Referenced in: none

Automatically associated channels: Kv11.1

Title: Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers.

Authors: Hyun Min Woo, Yun Suk Lee, Eun Joo Roh, Seon Hee Seo, Chi Man Song, Hye Jin Chung, Ae Nim Pae, Kye Jung Shin

Journal, date & volume: Bioorg. Med. Chem. Lett., 2011 Oct 1 , 21, 5910-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21843937

Abstract
To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 4-piperidinecarboxylate and 4-piperidinecyanide derivatives were prepared and evaluated for in vitro and in vivo activity against α(1G) calcium channel. Among them, several compounds showed good T-type calcium channel inhibitory activity and minimal off-target activity over hERG channel (% inhibition at 10 μM=61.85-71.99, hERG channel IC(50)=1.57 ± 0.14-4.98 ± 0.36 μM). Selected compound 31a was evaluated on SNL model of neuropathic pain and showed inhibitory effect on mechanical allodynia.