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Nifekalant hydrochloride

CAS No. : 130656-51-8

MCE 站：Nifekalant hydrochloride

产品活性：Nifekalant hydrochloride (MS-551) ，一种 III 类抗心律不齐化合物，是 IKr 钾通道阻滞剂，IC₅₀ 为10 ?M。Nifekalant hydrochloride 可用于快速室上性心律失常的研究。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: Nifekalant interacts with the cardiac M2 and the peripheral M3 receptors with a K_i value of 27 and 74 mM, respectively. Nifekalant dose dependently blocks HERG channels with an IC₅₀ value of 7.9 mM, but Nifekalant does not block minK currents in the Xenopus oocyte expression system. Nifekalant blocks HERG channels mainly in their open state in a frequency dependent manner. As a pure K⁺ channel blocker, Nifekalant does not have negative inotropic effects which amiodarone has via a β-blocking action and does not affect cardiac conduction.

In Vivo: In rats (a species deficient in functional cardiac IK), before coronary ligation, 3 mg/kg and 10 mg/kg MS-551 decreased the heart rate by 6% and 12%, and increased mean arterial pressure (MAP) by 14% and 33%, respectively. MS-551 prolongs the QT interval and reduced the incidence of sustained ventricular fibrillation (VF) after reperfusion.

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