94320-46-4Relevant academic research and scientific papers
Pilsicainide and its oxymethylene analog: Facile alternative syntheses and in vitro testing on human skeletal muscle sodium channels
Bruno, Claudio,Catalano, Alessia,Desaphy, Jean-Francois,Cavalluzzi, Maria M.,Carocci, Alessia,Dipalma, Antonella,Franchini, Carlo,Lentini, Giovanni,Camerino, Diana Conte,Tortorella, Vincenzo
, p. 2011 - 2026 (2008/09/18)
Facile, alternative synthetic routes gave access to both pilsicainide [N-(2,6-dimethylphenyl)-2-tetrahydro-lH-pyrrolizin-7a(5H)-ylacetamide, 1], a well-known Ic antiarrhythmic drug, and its oxymethylene analog 2. Both compounds were tested on human skeletal muscle voltage-gated sodium channels, hNavl.4, transfected in tsA201 cells. 7a-[2-(2,6-Dimethylphenoxy)ethyl]hexahydro-lH-pyrrolizine (2) behaved as a bioisostere of 1, exerting a 4-fold more potent use-dependent block.
