Binding of [3H]cyclohexyladenosine to adenosine recognition sites in guinea pig ileal membranes: comparison with binding in brain membranes.
The stable adenosine agonist [3H]cyclohexyladenosine binds to membranes prepared from guinea pig myenteric plexus with high affinity (Kd = 1.8 nM) in a saturable, reversible manner. Binding pharmacology was consistent with the labelling of an A1 type adenosine receptor with the R-isomer of N6-phenylisopropyladenosine (PIA) being 11 times more potent than the S-diastereomer. Binding was similar to that observed in brain tissue being displaced by a number of xanthine adenosine antagonists. In terms of density of binding sites, however, there were approximately 9 times fewer higher affinity binding sites in ileal membranes than in the central nervous system.
Williams
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D000241:Adenosine / Q000031:analogs & derivatives* / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008566:Membranes / Q000378:metabolism; D009197:Myenteric Plexus / Q000378:metabolism*; D010660:Phenylisopropyladenosine / Q000378:metabolism; D011869:Radioligand Assay; D011956:Receptors, Cell Surface / Q000032:analysis / Q000378:metabolism*; D011983:Receptors, Purinergic; D013045:Species Specificity; D014970:Xanthines / Q000378:metabolism
D011956:Receptors, Cell Surface; D011983:Receptors, Purinergic; D014970:Xanthines; D010660:Phenylisopropyladenosine; C027513:N(6)-cyclohexyladenosine; D000241:Adenosine