2258608-78-3

2258608-78-3 structure
2258608-78-3 structure
  • Name: UCM-1306
  • Chemical Name: UCM-1306
  • CAS Number: 2258608-78-3
  • Molecular Formula: C14H14FNO2S
  • Molecular Weight: 279.33
  • Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
  • Create Date: 2023-04-04 16:11:39
  • Modify Date: 2024-04-06 08:52:54
  • 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 not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD)[1].

Name UCM-1306
Description 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 not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD)[1].
Related Catalog
In Vitro 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: Adult C57BL/6J mice with cocaine-induced hyperactivity model[1] 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.
References

[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.  

Molecular Formula C14H14FNO2S
Molecular Weight 279.33
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