Literature DB >> 19501510

SAR of a series of inhaled A(2A) agonists and comparison of inhaled pharmacokinetics in a preclinical model with clinical pharmacokinetic data.

Simon J Mantell1, Peter T Stephenson, Sandra M Monaghan, Graham N Maw, Michael A Trevethick, Michael Yeadon, Don K Walker, Matthew D Selby, David V Batchelor, Stuart Rozze, Helene Chavaroche, Arnaud Lemaitre, Karen N Wright, Lynsey Whitlock, Emilio F Stuart, Patricia A Wright, Fiona Macintyre.   

Abstract

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.

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Year:  2009        PMID： 19501510     DOI： 10.1016/j.bmcl.2009.05.027

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time.

Authors:  Dong Guo; Thea Mulder-Krieger; Adriaan P IJzerman; Laura H Heitman
Journal:  Br J Pharmacol       Date:  2012-07       Impact factor: 8.739

Review 2.  Recent developments in adenosine receptor ligands and their potential as novel drugs.

Authors:  Christa E Müller; Kenneth A Jacobson
Journal:  Biochim Biophys Acta       Date:  2010-12-23

3.  Structure of an agonist-bound human A2A adenosine receptor.

Authors:  Fei Xu; Huixian Wu; Vsevolod Katritch; Gye Won Han; Kenneth A Jacobson; Zhan-Guo Gao; Vadim Cherezov; Raymond C Stevens
Journal:  Science       Date:  2011-03-10       Impact factor: 47.728

4.  Toll-like receptor (TLR) 3 immune modulation by unformulated small interfering RNA or DNA and the role of CD14 (in TLR-mediated effects).

Authors:  Cordula Weber; Christian Müller; Anja Podszuweit; Carmen Montino; Jörg Vollmer; Alexandra Forsbach
Journal:  Immunology       Date:  2012-05       Impact factor: 7.397

5.  Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A₂A adenosine receptor.

Authors:  Francesca Deflorian; T Santhosh Kumar; Khai Phan; Zhan-Guo Gao; Fei Xu; Huixian Wu; Vsevolod Katritch; Raymond C Stevens; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2011-12-12       Impact factor: 7.446

6.  Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.

Authors:  Ali El-Tayeb; Sebastian Michael; Aliaa Abdelrahman; Andrea Behrenswerth; Sabrina Gollos; Karen Nieber; Christa E Müller
Journal:  ACS Med Chem Lett       Date:  2011-10-10       Impact factor: 4.345

7.  Identification of Novel Chemical Entities for Adenosine Receptor Type 2A Using Molecular Modeling Approaches.

Authors:  Kelton L B Dos Santos; Jorddy N Cruz; Luciane B Silva; Ryan S Ramos; Moysés F A Neto; Cleison C Lobato; Sirlene S B Ota; Franco H A Leite; Rosivaldo S Borges; Carlos H T P da Silva; Joaquín M Campos; Cleydson B R Santos
Journal:  Molecules       Date:  2020-03-10       Impact factor: 4.411

Review 8.  Therapeutic applications.

Authors:  Stephen Tilley; Jon Volmer; Maryse Picher
Journal:  Subcell Biochem       Date:  2011

9.  The discovery of a selective and potent A2a agonist with extended lung retention.

Authors:  Annika B M Åstrand; Eva Lamm Bergström; Hui Zhang; Lena Börjesson; Therese Söderdahl; Cecilia Wingren; Anne-Helene Jansson; Amir Smailagic; Camilla Johansson; Håkan Bladh; Igor Shamovsky; Anders Tunek; Tomas Drmota
Journal:  Pharmacol Res Perspect       Date:  2015-05-04
  9 in total

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