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- W2080437029 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 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." @default.
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- W2080437029 date "2011-10-01" @default.
- W2080437029 modified "2023-10-18" @default.
- W2080437029 title "Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers" @default.
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- W2080437029 doi "https://doi.org/10.1016/j.bmcl.2011.07.087" @default.
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