|((7-吗啉-2,3-二氧代-6-三氟甲基-3,4-二氢喹恶啉-1(2H)-基)甲基)磷酸|CsnPharm

CAS No.: 161605-73-8

Fanapanel Catalog No. CSN17953

Synonyms: ZK200775;MPQX;ZK200775. 161605-73-8

ZK200775 is a highly selective AMPA/kainate antagonist with little activity against NMDA with Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

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The alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropion-ate (AMPA) subtype of ionotropic glutamate receptor mediates rapid responses at the majority of excitatory synapses in the CNS. These receptors are heterotetramers composed of various combinations of four subunits: GluR1-4^[3]. ZK200775 is a highly selective AMPA/kainate antagonist with little activity against NMDA (N-methyl-d-aspartate). In the cortical slice preparation assay, ZK200775 gave K_i values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. In the spreading depression assay, it gave IC₅₀ values of 200 nM, 76 nM, 13 μM, and 18 μM against quisqualate, kainate, NMDA, and glycine. Currents evoked by kainate (nondesensitizing AMPA agonist at 100 μM) were inhibited by ZK200775 with an IC₅₀ of 27 nM. Currents evoked by AMPA (100 μM) were inhibited by ZK200775 with IC₅₀s of 21 and 90 nM, for peak and plateau currents, respectively. ZK200775 in doses of 0.3-3 mg/kg i.p. significantly enhanced punished locomotor activity in mice, leaving spontaneous locomotor activity in unpunished mice unchanged. ZK200775 elevated the threshold for AMPA- and kainate-induced clonic seizures in mice with a THRD₅₀ (threshold dose) of 2.9 (1.7–4.6) and 1.6 (1.3–2.0) mg/kg i.v.. Moreover, ZK200775 in doses of 10 and 30 mg/kg i.v. reduced muscle tone in genetically spastic rats^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00999284	Visual Acuity	Phase 1	Completed	-	Germany ... more >> Charité Unviversitätsmedizin Berlin, Augenklinik Campus Virchow-Klinikum Berlin, Germany, 13353 Collapse <<

参考文献

[1] Kosowski AR, Cebers G, et al. Nicotine-induced dopamine release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551. Psychopharmacology (Berl). 2004 Aug;175(1):114-23.
[2] Turski L, Huth A, et al. ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10960-5.
[3] Horning MS, Kwon B, Blakemore LJ, et al. Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor subunit expression in rat olfactory bulb. Neurosci Lett. 2004;372(3):230‐234
[4] Turski L, Huth A, Sheardown M, et al. ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma. Proc Natl Acad Sci U S A. 1998;95(18):10960‐10965

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
- 2.4435 mL
- 12.2173 mL
- 24.4347 mL
- 5 mM
- 0.4887 mL
- 2.4435 mL
- 4.8869 mL
- 10 mM
- 0.2443 mL
- 1.2217 mL
- 2.4435 mL

技术信息

CAS号	161605-73-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C14H15F3N3O6P	运输	蓝冰
分子量	409.25	别名	ZK200775;MPQX;ZK200775. 161605-73-8

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Fanapanel Catalog No. CSN17953

靶点选择性

请登录您的专属账户

确认信息