您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > (1R,2S)-VU0155041
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
(1R,2S)-VU0155041
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(1R,2S)-VU0155041图片
CAS NO:1263273-14-8
规格:98%
分子量:316.18
包装与价格:
包装价格(元)
100mg电议
50mg电议
5mg电议
10mg电议
25mg电议

产品介绍
(1R,2S)-VU0155041是VU0155041的顺式异构体。(1R,2S)-VU0155041是mGluR4的部分激动剂,EC50值为2.35 μM。
CAS:1263273-14-8
分子式:C14H15Cl2NO3
分子量:316.18
纯度:98%
存储:Store at -20°C

Background:

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.


At both human and rat receptors, the Cis regioisomer of VU0155041 is similar in potency (798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4). Conversely, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. Fold-shift experiments at 30 μM of VU0155041 also shows that the Cis regioisomer is more effective at this concentration on both human and rat mGluR4. VU0155041, induces concentration-dependent shifts in the baseline when examined in fold shift experiments using the thallium flux assay. VU0155041 induces a response that reaches approximately 45% of the maximal glutamate response. VU0155041is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site. VU0155041 exhibitsselectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors[1].


VU0155041 is soluble in an aqueous vehicle and intracerebroventricular administration of 31 to 316 nM of VU0155041 dose-dependently decreases haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041, at doses of 31 and 92 nmol, is also able to significantly decrease the cataleptic effects of haloperidol, and the effects of the compound are still present 30 min after infusion. Icv infusion of a 316 nmol dose of VU0155041 also results in a significant reversal of akinesia[1].


参考文献:
[1]. Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positiveallosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58.