1355355-49-5Relevant articles and documents
Discovery and evaluation of Cav3.1-selective T-type calcium channel blockers
Bezen?on, Olivier,Remeň, Lubo?,Richard, Sylvia,Roch, Catherine,Kessler, Melanie,Moon, Richard,Mawet, Jacques,Ertel, Eric A.,Pfeifer, Thomas,Capeleto, Bruno
, p. 5322 - 5325 (2017)
We identified and characterized a series of pyrazole amides as potent, selective Cav3.1-blockers. This series culminated with the identification of pyrazole amides 5a and 12d, with excellent potencies and/or selectivities toward the Cav3.2- and Cav3.3-channels. This compound displays poor DMPK properties, making its use difficult for in vivo applications. Nevertheless, this compound as well as analogous ones are well-suited for in vitro studies.