(1R,2S)-VU0155041
目录号 : GC34963(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 No.:1263273-14-8
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Animal experiment: | Rats: TVC rats are injected with reserpine and kept in their home cages for 2 hr after injection. Activity is measured by placing rats in photocell activity cages equipped with 16×16 infrared beams. After a 30 min baseline period, rats are given a single intracerebroventricular injection of either L-AP4 (100, 300 or 1000 nM), VU0155041 (93 or 316 nM), or corresponding vehicles, and motor activity is recorded for an additional 30 min[1]. |
References: [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. |
(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].
References:
[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.
Cas No. | 1263273-14-8 | SDF | |
Canonical SMILES | O=C([C@H]1[C@@H](C(NC2=CC(Cl)=CC(Cl)=C2)=O)CCCC1)O | ||
分子式 | C14H15Cl2NO3 | 分子量 | 316.18 |
溶解度 | DMSO: ≥ 59 mg/mL (186.60 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.1628 mL | 15.8138 mL | 31.6276 mL |
5 mM | 0.6326 mL | 3.1628 mL | 6.3255 mL |
10 mM | 0.3163 mL | 1.5814 mL | 3.1628 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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