781652-57-1|3-Cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide|CsnPharm

CAS No.: 781652-57-1

CDPPB Catalog No. CSN27612

Synonyms: 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. At 1 mM, CDPPB shifted mGluR5 agonist concentration response curves to glutamate, quisqualate, and (R,S)-3,5-dihydroxyphenylglycine 3- to 9-fold to the left. At higher concentrations, CDPPB exhibited agonist-like activity on cells expressing mGluR5^[1]. Chronic treatment of BACHD mice with CDPPB 1.5 mg/kg s.c. for 18 weeks increased the activation of cell signaling pathways important for neuronal survival, including increased AKT and ERK1/2 phosphorylation and augmented the BDNF mRNA expression. CDPPB chronic treatment was also able to prevent the neuronal cell loss that takes place in the striatum of BACHD mice and decrease htt aggregate formation. Moreover, CDPPB chronic treatment was efficient to partially ameliorate motor incoordination and to rescue the memory deficit exhibited by BACHD mice^[2]. Consistent with a reduction of cortical mGlu5 receptor density and phosphorylation, CDPPB (30 mg/kg) significantly affected sleep architecture as determined by cortical EEG at day one however by the seventh day of dosing all sleep changes were absent^[3].
参考文献

[1] Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J Pharmacol Exp Ther. 2005 Apr;313(1):199-206
[2] Doria JG, de Souza JM, Andrade JN, Rodrigues HA, Guimaraes IM, Carvalho TG, Guatimosim C, Dobransky T, Ribeiro FM. The mGluR5 positive allosteric modulator, CDPPB, ameliorates pathology and phenotypic signs of a mouse model of Huntington's disease. Neurobiol Dis. 2015 Jan;73:163-73
[3] Parmentier-Batteur S, O'Brien JA, Doran S, Nguyen SJ, Flick RB, Uslaner JM, Chen H, Finger EN, Williams TM, Jacobson MA, Hutson PH. Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration. Neuropharmacology. 2012 Mar;62(3):1453-60

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
- 2.7442 mL
- 13.7212 mL
- 27.4424 mL
- 5 mM
- 0.5488 mL
- 2.7442 mL
- 5.4885 mL
- 10 mM
- 0.2744 mL
- 1.3721 mL
- 2.7442 mL

技术信息

CAS号	781652-57-1	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C23H16N4O	运输	蓝冰
分子量	364.40	别名	3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

CDPPB Catalog No. CSN27612

靶点选择性

请登录您的专属账户

确认信息