1071874-96-8Relevant articles and documents
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels
Yang, Zhi-Qiang,Barrow, James C.,Snipe, William D.,Schlegel, Kelly-Ann S.,Shu, Youheng,Yang, F. Vivien,Lindsley, Craig W.,Rittle, Kenneth E.,Bock, Mark G.,Hartman, George D.,Uebele, Victor N.,Nuss, Cindy E.,Fox, Steve V.,Kraus, Richard L.,Doran, Scott M.,Connolly, Thomas M.,Tang, Cuyue,Ballard, Jeanine E.,Kuo, Yuhsin,Adarayan, Emily D.,Prueksaritanont, Thomayant,Zrada, Matthew M.,Marino, Michael J.,Graufelds, Valerie Kuzmick,DiLella, Anthony G.,Reynolds, Ian J.,Vargas, Hugo M.,Bunting, Patricia B.,Woltmann, Richard F.,Magee, Michael M.,Koblan, Kenneth S.,Renger, John J.
, p. 6471 - 6477 (2008)
The discovery of a novel series of potent and selective T-type calcium channel antagonists is reported. Initial optimization of high-throughput screening leads afforded a 1,4-substituted piperidine amide 6 with good potency and limited selectivity over hE
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4- piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor
Giordanetto, Fabrizio,W?llberg, Andreas,Knerr, Laurent,Selmi, Nidhal,Ullah, Victoria,Thorstensson, Fredrik,Lindelo, Asa,Karlsson, Staffan,Nikitidis, Grigorios,Llinas, Antonio,Wang, Qing-Dong,Lindqvist, Anders,H?gberg, ?got,Lindhardt, Emma,Astrand, Annika,Duker, G?ran
, p. 119 - 124 (2013/02/25)
The T-type calcium channel inhibitor Mibefradil was reported to protect the heart from atrial remodeling, a key process involved in the development of atrial fibrillation and arrhythmias. Mibefradil is not a selective T-type calcium channel inhibitor and also affects the function of different ion channels. Our aim was to develop a selective T-type calcium channel inhibitor to validate the importance of T-type-related pharmacology in atrial fibrillation. Structural optimisation of a previously disclosed hit series focussed on minimising exposure to the central nervous system and improving pharmacokinetic properties, while maintain adequate potency and selectivity. This resulted in the design of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4- piperidyl]methyl]-3,5-dichloro-benzamide, a novel, selective, peripherally restricted chemical probe to verify the role of T-type calcium channel inhibition on atrial fibrillation protection.
