The discovery of novel openers of Ca2+-dependent large-conductance potassium channels: Pharmacophore search and physiological evaluation of flavonoids

被引：15

作者：

Li, Y

Starrett, JE

Meanwell, NA

Johnson, G

Harte, WE

Dworetzky, SI

Boissard, CG

Gribkoff, VK

机构：

[1] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,DEPT CHEM,WALLINGFORD,CT 06492

[2] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,DEPT CENT NERVOUS SYST DRUG DISCOVERY,WALLINGFORD,CT 06492

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(97)00076-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three-dimensional database searching based on the pharmacophore model of the known maxi-K opener NS-004 (1) and electrophysiological evaluation led to the discovery of flavonoids (3c and 3d) as openers of the cloned maxi-K channel mSlo expressed in Xenopus laevis oocytes. The cyclic constrained flavonoids were found to be more efficacious than the acyclic phloretin. (C) 1997 Bristol-Myers Squibb.

引用

页码：759 / 762

页数：4

共 22 条

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Allen F.H., 1993, CHEM AUTOMAT NEWS, V8, P31

[2]

ALLEN FH, 1993, CHEM DESIGN AUTOMATI, V8, P1

[3] MSLO, A COMPLEX MOUSE GENE ENCODING MAXI CALCIUM-ACTIVATED POTASSIUM CHANNELS [J].