产品
编 号:F387098
分子式:C20H26N2O6S
分子量:422.5
产品类型
结构图
CAS No: 549-56-4
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产品详情
生物活性:
Quinidine sulfate is an antiarrhythmic agent. Quinidine sulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine sulfate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine sulfate can be used for malaria research.
体内研究:
Quinidine sulfate is rapidly absorbed, with peak plasma concentrations 60-90 min after an oral dose. Other salts (gluconate, polygalacturonate) are more slowly absorbed, with lower peak concentrations. Quinidine sulfate is approximately 70-90 % bound to plasma proteins. It undergoes hepatic oxidative metabolism to form an N-oxide, a 3-hydroxy form, an O-demethyl form and 2'-quinidinone. Quinidine sulfate inhibits metabolism of amphetamine in rats. Quinidine sulfate pretreatment results in a significant decrease in the excretion of p-hydroxyamphetamine at 24 and 48 h to 7.2 and 24.1% of the vehicle-control levels, respectively, accompanied by a significant increase in amphetamine excretion between 24 and 48 h to 542% of the control.
体外研究:
Quinidine sulfate is an anti-arrythmic drug which affects ionic currents in heart muscle and which has also been shown to be a potent blocker of several classes of K+ channel in a variety of cell types. Bath application of quinidine sulfate causes a dose-dependent reduction of the peak amplitude of Ik. The Kd for blockade of Ik at 0 mV is estimated to be 41 μM.Quinidine sulfate elicits a dose-dependent increase of the rate of the decay of Ik and this effect is enhanced by membrane depolarization. Quinidine sulfate also causes a 5 mV hyperpolarizing shift of the steady-state inactivation curve and increases the half-time for recovery from inactivation. Quinidine sulfate does not affect the onset of inactivation measured at -30 mV.