Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats

被引：17

作者：

Lugar, CW ^{[1
]}

Clay, MP ^{[1
]}

Lindstrom, TD ^{[1
]}

Woodson, AL ^{[1
]}

Smiley, D ^{[1
]}

Heiman, ML ^{[1
]}

Dodge, JA ^{[1
]}

机构：

[1] Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 23期

关键词：

ghrelin; growth hormone secretagogues; energy expenditure; food consumption;

D O I：

10.1016/j.bmcl.2004.09.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-(2-Amino-2-methyl-propionylamino)-5-phenyl-pentanoic acid {1-[1-(4-methoxy-phenyl)-1-methyl-2-oxo-2-pyrrolidin-1-yl-ethyll-lH-imidazol-4-yl}-amide (LY444711, 6) is an orally active ghrelin agonist that binds with high affinity to and is a potent activator of the growth hormone secretagogue receptor la (GHS-R1a) receptor. In rat models of feeding behavior and pharmacology, 6 creates a positive energy balance and induces adiposity by stimulating food consumption and sparing fat utilization. As an orally active ghrelin agonist, 6 represents a new pharmacological tool to investigate the orexigenic role of ghrelin in regulating energy homeostasis. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5873 / 5876

页数：4

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