Synonyms: KW-6002 | KW6002 | Nourianz®
istradefylline is an approved drug (Japan (2013), FDA (2019))
Compound class:
Synthetic organic
Comment: Istradefylline is a high affinity, selective adenosine A2A receptor antagonist. Chemically it is a caffeine analogue. Istradefylline was developed to treat adult Parkinson's disease patients experiencing "OFF" episodes, as an adjunct to levodopa/carbidopa therapy.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
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2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem, 50 (4): 828-34. [PMID:17300165] |
2. Dungo R, Deeks ED. (2013)
Istradefylline: first global approval. Drugs, 73 (8): 875-82. [PMID:23700273] |
3. Fredholm BB, IJzerman AP, Jacobson KA, Linden J, Müller CE. (2011)
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacol Rev, 63 (1): 1-34. [PMID:21303899] |
4. Pretorius J, Malan SF, Castagnoli N, Bergh JJ, Petzer JP. (2008)
Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues. Bioorg Med Chem, 16 (18): 8676-84. [PMID:18723354] |
5. Shimada J, Koike N Nonaka H, Shiozaki S, Yanagawa K, Kanda T, Kobayashi H, Ichimura M, Nakamura J, Kase H et al.. (1997)
Adenosine A2A antagonists with potent anti-cataleptic activity. Bioorg Med Chem Lett, (7): 2349-2352. |