Istradefylline

Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

Product Specifications

CAS Number

[155270-99-8]

Product Name Alternative

KW-6002

UNSPSC

12352005

Hazard Statement

H301

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Istradefylline.html

Purity

99.89

Solubility

DMSO : 25.33 mg/mL (ultrasonic; warming)

Smiles

O=C1C2=C(N=C(/C=C/C3=CC(OC)=C(OC)C=C3)N2C)N(CC)C(N1CC)=O

Molecular Formula

C20H24N4O4

Molecular Weight

384.43

Precautions

H301

References & Citations

[1]Chen JF, et al. Neuroprotection by caffeine and A (2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001 May 15;21 (10) :RC143.|[2]Shiozaki S, et al. 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.|[3]Kanda T, 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.|[4]Brambilla R, et al. 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.|[5]Mihara T, et al. 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 Pharm