MSX3
MSX3 is an orally active, selective A2a adenosine receptor antagonist and a prodrug of MSX2 (HY-117184). MSX3 reduces hyperphosphorylation of Tau at specific epitopes in mice without altering total Tau levels, Tau fragments, or Tau aggregation in these animals. MSX3 enhances spatial memory. MSX3 regulates effort-related decision-making behaviors. MSX3 reverses D2 antagonist-induced suppression of lever pressing, increased Chow feed intake, reduced selection of high-barrier arms, and prolonged response latency, and also slightly attenuates effects induced by D1 antagonists. MSX3 can be used in the research of Tauopathies (Alzheimer's disease-related), depression, and Parkinsonism.
For research use only. We do not sell to patients.
- CAS No.: 261717-23-1
- Formula: C21H21N4Na2O7P
- Molecular Weight:518.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
A2AR |
In Vivo
MSX3 (i.p.; single administration; 20 min before testing; 0.75-3.0 mg/kg) dose-dependently reverses Haloperidol (HY-14538)-induced impairments in effort-related choice and response latency in rats, with the 3.0 mg/kg dose fully restoring T-maze performance to the level of the vehicle control group; administration of the 3.0 mg/kg dose alone exerts no significant effect on T-maze performance[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl6/J THY-Tau22 (male, 6 months of age at treatment initiation, Alzheimer's disease tauopathy model)[1]
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Dosage:0.3 g/l; 1.4 mg per mouse daily
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Administration:p.o.; daily
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Result:Increased Y-maze discrimination index significantly relative to water-treated THY-Tau22 mice (P = 0.05, one-way ANOVA) and normalized to wild-type levels.
Reduced acidic Tau isovariants, indicating decreased global Tau phosphorylation.
Reduced Tau phosphorylation at Ser262 (P < 0.01), Ser404 (P < 0.05), and Ser214 (P < 0.05) relative to water-treated THY-Tau22 mice.
Left total Tau protein levels, Tau proteolytic fragments, and sarkosyl-insoluble Tau unchanged.
Showed no significant differences in body weight gain or body temperature relative to water-treated groups.
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Animal Model:Sprague-Dawley (adult male, drug-naive, 290-340 g at study start, food-deprived to 85% free-feeding body weight, psychomotor/motivational impairment induced via i.p. haloperidol)[3]
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Dosage:0.75 mg/kg (co-administered with haloperidol); 1.5 mg/kg (co-administered with haloperidol); 3.0 mg/kg (co-administered with haloperidol); 3.0 mg/kg (administered alone)
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Administration:i.p.; single dose; 20 min before testing
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Result:Produced a dose-related increase in selection of the high-density barrier arm relative to haloperidol plus vehicle-treated rats (p<0.01).
Completely reversed haloperidol-induced reduction in high-density arm selection at 3.0 mg/kg, with rats choosing the barrier arm at levels equivalent to vehicle control.
Reduced haloperidol-induced increased response latency significantly at 0.75 mg/kg (p<0.001) and at 1.5 and 3.0 mg/kg (p<0.05) relative to haloperidol plus vehicle.
Showed no significant effect on high-density arm selections (mean 28.6 vs. vehicle mean 28.0; t=-1.0, df=4, n.s.) when administered alone at 3.0 mg/kg.
Showed no significant effect on average run latency (mean 3.33 vs. vehicle mean 3.67; t=2.4, df=4, n.s.) when administered alone at 3.0 mg/kg.
Chemical Information
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CAS No. 261717-23-1
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Molecular Weight 518.37
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Formula C21H21N4Na2O7P
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SMILES
O=C(N1CC#C)N(CCCOP(O[Na])(O[Na])=O)C2=C(N(C)C(/C=C/C3=CC=CC(OC)=C3)=N2)C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Protocol for Water Maze
The Morris Water Maze is a rodent spatial learning and memory assay in which a mouse or rat swims in opaque water to find an escape platform; in the hidden-platform version, the animal cannot see the platform and must use distal extra-maze cues to learn its fixed spatial location. The assay primarily measures hippocampus-dependent spatial learning during acquisition trials and spatial reference memory during probe trials after platform removal; readouts include escape latency, swim path length, swim speed, quadrant occupancy, platform-site crossings, and proximity to the former platform location.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
[1]. Laurent C, et al. A2A adenosine receptor deletion is protective in a mouse model of Tauopathy. Molecular psychiatry. 2016 Jan;21(1):97-107. [Content Brief]
[2]. Worden LT, et al. The adenosine A2A antagonist MSX-3 reverses the effort-related effects of dopamine blockade: differential interaction with D1 and D2 family antagonists. Psychopharmacology. 2009 Apr;203(3):489-99. [Content Brief]
[3]. Mott AM, et al. The adenosine A2A antagonist MSX-3 reverses the effects of the dopamine antagonist haloperidol on effort-related decision making in a T-maze cost/benefit procedure. Psychopharmacology. 2009 May;204(1):103-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MSX3 Related Classifications
HY-102086 Related Classifications
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