1338251-74-3Relevant articles and documents
Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers
Woo, Hyun Min,Lee, Yun Suk,Roh, Eun Joo,Seo, Seon Hee,Song, Chi Man,Chung, Hye Jin,Pae, Ae Nim,Shin, Kye Jung
, p. 5910 - 5915 (2011/10/09)
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 α1G 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 IC50 = 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.