- ￥119 - 3717
- AmBeed
- A791038
- 2026年07月23日
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- 详细信息
- 文献和实验
- 技术资料
- 英文名：
(E)-8-(3,4-Dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione
- 供应商：
上海安毕达生物科技有限公司
- CAS号：
155270-99-8
- 规格：
50μL/1mL/1mg/5mg/10mg/25mg/50mg/100mg/250mg/500mg
| 规格： | 50μL | 产品价格： | ￥119.0 |
|---|---|---|---|
| 规格： | 1mL | 产品价格： | ￥508.0 |
| 规格： | 1mg | 产品价格： | ￥130.0 |
| 规格： | 5mg | 产品价格： | ￥260.0 |
| 规格： | 10mg | 产品价格： | ￥416.0 |
| 规格： | 25mg | 产品价格： | ￥739.0 |
| 规格： | 50mg | 产品价格： | ￥976.0 |
| 规格： | 100mg | 产品价格： | ￥1410.0 |
| 规格： | 250mg | 产品价格： | ￥2031.0 |
| 规格： | 500mg | 产品价格： | ￥3717.0 |
A2A receptor (A2AR) with Ki of 2.2 nM. The affinity of it for the A2AR is 70-fold greater than that for the A1 receptor 11. Istradefylline binds to A1R, A2AR, and A3R in human with Kis of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1R and A2AR in rat, 105.02 nM and 1.87 nM for A1R and A2AR in mouse, respectively 6. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes 7. The ED50s of istradefylline in the reversal of CGS21680-induced and reserpine-induced catalepsy were 0.05 mg/kg, PO and 0.26 mg/kg, PO, respectively. Compared to the ED50 of other adenosine antagonists and dopamine agonist drugs, istradefylline is over 10 times as potent in these models. Istradefylline also ameliorated the hypolocomotion (minimum effective dose; 0.16 mg/kg) induced by nigral dopaminergic dysfunction with MPTP or reserpine treatment. Combined administrations of subthreshold doses of istradefylline and L-dopa (50 mg/kg, PO) exerted prominent effects on haloperidol-induced and reserpine-induced catalepsy, suggesting that there may be a synergism between the adenosine A2AR antagonist istradefylline and dopaminergic agents 8. Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later 9. Oral administration of istradefylline protected against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats. It also prevented the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP in mice 10.
溶解方案(细胞实验)
DMSO 中的溶解度 : 25.33 mg/mL (65.89 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)
溶解方案(动物实验)
"方案 一": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (5.41 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"
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文献和实验Kanda T, Jackson MJ, et al. Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol. 2000 Apr;162(2):321-7.
Yamada K, Kobayashi M, et al. Antidepressant-like activity of the adenosine A(2A) receptor antagonist, istradefylline (KW-6002), in the forced swim test and the tail suspension test in rodents. Pharmacol Biochem Behav. 2013 Dec;114-115:23-30.
Uchida S, Soshiroda K, et al. The adenosine A2A receptor antagonist, istradefylline enhances anti-parkinsonian activity induced by combined treatment with low doses of L-DOPA and dopamine agonists in MPTP-treated common marmosets. Eur J Pharmacol. 2015 Nov 5;766:25-30.
KW-6002
Mihara T. Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson's disease and cognition. J Pharmacol Exp Ther. 2007 Nov;323(2):708-19.
Brambilla R. Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in rat striatal primary astrocytes. Glia. 2003 Aug;43(2):190-4.
Shiozaki S. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999 Nov;147(1):90-5.
Chen JF. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001 May 15;21(10)
Ikeda K. Neuroprotection by adenosine A2A receptor blockade in experimental models of Parkinson's disease. J Neurochem. 2002 Jan;80(2):262-70. doi: 10.1046/j.0022-3042.2001.00694.x.
Chen JF, Xu K, Petzer JP, Staal R, Xu YH, Beilstein M, Sonsalla PK, Castagnoli K, Castagnoli N Jr, Schwarzschild MA. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001 May 15;21(10):RC143. doi: 10.1523/JNEUROSCI.21-10-j0001.2001. PMID: 11319241; PMCID: PMC6762498.
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