Istradefylline
This adenosine A2A receptor antagonist is used as an add-on therapy in adults with Parkinson's disease experiencing wearing-off episodes with levodopa treatment. It reduces the time patients spend in an "off" state (with return of Parkinson's symptoms) by modulating dopaminergic signaling through the indirect pathway of the basal ganglia. It is the first drug in its class approved for Parkinson's disease in the United States.
Masse moléculaire
384,4000 g/mol
LogP
2,50
TPSA
76,90 Ų
Règle des 5 de Lipinski
Conforme
Aires thérapeutiques
Mécanisme d'action
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Structure 2D
Cite this structure
Embed this structure
SMILES
CCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CC)c1=O
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+
Molecular Formula
C20H24N4O4
HBD / HBA
- / 5
Liaisons Rotatives
6
Atomes Lourds
28
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Foire aux questions
This adenosine A2A receptor antagonist is used as an add-on therapy in adults with Parkinson's disease experiencing wearing-off episodes with levodopa treatment. It reduces the time patients spend in an "off" state (with return of Parkinson's symptoms) by modulating dopaminergic signaling through the indirect pathway of the basal ganglia. It is the first drug in its class approved for Parkinson's disease in the United States.
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Yes, Istradefylline is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL431770. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 5311037. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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