The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma
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 affinit...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (3), p.609-612 |
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| container_issue | 3 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 15 |
| creator | Zablocki, Jeff Kalla, Rao Perry, Thao Palle, Venkata Varkhedkar, Vaibhav Xiao, Dengming Piscopio, Anthony Maa, Tenning Gimbel, Art Hao, Jia Chu, Nancy Leung, Kwan Zeng, Dewan |
| description | 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). |
| doi_str_mv | 10.1016/j.bmcl.2004.11.044 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2005-02, Vol.15 (3), p.609-612 |
| issn | 0960-894X |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Adenosine A2 Receptor Antagonists Asthma - drug therapy Drug Stability Humans Liver - cytology Liver - metabolism Structure-Activity Relationship Xanthines - chemical synthesis Xanthines - pharmacology |
| title | The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma |
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