Discovery and evaluation of Ca v 3.1-selective T-type calcium channel blockers.

We identified and characterized a series of pyrazole amides as potent, selective Cav 3.1-blockers. This series culminated with the identification of pyrazole amides 5a and 12d, with excellent potencies and/or selectivities toward the Cav 3.2- and Cav 3.3-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.