Abstract
The synthesis of an important set of 3-furfurylxanthine derivatives is described. Binding affinities were determined for rat A(1) and human A(2A), A(2B) and A(3) receptors. Several of the 3-furfuryl-7-methylxanthine derivatives showed moderate-to-high affinity at human A(2B) receptors, the most active compound (10d) having a K(i) of 7.4 nM for hA(2B) receptors, with selectivities over rA(1) and hA(2A) receptors up to 14-fold and 11-fold, respectively. Affinities for hA(3) receptors were very low for all members of the set.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine A1 Receptor Antagonists
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Adenosine A2 Receptor Antagonists
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Adenosine A3 Receptor Antagonists
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Animals
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Cell Line
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Humans
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Protein Binding
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Purinergic P1 Receptor Antagonists*
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Rats
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Receptor, Adenosine A1 / metabolism
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Receptor, Adenosine A2A / metabolism
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Receptor, Adenosine A2B / metabolism
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Receptor, Adenosine A3 / metabolism
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Receptors, Purinergic P1 / metabolism*
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Structure-Activity Relationship
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Xanthines / chemical synthesis
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Xanthines / chemistry*
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Xanthines / pharmacology*
Substances
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Adenosine A1 Receptor Antagonists
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Adenosine A2 Receptor Antagonists
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Adenosine A3 Receptor Antagonists
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Purinergic P1 Receptor Antagonists
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Receptor, Adenosine A1
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Receptor, Adenosine A2A
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Receptor, Adenosine A2B
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Receptor, Adenosine A3
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Receptors, Purinergic P1
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Xanthines