| Chemical Properties | Back Directory | [Boiling point ]
377.5±52.0 °C(Predicted) | [density ]
1.21±0.1 g/cm3(Predicted) | [solubility ]
DMSO: 2 mg/mL, clear (Warmed) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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 Tmax at 0.5 h[1].
UCM-1306 (1 mg/kg; ip) enhances cocaine-induced hyperlocomotion in adult mice[1].
UCM-1306 (1 mg/kg; ip) helps consolidate long-term memory formation[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. DOI:10.1021/acs.jmedchem.2c00949 |
|
|