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。
生物活性 | Quinidine hydrobromide is an antiarrhythmic agent. Quinidine is a potent, orally active, selectivecytochrome P450dbinhibitor. Quinidine hydrobromide is also aK+channelblocker with anIC50of 19.9 μM. Quinidine hydrobromide can be used for malaria research[1][2][3]. |
体外研究 (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[1]. Bath application of quinidine hydrobromide causes a dose-dependent reduction of the peak amplitude of Ik. The Kdfor blockade of Ikat 0 mV is estimated to be 41 μM[1]. Quinidine hydrobromide elicits a dose-dependent increase of the rate of the decay of Ikand 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[1].
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体内研究 (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[2]. 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'-quinidinone[2]. 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[3].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |