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Istradefylline-13C, d3

Istradefylline-13C, d3 is the 13C- and deuterium labeled 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

2749234-46-4

Product Name Alternative

KW-6002-13C, d3

UNSPSC

12352005

Target

Adenosine Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Purity

98.27

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1CC)N(CC)C2=C(N([13C]([2H])([2H])[2H])C(/C=C/C3=CC=C(OC)C(OC)=C3)=N2)C1=O

Molecular Formula

C19 13CH21D3N4O4

Molecular Weight

388.44

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-223.|[2]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.|[3]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.|[4]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.|[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|[6]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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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