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Quinidine

CAS No. : 56-54-2

MCE 站：Quinidine

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

研究领域：Anti-infection

作用靶点：Parasite

In Vitro: Quinidine is a clinical 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 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 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 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. Over one-half of patients starting quinidine stop within the first year of therapy because of side effects. These include, commonly, diarrhea, nausea, and vomiting which are not necessarily related to high plasma concentrations. Quinidine 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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