Literature DB >> 15664822

The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.

Jeff Zablocki1, Rao Kalla, Thao Perry, Venkata Palle, Vaibhav Varkhedkar, Dengming Xiao, Anthony Piscopio, Tenning Maa, Art Gimbel, Jia Hao, Nancy Chu, Kwan Leung, Dewan Zeng.   

Abstract

Adenosine has been suggested to play a role in asthma, possibly via activation of A(2B) adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A(2B) AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A(2B) AdoR antagonist with good selectivity (A(2B) AdoR K(i)=50 nM, selectivity A(1)>200: A(2A)>200: A(3)>167).

Entities:  

Mesh：

Substances：

Year:  2005        PMID： 15664822     DOI： 10.1016/j.bmcl.2004.11.044

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


  7 in total

Review 1.  Xanthines as adenosine receptor antagonists.

Authors:  Christa E Müller; Kenneth A Jacobson
Journal:  Handb Exp Pharmacol       Date:  2011

2.  Synthesis of a library of "lead-like" γ-lactams by a one pot, four-component reaction.

Authors:  Kevin S Martin; Michael J Di Maso; James C Fettinger; Jared T Shaw
Journal:  ACS Comb Sci       Date:  2013-06-12       Impact factor: 3.784

Review 3.  Recovery of respiratory activity after C2 hemisection (C2HS): involvement of adenosinergic mechanisms.

Authors:  Kwaku D Nantwi
Journal:  Respir Physiol Neurobiol       Date:  2009-08-03       Impact factor: 1.931

Review 4.  Progress in the pursuit of therapeutic adenosine receptor antagonists.

Authors:  Stefano Moro; Zhan-Guo Gao; Kenneth A Jacobson; Giampiero Spalluto
Journal:  Med Res Rev       Date:  2006-03       Impact factor: 12.388

5.  Mast cell adenosine receptors function: a focus on the a3 adenosine receptor and inflammation.

Authors:  Noam Rudich; Katya Ravid; Ronit Sagi-Eisenberg
Journal:  Front Immunol       Date:  2012-06-04       Impact factor: 7.561

Review 6.  Purinergic Signaling in Mast Cell Degranulation and Asthma.

Authors:  Zhan-Guo Gao; Kenneth A Jacobson
Journal:  Front Pharmacol       Date:  2017-12-22       Impact factor: 5.810

7.  Progress in the discovery of selective, high affinity A(2B) adenosine receptor antagonists as clinical candidates.

Authors:  Rao V Kalla; Jeff Zablocki
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.