產(chǎn)品描述: | ZM-241385是一種高親和力的腺苷A2A受體拮抗劑 |
靶點(diǎn): |
adenosine A2A receptor;AdenosineReceptor |
體外研究: |
ZM 241385對(duì)A2a受體具有高親和力。在大鼠嗜鉻細(xì)胞瘤細(xì)胞膜上,ZM 241385置換NECA(5'-N-ethylcarboxamidoadenosine),pIC50為9.52。ZM241385推遲缺氧去極化的出現(xiàn)(缺氧去極化與細(xì)胞損傷、死亡相關(guān))、避免突觸活性降低、保護(hù)CA1神經(jīng)元和星形膠質(zhì)細(xì)胞,使其免受傷害 |
體內(nèi)研究: |
ZM-241385顯著減弱CCPA和NECA的降壓作用,而不改變它們所誘導(dǎo)的心動(dòng)過緩的現(xiàn)象。它能抑制腺苷受體受體激動(dòng)劑(CCPA和NECA)的心肌保護(hù)作用 |
細(xì)胞實(shí)驗(yàn): |
Cell lines: PC12細(xì)胞 Concentrations: 1 μM Incubation Time: 24 h Method: 細(xì)胞用1 μM CG21680或1 μM ZM241385進(jìn)行24小時(shí)孵育后,將其培養(yǎng)液收集起來,與130 μL dH2O和20μL Griess reagent混合起來。室溫30分鐘后,通過檢測(cè)其中亞硝酸鹽含量,測(cè)定NO的產(chǎn)生量。 |
動(dòng)物實(shí)驗(yàn): |
Animal Models: 成年Sprague-Dawley大鼠 Dosages: 1.5 mg/kg Administration: 靜脈注射 |
參考文獻(xiàn): |
1. Lasley RD, et al. The A2a/A2b receptor antagonist ZM-241385 blocks the cardioprotective effect of adenosine agonist pretreatment in in vivo rat myocardium. Am J Physiol Heart Circ Physiol. 2007, 292(1):H426-31. 2. Wang Z, et al. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385. PLoS One. 2010, 5(11):e13883. 3. S. M. Poucher, et al. The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist. Br J Pharmacol. 1995, 115(6): 1096–1102. 4. Pedata F, et al. Adenosine A2A receptors modulate acute injury and neuroinflammation in brain ischemia. Mediators Inflamm. 2014: 805198. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.964 ml |
14.822 ml |
29.644 ml |
5 mM |
0.593 ml |
2.964 ml |
5.929 ml |
10 mM |
0.296 ml |
1.482 ml |
2.964 ml |
50 mM |
0.059 ml |
0.296 ml |
0.593 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。 |