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

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

  • Bioorg Med Chem Lett. 2005 Feb 1;15(3):609-12. doi: 10.1016/j.bmcl.2004.11.044.
Jeff Zablocki 1,  Rao Kalla,  Thao Perry,  Venkata Palle,  Vaibhav Varkhedkar,  Dengming Xiao,  Anthony Piscopio,  Tenning Maa,  Art Gimbel,  Jia Hao,  Nancy Chu,  Kwan Leung,  Dewan Zeng
Affiliations

Affiliation

  • 1 Department of Bioorganic Chemistry, CV Therapeutics, Inc., 3172 Porter Dr., Palo Alto, CA 94304, USA. jeff.zablocki@cvt.com
PMID: 15664822 DOI: 10.1016/j.bmcl.2004.11.044
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).

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