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Submit ReviewIstradefylline is a potent and selective adenosine A2A receptor antagonist (Ki values are 2.2 and 150 nM for A2A and A1 receptors respectively). Anticataleptic and antiparkinson agent; reverses drug-induced motor dysfunction in animal models.
分子量 | 384.43 |
公式 | C20H24N4O4 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 155270-99-8 |
PubChem ID | 5311037 |
InChI Key | IQVRBWUUXZMOPW-PKNBQFBNSA-N |
Smiles | O=C1N(CC)C(C(N(C)C(/C=C/C3=CC(OC)=C(OC)C=C3)=N2)=C2N1CC)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 7.69 | 20 |
以下数据基于产品分子量 384.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 13.01 mL | 65.03 mL | 130.06 mL |
1 mM | 2.6 mL | 13.01 mL | 26.01 mL |
2 mM | 1.3 mL | 6.5 mL | 13.01 mL |
10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
参考文献是支持产品生物活性的出版物。
Shimada et al (1997) Adenosine A2A antagonists with potent anti-cataleptic activity. Bioorg.Med.Chem.Lett. 7 2349
Kanda et al (1998) Adenosine A2A receptors modify motor function in MPTP-treated common marmosets. Neuroreport 9 2857 PMID: 9760134
Shiozaki et al (1999) Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by rese. or MPTP. Psychopharmacology 147 90 PMID: 10591873
If you know of a relevant reference for Istradefylline, please let us know.
关键词: Istradefylline, Istradefylline supplier, Potent, selective, Adenosine, A2A, receptor, antagonists, KW-6002, KW6002, AA2AR, antiparkinsons, activity, antiparkinsonian, anticataleptics, Receptors, 5147, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Istradefylline 的部分引用包括:
John M et al (2021) Cannabis sativa terpenes are cannabimimetic and selectively enhance cannabinoid activity. Sci Rep 11 8232 PMID: 33859287
Cheng et al (2017) Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity. Structure 25 1275 PMID: 28712806
Orr et al (2018) Istradefylline reduces memory deficits in aging mice with amyloid pathology. Neurobiol Dis 110 29 PMID: 29100987
Wydra et al (2015) On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats. PLoS One 232 1767 PMID: 25420611
您是否知道使用了 Tocris Istradefylline 的优秀论文? 请告知我们.
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Istradefylline from Tocris worked wonderfully. At 3 mg/kg (in suspension in 8% Tween 80 in 0.9% saline), it reversed motor impairment induced by 0.16 mg/kg of the D2R antagonist eticlopride
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.