Description
Nifekalant is a novel and pure class III anti-arrhythmic agent introduced
in Japan as Shinbit injection for the treatment of serious ventricular arrhythmias.
It can be synthesized in 3 steps with a final assembly of two ethanolamine
blocks. Nifekalant is a non-selective blocker of myocardial repolarizing
potassium currents and is completely devoid of any β-adrenergic blocking effect .
In hearts from different species, Nifekalant significantly prolonged action
potential duration, atrial and ventricular refractory periods in in situ and in
isolation studies. In intact animals, hemodynamic parameters were not affected
by doses up to 1 mg/kg. The specific characteristics of its voltage- and timedependent
K+ current blockade might differentiate Nifekalant from other class III
agents currently in use.
Description
Nifekalant is a class III antiarrhythmic agent that has been shown to be beneficial to initial resuscitation after cardiac arrest in clinical trials. It blocks the rapidly activating delayed rectifier potassium channel (I
Kr; IC
50 = 10 μM). Nifekalant is also inhibits the human multidrug and toxin extrusion (MATE) transporter 1 (MATE1; IC
50 = 6.5 μM).
Chemical Properties
Yellow Solid
Originator
Mitsui (Japan)
Uses
Nifekalant Hydrochloride is a class III antiarrhythmic agent. Nifekalant Hydrochloride is used in the treatment of patients with extensive anterior infarction and severe ventricular dysfunction.
Definition
ChEBI: Nifekalant hydrochloride is an amine. It contains a Nifekalant.
