Regulatory molecules for the 5-HT3 receptor ion channel gating system

被引：43

作者：

Yoshida, Satoshi ^{[1
]}

Watanabe, Takashi ^{[1
]}

Sato, Yasuo ^{[1
]}

机构：

[1] Meiji Seika Kaisha Ltd, Pharmaceut Res Dept, Kohoku Ku, Yokohama, Kanagawa 2228567, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 10期

关键词：

5-HT3; receptor; LGIC; partial agonist; ion channels; molecular modeling;

D O I：

10.1016/j.bmc.2007.02.054

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Substituted benzoxazole derivatives which possess a nitrogen containing heterocycle at C2 are selective partial agonists of the 5-HT3 receptor. Alteration of substituents on the benzoxazole nucleus affords both agonist-like and antagonist-like compounds, and uniquely modifies the function of the 5-HT3 receptor ion channel gating system. SAR and corroborative computational docking study for these partial agonists successfully explained structure and function of the 5-HT3 receptor. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3515 / 3523

页数：9

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