Клофилиум

Description

Clofilium is a quaternary ammonium compound of the benzenebutanaminium series, an experimental class III antiarrhythmic drug, CAS 68379-02-2. The supplier's source data for this item does not contain a detailed dump of physicochemical and regulatory attributes - the information below is collected from open scientific sources by CAS number and English name.

Basic Attributes

• CAS No: 68379-02-2
• Chemical formula: C21H37ClN
• English name: Clofilium
• Synonyms: 4-chloro-N,N-diethyl-N-heptylbenzenebutanaminium (4-Chloro-N,N-diethyl-N-heptylbenzenebutanaminium)

Physico-chemical characteristics

The values ​​of molecular weight, melting and boiling points, density and solubility in the supplier’s passport data and in freely available databases are not given in a sufficiently verified form and are not indicated here in order to avoid entering unreliable values.

Mechanism of action

Clofilium selectively increases the refractoriness of myocardial cells by prolonging the duration of the action potential - a classic effect of a class III antiarrhythmic drug. Blocks various delayed rectifier K+ potassium channels in micromolar concentrations, including the rapidly activated IK current component (sensitive to E-4031, i.e. associated with HERG channels), reversibly reduces L-type calcium current and suppresses sodium current by a voltage-dependent mechanism. In relation to HERG channels, it exhibits voltage-dependent blockade with an IC50 of the order of 150–250 nM.

Scope of application

It was used in experimental cardiology and pharmacological studies as a model compound for studying the electrophysiological effects of class III antiarrhythmic drugs, including for studying the proarrhythmic potential (prolongation of the QT interval, development of ventricular arrhythmias) in experimental models on an isolated heart. It has not entered clinical practice as an independent drug; used primarily as a research reagent.

Storage and transportation

No special storage conditions, UN transport codes or hazard statements are provided in available sources; As a research reagent, it is recommended to store it in a dry, cool place, protected from light, in a tightly closed container according to the general rules for handling organic ammonium compounds.

Clinical significance and future developments

Clofilium belongs to a group of compounds studied in the 1980s and 1990s as part of the search for selective class III potassium channel blockers, work that subsequently contributed to the development of a number of clinically used antiarrhythmic drugs. The proarrhythmogenic potential demonstrated by Clofilium (the risk of prolongation of the QT interval and the development of torsade de pointes) has become an important example in formulating the requirements for the electrophysiological safety of new class III drugs at the preclinical stage of development.