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Peer-reviewed veterinary case report

Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2009
Authors:
Piatnitski Chekler, Eugene L et al.
Affiliation:
Wyeth Research · United States

Abstract

In an effort to discover potent, orally bioavailable compounds for the treatment of atrial fibrillation (AF) and ventricular tachycardia (VT), we developed a class of gap-junction modifiers typified by GAP-134 (1, R(1)=OH, R(2)=NH(2)), a compound currently under clinical evaluation. Selected compounds with the desired in-vitro profile demonstrated positive in vivo results in the mouse CaCl(2) arrhythmia model upon oral administration.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/19616941/