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Istradefylline
- KW6002- Soluble in DMSO
- MF: C20H24N4O4
- MW: 384.43
Description
Istradefylline is a potent, selective and orally active adenosine A2A receptor antagonist used to reduce A2A-mediated inhibition of dopaminergic motor signaling.
A2A receptors are highly expressed in the striatum and functionally oppose dopamine D2 receptor pathways. Istradefylline is a clinically validated reference for Parkinson disease, basal-ganglia circuitry and adenosine–dopamine receptor interactions.
Key Features
- Selective adenosine A2A receptor antagonist
- Orally active CNS pharmacology
- Enhances dopaminergic motor-pathway output
- Clinically validated Parkinson disease mechanism
Applications
- A2A receptor binding and functional assays
- Parkinson disease and motor-circuit research
- Adenosine–dopamine receptor interaction studies
- Basal ganglia and striatal signaling models
More Information
| Parent CAS No. | 155270-99-8 |
|---|---|
| Chemical Name | (E)-8-(3,4-Dimethoxystyryl)-1,3-diethyl-7-methyl-1H-purine-2,6(3H,7H)-dione |
| SMILES | C1(=O)N(CC)C(=O)N(CC)C2N=C(/C=C/C3C=C(OC)C(OC)=CC=3)N(C)C1=2 |
| MFCD | MFCD00928421 |
| InChi | InChI=1S/C20H24N4O4/c1-6-23-18-17(19(25)24(7-2)20(23)26)22(3)16(21-18)11-9-13-8-10-14(27-4)15(12-13)28-5/h8-12H,6-7H2,1-5H3/b11-9+ |
| InChiKey | IQVRBWUUXZMOPW-PKNBQFBNSA-N |
| CID | 5311037 |
| Short Description | A2A antagonist |
References
- S Shiozaki et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999, 147(1), 90-95.
- TN Chase et al. Translating A2A antagonist KW6002 from animal models to parkinsonian patients. Neurology 2003, 61(11 Suppl 6), S107-11.
- PA LeWitt et al. Adenosine A2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson's disease: a double-blind, randomized, multicenter clinical trial (6002-US-005). Ann. Neurol. 2008, 63(3), 295-302.
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