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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- No. CAS: 851087-60-0
- Fòrmula: C18H17FN4O
- Peso molecular:324.35
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Almacenamiento:
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Chemical Information
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Actividad biológica
ASP5854 (various concentrations; 60 min) potently and selectively binds to human, rat, and mouse adenosine A1 and A2a receptors, with Ki values ranging from 1.24 to 12.48 nM, and exhibits no significant affinity for A3 receptors[2].
ASP5854 displays dual A2A/A1 AR binding affinity with a Ki of 1.76 nM at human A2A AR and 9.03 nM at human A1 AR[1].
ASP5854 (various concentrations; 10 s) acts as a potent functional antagonist of human adenosine A1 and A2a receptors in transfected CHO cells, inhibiting agonist-induced intracellular Ca2+ elevation with IC50 values of 59.81 nM and 4.21 nM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ASP5854 (0.01-3.2 mg/kg; p.o.; single dose) dose-dependently reverses haloperidol-induced catalepsy in mice with an ED50 of 0.066 mg/kg, showing significant efficacy at doses ≥0.1 mg/kg[2].
ASP5854 (0.01-1 mg/kg; p.o.; single dose) reduces haloperidol-induced cataleptic duration in rats, with significant efficacy starting at a dose of 0.1 mg/kg[2].
ASP5854 (0.01-1 mg/kg; p.o.; single dose) significantly potentiates L-DOPA-induced contralateral turning behavior in 6-hydroxydopamine-lesioned hemiparkinsonian rats at doses of 0.032 to 1 mg/kg[2].
ASP5854 (0.032-3.2 mg/kg; p.o.; single dose) reverses scopolamine-induced spontaneous alternation deficits in the mouse Y-maze test, showing significant efficacy at doses of 0.32 and 1 mg/kg[2].
ASP5854 (0.032-1 mg/kg; p.o.; single dose) reverses MK-801-induced spontaneous alternation deficits in the mouse Y-maze test, showing significant efficacy at doses of 0.32 and 1 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, 7 weeks old, intracerebroventricular injection of CGS21680-induced catalepsy)[2]
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Dosage:0.01 mg/kg; 0.032 mg/kg; 0.1 mg/kg; 0.32 mg/kg; 1 mg/kg; 3.2 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently ameliorated CGS21680-induced catalepsy, with an ED50 value of 0.147 mg/kg.
Showed statistically significant effects at doses of 0.32 mg/kg and higher.
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Animal Model:Sprague-Dawley rats (male, 7 weeks old, intraperitoneal injection of haloperidol-induced catalepsy)[2]
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Dosage:0.01 mg/kg; 0.032 mg/kg; 0.1 mg/kg; 0.32 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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Result:Reduced the cataleptic duration, with a minimum effective dose of 0.1 mg/kg.
Showed statistically significant reductions at doses of 0.1 mg/kg and higher.
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Animal Model:Fisher rats (male, 14 weeks old at surgery, stereotaxic unilateral injection of 6-hydroxydopamine-induced hemiparkinsonism, selected based on apomorphine-induced contralateral rotations)[2]
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Dosage:0.01 mg/kg; 0.032 mg/kg; 0.1 mg/kg; 0.32 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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Result:Significantly potentiated L-DOPA-induced contralateral turning behavior at doses of 0.032 to 1 mg/kg.
Minimally induced turning behavior when administered alone.
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Animal Model:Wistar rats (male, 8 weeks old, intraperitoneal injection of scopolamine-induced memory deficits in passive avoidance test)[2]
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Dosage:0.032 mg/kg; 0.1 mg/kg; 0.32 mg/kg; 1 mg/kg; 3.2 mg/kg
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Administration:i.p.; single dose
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Result:Prolonged retention latency in scopolamine-treated rats in a bell-shaped dose-response manner.
Showed statistically significant effects at doses of 0.1 to 3.2 mg/kg.
Chemical Information
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No. CAS 851087-60-0
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Peso molecular 324.35
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Fòrmula C18H17FN4O
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SMILES
O=C1C=CC(C2=NC=C(N)N=C2C3=CC=C(F)C=C3)=CN1C(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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