A transient outward potassium current activator recapitulates the electrocardiographic manifestations of Brugada syndrome was written by Calloe, Kirstine;Cordeiro, Jonathan M.;Di Diego, Jose M.;Hansen, Rie S.;Grunnet, Morten;Olesen, Soren Peter;Antzelevitch, Charles. And the article was included in Cardiovascular Research in 2009.Computed Properties of C7H4Br2N2 This article mentions the following:
Aims: Transient outward potassium current (Ito) is thought to be central to the pathogenesis of the Brugada syndrome (BrS). However, an Ito activator has not been available with which to validate this hypothesis. Here, we provide a direct test of the hypothesis using a novel Ito activator, NS 5806 (I). Methods and results: Isolated canine ventricular myocytes and coronary-perfused wedge preparations were used. Whole-cell patch-clamp studies showed that I (10 μM) increased peak Ito at +40 mV by 79 ± 4% (24.5 ± 2.2 to 43.6 ± 3.4 pA/pF, n = 7) and slowed the time constant of inactivation from 12.6 ± 3.2 to 20.3 ± 2.9 ms (n = 7). The total charge carried by Ito increased by 186% (from 363.9 ± 40.0 to 1042.0 ± 103.5 pA·ms/pF, n = 7). In ventricular wedge preparations, I increased phase 1 and notch amplitude of the action potential in the epicardium, but not in the endocardium, and accentuated the ECG J-wave, leading to the development of phase 2 re-entry and polymorphic ventricular tachycardia (n = 9). Although sodium and calcium channel blockers are capable of inducing BrS only in right ventricular (RV) wedge preparations, the Ito activator was able to induce the phenotype in wedges from both ventricles. I induced BrS in 4/6 right and 2/10 left ventricular wedge preparations Conclusion: The Ito activator I recapitulates the electrog. and arrhythmic manifestation of BrS, providing evidence in support of its pivotal role in the genesis of the disease. Our findings also suggest that a genetic defect leading to a gain of function of Ito could explain variants of BrS, in which ST-segment elevation or J-waves are evident in both right and left ECG leads. In the experiment, the researchers used many compounds, for example, 2-Amino-3,5-dibromobenzonitrile (cas: 68385-95-5Computed Properties of C7H4Br2N2).
2-Amino-3,5-dibromobenzonitrile (cas: 68385-95-5) belongs to nitriles. Nitrile function is a very important functional group because it can be manipulated to other functional groups such as carboxylic acid by hydrolysis or amine by reduction, respectively. Nitrile groups in organic compounds can undergo a variety of reactions depending on the reactants or conditions. A nitrile group can be hydrolyzed, reduced, or ejected from a molecule as a cyanide ion.Computed Properties of C7H4Br2N2
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts