Abstract
A series of 8-substituted xanthines were synthesized and their affinity in vitro towards A1, A2A-adenosine receptors was evaluated by radioligand receptor binding assays. All compounds showed a greater affinity and selectivity towards the A1-adenosine receptor than theophylline. The compounds in which the n-proyl group is in 1-position of the xanthine nucleus and the pyridazinone system in 8-position is linked through a chain of two or four carbon atoms, showed the highest affinity and selectivity.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Binding, Competitive
-
Cattle
-
Cell Membrane / chemistry
-
Cell Membrane / metabolism
-
Cerebral Cortex / cytology
-
Cerebral Cortex / ultrastructure
-
Corpus Striatum / cytology
-
Corpus Striatum / ultrastructure
-
Purinergic P1 Receptor Antagonists*
-
Radioligand Assay
-
Receptors, Purinergic P1 / metabolism
-
Structure-Activity Relationship
-
Theophylline / chemical synthesis
-
Theophylline / metabolism
-
Theophylline / pharmacology
-
Xanthines / chemistry
-
Xanthines / metabolism
-
Xanthines / pharmacology*
Substances
-
Purinergic P1 Receptor Antagonists
-
Receptors, Purinergic P1
-
Xanthines
-
Theophylline