您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Fanapanel hydrate
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:
 
Fanapanel hydrate
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。
Fanapanel hydrate图片
CAS NO:1255517-78-2
规格:98%
分子量:427.27
包装与价格:
包装价格(元)
100mg电议
200mg电议
10mg电议
50mg电议

产品介绍
Fanapanel hydrate (ZK200775 hydrate) 是高选择性AMPA拮抗剂。
CAS:1255517-78-2
分子式:C14H17F3N3O7P
分子量:427.27
纯度:98%
存储:Store at -20°C

Background:

Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. AMPAR


In the cortical slice preparation assay, ZK200775 gave Ki 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 [1].


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., whereas the threshold for NMDA-induced seizures was elevated only in doses, THRD50 of 24.1 (21.9-26.5) mg/kg i.v., which affected motor coordination in the rotating rod, ED50 14.6 (12.1-17.6) mg/kg. ZK200775 in doses of 10 and 30 mg/kg i.v. reduced muscle tone in genetically spastic rats [1]. ZK200775 (3.0 but not 1.5 or 6.0 mg/kg) significantly decreased the nicotine-induced (0.6 mg/kg) DA release in the NAcc and nicotine-stimulated LMA. ZK200775 (1.5, 3.0, 6.0 mg/kg) alone influenced neither DA release nor LMA. ZK200775 showed 34-fold selectivity for AMPA receptors compared to NMDA receptors and no affinity to nicotine receptors [2].


[1]. Turski L, 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. [2]. Kosowski AR, 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.