产品
编 号:F741475
分子式:C14H14FNO2S
分子量:279.33
产品类型
结构图
CAS No: 2258608-78-3
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生物活性:
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).
体内研究:
UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl; 5 mg/kg; p.o.; C57BL/6J 小鼠) 具有良好的脑穿透性和口服可用性。血浆浓度可在 8 小时内定量,Tmax 为 0.5 小时。UCM-1306 (1 mg/kg; ip) 增强成年小鼠可卡因诱导的过度运动。UCM-1306 (1 mg/kg; ip) 有助于巩固长期记忆的形成。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.
体外研究:
UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl; 1-10 μM) 以浓度-响应的方式增强 cAMP,且 EC50=60 nM。