Abstract
Adenosine receptor (AR) antagonists belong to two major groups of compounds: xanthines and non-xanthines. Recently several annelated xanthine derivatives have been described as selective A(1), A(2A), A(2B) and A(3) ARs antagonists. Contrary to dipropyl derivatives, in the group of dimethyl (un)substituted arylalkyl pyrimido[2,1-f]purindiones selective mainly adenosine A(2A) receptor antagonists were identified. Their activity depended on aryl substitution and its distance from pyrimido[2,1-f]purindione.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine A2 Receptor Antagonists
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Animals
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Humans
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Molecular Structure
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Purinergic P1 Receptor Antagonists*
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Purines / chemistry*
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Purines / metabolism*
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Purines / pharmacology
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Pyrimidines / chemistry*
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Pyrimidines / metabolism*
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Pyrimidines / pharmacology
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Rats
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Receptor, Adenosine A2A / metabolism
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Receptors, Purinergic P1 / metabolism
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Stereoisomerism
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Structure-Activity Relationship
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Theophylline / chemistry
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Theophylline / metabolism
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Theophylline / pharmacology
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Xanthines / chemistry
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Xanthines / metabolism
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Xanthines / pharmacology
Substances
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Adenosine A2 Receptor Antagonists
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Purinergic P1 Receptor Antagonists
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Purines
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Pyrimidines
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Receptor, Adenosine A2A
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Receptors, Purinergic P1
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Xanthines
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Theophylline