phosphorylation induced by high concentrations of agonists [3].in vivo: N/AToxicity: N/AClinical trial: N/A
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