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.
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- CAS 番号: 261717-23-1
- 分子式: C21H21N4Na2O7P
- 分子量:518.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Adenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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A2AR |
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.
化学情報
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CAS 番号 261717-23-1
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分子量 518.37
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MSX3 関連分類
HY-102086 関連分類
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