Description
Amiodarone-d
4 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 IC
50 value of 1 μM. In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid Δ
8Δ
7 isomerase, and C-8 sterol isomerase (K
is = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC
50s = 0.6 and 0.65 μM, respectively). It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4
in vitro at low micromolar concentrations.
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.
