| 產(chǎn)品描述： | CFM-2 is a potent and selective non-competitive AMPAR antagonist. CFM-2 possesses anticonvulsant activity in various models of seizures |
| 靶點(diǎn)： |
AMPA Receptor;iGluR |
| 體內(nèi)研究： |
Pretreatment with CFM-2 delays the progression of seizure rank during repeated administration of pentylentetrazole. At the end of the period of repeated pentylentetrazole treatment (6 weeks) the mean seizure score was 0 in vehicle treated controls, 4.3 in animals treated with vehicle + pentylentetrazole, 2.2 in rats treated chronically with CFM-2 (20 μmol/kg; i.p.) + pentylentetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 μmol/kg; i.p.) + pentylenetetrazole. CFM-2 is also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylentetrazole-kindled animals. Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50μg), significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affects the contralateral basal responses to thermal and mechanical stimuli |
| 參考文獻(xiàn)： |
1. De Sarro G, et al. Effects of some AMPA receptor antagonists on the development of tolerance in epilepsy-prone rats and in pentylenetetrazole kindled rats. Eur J Pharmacol. 1999 Mar 5;368(2-3):149-59. 2. Rizzo M, et al. Determination of new 2,3-benzodiazepines in rat plasma using high-performance liquid chromatography with ultraviolet detection. J Chromatogr B Biomed Sci Appl. 1999 Aug 20;731(2):207-15. 3. Stepulak A, et al. AMPA antagonists inhibit the extracellular signal regulated kinase pathway and suppress lung cancer growth. Cancer Biol Ther. 2007 Dec;6(12):1908-15. 4. Park JS, et al. Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in complete Freund's adjuvant-induced inflammatory pain. Mol Pain. 2008 Dec 30;4:67. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.212 ml |
16.06 ml |
32.119 ml |
| 5 mM |
0.642 ml |
3.212 ml |
6.424 ml |
| 10 mM |
0.321 ml |
1.606 ml |
3.212 ml |
| 50 mM |
0.064 ml |
0.321 ml |
0.642 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京