851087-60-0
Chemical Structure
ASP5854
- CAS No.: 851087-60-0
- Formula:C18H17FN4O
- Molecular Weight:324.35
IUPAC Name: 5-(5-amino-3-(4-fluorophenyl)pyrazin-2-yl)-1-isopropylpyridin-2(1H)-one
InChIKey: MNUJNGGYFNZUNB-UHFFFAOYSA-N
SMILES: O=C1C=CC(C2=NC=C(N)N=C2C3=CC=C(F)C=C3)=CN1C(C)C
Biological Activity: ASP5854 is an orally active, blood-brain barrier permeable adenosine A1/A2a dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal A2a receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease[1][2][3][4].
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ASP5854 | ASP5854 is an orally active, blood-brain barrier permeable adenosine A1/A2a dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal A2a receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease. | |||||||||||||||||||||
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- [1]. Tang ML, et al. Discovery of Pyridone-Substituted Triazolopyrimidine Dual A2A/A1 AR Antagonists for the Treatment of Ischemic Stroke. ACS Med Chem Lett. 2022;13(3):436-442. Published 2022 Feb 21. [Content Brief]
- [2]. 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 (1 H)-one (ASP5854), in models of Parkinson’s disease and cognition[J]. The journal of pharmacology and experimental therapeutics, 2007, 323(2): 708-719.
- [3]. Brunschweiger A, et al. 8-Benzyltetrahydropyrazino[2,1-f]purinediones: water-soluble tricyclic xanthine derivatives as multitarget drugs for neurodegenerative diseases. ChemMedChem. 2014;9(8):1704-1724. [Content Brief]
- [4]. Mihara T, et al. Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: relationship to anticataleptic effect. J Nucl Med. 2008;49(7):1183-1188. [Content Brief]
Keywords
