Istradefylline
Istradefylline is a competitive inhibitor of adenosine A2A receptors that exhibits tremorlytic activity. Istradefylline is currently under examination as a potential treatment for Parkinson’s disease, as it decreases “off” time in subjects with Parkinson’s disease without worsening dyskinesia. Istradefylline increases dopamine levels in normal and 6-OHDA-lesioned animal models, improving cognitive performance. In other animal models, istradefylline decreases GABA release and elicits conditioned place preference (CPP) and increases locomotor activity, indicating a potential role for adenosine receptors in reward and reinforcement.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18935759
| Cas No. |
155270-99-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C20H24N4O4 |
| Formula Wt. |
384.43 |
| Chemical Name |
(E)-8-(3,4-Dimethoxystyryl)-1,3-diethyl-7-methylxanthine |
| IUPAC Name |
8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione |
| Synonym |
8-[(1E)-2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione, KW-6002 |
| Appearance |
White to off white powder |
Kadowaki Horita T, Kobayashi M, Mori A, et al. Effects of the adenosine A2A antagonist istradefylline on cognitive performance in rats with a 6-OHDA lesion in prefrontal cortex. Psychopharmacology (Berl). 2013 Dec;230(3):345-52. PMID: 23748382.
Saki M, Yamada K, Koshimura E, et al. In vitro pharmacological profile of the A2A receptor antagonist istradefylline. Naunyn Schmiedebergs Arch Pharmacol. 2013 Nov;386(11):963-72. PMID: 23812646.
Mizuno Y, Hasegawa K, Kondo T, et al. Clinical efficacy of istradefylline (KW-6002) in Parkinsons disease: a randomized, controlled study. Mov Disord. 2010 Jul 30;25(10):1437-43. PMID: 20629136.
Salamone JD, Betz AJ, Ishiwari K, et al. Tremorolytic effects of adenosine A2A antagonists: implications for parkinsonism. Front Biosci. 2008 May 1;13:3594-605. PMID: 18508458.
Harper LK, Beckett SR, Marsden CA, et al. Effects of the A 2A adenosine receptor antagonist KW6002 in the nucleus accumbens in vitro and in vivo. Pharmacol Biochem Behav. 2006 Jan;83(1):114-21. PMID: 16451807.
