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Quinine sulfate

CAS No. : 549-56-4

MCE 站：Quinine sulfate

产品活性：Quinidine sulfate 是一种抗心律失常剂。Quinidine sulfate 是一种有效的、具有口服活性的、选择性的细胞色素 P450db (cytochrome P450db) 抑制剂，也是 K⁺ 通道 (K⁺ channel) 的有效阻断剂，其 IC₅₀ 值为 19.9 μM。Quinidine sulfate 也可用作疟疾的研究。

研究领域：Anti-infection  |  Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease

作用靶点：Parasite  |  Potassium Channel  |  Cytochrome P450

In Vitro: 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 I_k. The K_d for blockade of I_k at 0 mV is estimated to be 41 μM.
Quinidine sulfate elicits a dose-dependent increase of the rate of the decay of I_k ａnd this effect is enhanced by membrane depolarization. Quinidine also causes a 5 mV hyperpolarizing shift of the steady-state inactivation curve ａnd increases the half-time for recovery from inactivation. Quinidine does not affect the onset of inactivation measured at -30 mV.

In Vivo: 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＇-quinidi.
Quinidine sulfate inhibits metabolism of amphetamine in rats. Quinidine 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.

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