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
  • 1. Department of Bioorganic Chemistry, CV Therapeutics, Inc., 3172 Porter Dr., Palo Alto, CA 94304, USA. [email protected]
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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