| Bioactivity | 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)[1]. | |||||||||
| Invitro | 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。 | |||||||||
| In Vivo | 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[1]。UCM-1306 (1 mg/kg; ip) 增强成年小鼠可卡因诱导的过度运动[1]。UCM-1306 (1 mg/kg; ip) 有助于巩固长期记忆的形成[1]。 Animal Model: | |||||||||
| Name | UCM-1306 | |||||||||
| CAS | 2258608-78-3 | |||||||||
| Formula | C14H14FNO2S | |||||||||
| Molar Mass | 279.33 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. García-Cárceles J, et, al. 2-(Fluoromethoxy)-4'-(S-methanesulfonimidoyl)-1,1'-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D1 Receptor for Parkinson's Disease. J Med Chem. 2022 Sep 22;65(18):12256-12272. |
UCM-1306
CAS: 2258608-78-3 F: C14H14FNO2S W: 279.33
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the end
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