1282918-50-6Relevant academic research and scientific papers
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.
