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Quinine hydrobromide
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Quinine hydrobromide
CAS No. : 549-49-5
MCE 站:Quinine hydrobromide
产品活性:Quinidine hydrobromide 是一种抗心律失常剂。Quinidine hydrobromide 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 hydrobromide 也可用作疟疾的研究。
研究领域:Anti-infection | Metabolic Enzyme/Protease | Membrane Transporter/Ion Channel
作用靶点:Parasite | Cytochrome P450 | Potassium Channel
In Vitro: Quinidine hydrobromide 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 hydrobromide 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 hydrobromide elicits a dose-dependent increase of the rate of the decay of Ik 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 hydrobromide does not affect the onset of inactivation measured at -30 mV.
In Vivo: Quinidine hydrobromide 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 hydrobromide 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 hydrobromide inhibits metabolism of amphetamine in rats. Quinidine hydrobromide 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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