产品
编 号：F756857
分子式：C18H23ClN4O2
分子量：362.85
分子式：C18H23ClN4O2
分子量：362.85
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CAS No: 2919851-73-1
产品详情
生物活性：
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease.
体内研究：
CVN417 (3 mg/kg, 10 mg/kg, 25 mg/kg; 口服) 大鼠震颤模型中震颤下颌运动持续时间呈剂量依赖性减少。在大鼠中对 CVN417 的药代动力学分析RouteDose (mg/kg)Cl (mL/min/kg)Vdss (L/kg)AUC0-∞ (ng·h/mL)Cmax (μM)F (%)T1/2 (h)Cbrain,total (2 h)Kp, Kpu/u
i.v.0.538.212.3205
p.o.100.35775115.91.824.1, 1.4
体外研究：
CVN417 (10 μM; 0-2 h) 在人肝微粒或肝细胞中表现出较低的代谢周转特性。CVN417 的体外 ADME 数据humanratmousedog
liver microsomes Clint (μL/min/mg)2.831.233.327.7
hepatocytes (mL/min/106 cells)3.720.825.132.3
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease.
体内研究：
CVN417 (3 mg/kg, 10 mg/kg, 25 mg/kg; 口服) 大鼠震颤模型中震颤下颌运动持续时间呈剂量依赖性减少。在大鼠中对 CVN417 的药代动力学分析RouteDose (mg/kg)Cl (mL/min/kg)Vdss (L/kg)AUC0-∞ (ng·h/mL)Cmax (μM)F (%)T1/2 (h)Cbrain,total (2 h)Kp, Kpu/u
i.v.0.538.212.3205
p.o.100.35775115.91.824.1, 1.4
体外研究：
CVN417 (10 μM; 0-2 h) 在人肝微粒或肝细胞中表现出较低的代谢周转特性。CVN417 的体外 ADME 数据humanratmousedog
liver microsomes Clint (μL/min/mg)2.831.233.327.7
hepatocytes (mL/min/106 cells)3.720.825.132.3
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