SAR of a series of inhaled A2A agonists and comparison of inhaled pharmacokinetics in a preclinical model with clinical pharmacokinetic data

被引：24

作者：

Mantell, Simon J. ^{[1
]}

Stephenson, Peter T. ^{[1
]}

Monaghan, Sandra M. ^{[1
]}

Maw, Graham N. ^{[1
]}

Trevethick, Michael A. ^{[1
]}

Yeadon, Michael ^{[1
]}

Walker, Don K. ^{[1
]}

Selby, Matthew D. ^{[1
]}

Batchelor, David V. ^{[1
]}

Rozze, Stuart ^{[1
]}

Chavaroche, Helene ^{[1
]}

Lemaitre, Arnaud ^{[1
]}

Wright, Karen N. ^{[1
]}

Whitlock, Lynsey ^{[1
]}

Stuart, Emilio F. ^{[1
]}

Wright, Patricia A. ^{[1
]}

Macintyre, Fiona ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Sandwich Labs, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期

关键词：

A2A; COPD; Pharmacokinetics; Inhalation; OBSTRUCTIVE PULMONARY-DISEASE; RECEPTOR AGONIST; INFLAMMATION; THERAPY;

D O I：

10.1016/j.bmcl.2009.05.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be therapeutically useful. The pharmacological and pharmacokinetic SAR of a series of inhaled A(2A) agonists is described leading through to human pharmacokinetic data for a clinical candidate. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4471 / 4475

页数：5

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