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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).
In Vitro
UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl; 1-10 μM) increases cAMP in a concentration-response manner with high potency (EC 50 =60 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl; 5 mg/kg; p.o.; C57BL/6J mice) has good brain penetration and oral availability. Plasma concentration can be quantified for up to 8 h with T max at 0.5 h . UCM-1306 (1 mg/kg; ip) enhances cocaine-induced hyperlocomotion in adult mice . UCM-1306 (1 mg/kg; ip) helps consolidate long-term memory formation . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult C57BL/6J mice with cocaine-induced hyperactivity model Dosage: 1 mg/kg; cocaine (20 mg/kg, sc) Administration: Intraperitoneal injection Result: Increased cocaine-induced hyperlocomotion, suggesting an in vivo potentiation of DA action at the D1R. Animal Model: Adult C57BL/6J mice Dosage: 1 mg/kg Administration: Intraperitoneal injection Result: Increased memory trace in C57BL/6J mice.
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