Title of article
Synthesis and evaluation of α,α′-disubstituted phenylacetate derivatives for T-type calcium channel blockers
Author/Authors
Hyung Kook Lee، نويسنده , , Yun Suk Lee، نويسنده , , Eun Joo Roh، نويسنده , , Hyewhon Rhim، نويسنده , , Jae Yeol Lee، نويسنده , , Kye Jung Shin، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
4424
To page
4427
Abstract
We have synthesized and evaluated α,α′-disubstituted phenylacetate derivatives that were designed as T-type calcium channel blockers. Among them, compound 10e (IC50 = 8.17 ± 0.48 nM) showed the most potent T-type calcium current blocking activity and higher potency than Mibefradil (IC50 = 1.34 ± 0.49 μM). The PK profile and subtype selectivity over L-type calcium channel were satisfied for further animal assay using disease model.
Keywords
T-type calcium channel , Neuropathic pain , Patch-clamp
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799799
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