A positive allosteric modulator of the mGluR5; potentiates human and rat mGluR5 activation by glutamate

CPPHA – 1 mg

Brand:
Cayman
CAS:
693288-97-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

CPPHA is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) that potentiates human and rat mGluR5 activation by glutamate, 3,5-DHPG (Item No. 14411), and quisqualate (EC50s = 0.316-0.5 and 0.634-1.16 μM for human and rat mGluR5, respectively).{35227} It is selective for mGluR5 over other mGluRs but exhibits submicromolar activity at PDE6, δ- and κ-opioid receptors, and the ether-a-go-go related gene (ERG) potassium channel (Kis = 500, 352, 474, and 813 nM, respectively). CPPHA potentiates 3,5-DHPG-induced NMDA currents in CA1 pyramidal cells and the depolarization of rat subthalamic nucleus (STN) neurons.  

 

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Description

A positive allosteric modulator of the mGluR5; potentiates human and rat mGluR5 activation by glutamate, 3,5-DHPG, and quisqualate (EC50s = 0.316-0.5 and 0.634-1.16 μM for human and rat mGluR5, respectively); potentiates 3,5-DHPG-induced NMDA currents in CA1 pyramidal cells and the depolarization of STN neurons

Formal name: N-[4-chloro-2-[(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)methyl]phenyl]-2-hydroxy-benzamide

Synonyms: 

Molecular weight: 406.8

CAS: 693288-97-0

Purity: ≥98%

Formulation: A powder

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience

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