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CPPHA

Catalog No. T10881 CAS 693288-97-0

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

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CPPHA, CAS 693288-97-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 55.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 189.00
50 mg	In stock	$ 319.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.61%

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Description	CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.
In vitro	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 (EC50s: 400 to 800 nM), and at 10 μM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and DHPG 4- to 7-fold to the left. CPPHA (10 μM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 μM 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].
Cell Research	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 (EC50s: 400 to 800 nM), and at 10 μM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and DHPG 4- to 7-fold to the left. CPPHA (10 μM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 μM 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].

Molecular Weight	406.82
Formula	C22H15ClN2O4
CAS No.	693288-97-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (221.2 mM), Sonication is recommended.

References and Literature

1. Liu F, et al. The effect of mGlu5 receptor positive allosteric modulators on signaling molecules in brain slices. Eur J Pharmacol. 2006 May 1;536(3):262-8. 2. O'Brien JA, et al. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther. 2004 May;309(2):568-77. 3. Zhang Y, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. J Pharmacol Exp Ther. 2005 Dec;315(3):1212-9.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

CPPHA 693288-97-0 Neuroscience GluR inhibitor inhibit

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