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Bioorg Med Chem Lett
; 21(19): 5910-5, 2011 Oct 01.
Article
in English
| MEDLINE
| ID: mdl-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.