Amiodarone-D4 HCl

Description

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.

The Uses of Amiodarone-D4 HCl

A Labelled non-selective ion channel blocker. Antiarrhythmic (class III).

General Description

A Certified Spiking Solution^?and stable-labeled internal standard for use in therapeutic drug monitoring analyses by LC/MS. Amiodarone, an antiarrhythmic agent marketed as Pacerone^?, Cordarone^?, Aratac, Atlansil, is monitored by clinical labs to ensure patients remain within the drug′s therapeutic range.