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説明

Amiodarone-d₄ is intended for use as an internal standard for the quantification of amiodarone by GC- or LC-MS. Amiodarone is a class III antiarrhythmic agent, in that it prolongs both cardiac action potential and refractoriness by blocking potassium currents. It inhibits the voltage-gated potassium channel hERG, also known as KCNH2, with an IC₅₀ value of 1 μM. In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid Δ⁸Δ⁷ isomerase, and C-8 sterol isomerase (K_is = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC₅₀s = 0.6 and 0.65 μM, respectively). It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.