产品
编 号:F428570
分子式:C22H15ClN2O4
分子量:406.82
产品类型
结构图
CAS No: 693288-97-0
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产品详情
生物活性:
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.
体外研究:
CPPHA alone has no agonist activity.CPPHA causes concentration-dependent potentiation of the response of human mGluR5 CHO cells to agonists.CPPHA potentiates threshold response to glutamate in fluorometric Ca2+ assays 7- to 8-fold with EC50 values in the 400 to 800 nM range.CPPHA (20 μM; 15 minutes) potentiates the response to a subthreshold concentration of DHPG (HY-12598A) on ERK and cyclic-AMP responsive element-binding protein (CREB) activity, as well as NMDA receptor subunit NR1 phosphorylation in cortical and hippocampal slices.