ChemInform Abstract: N-Cycloalkyl Derivatives of Adenosine and 1-Deazaadenosine as Agonists and Partial Agonists of the A1 Adenosine Receptor.
Abstract
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ChemInform Abstract
Adenosine derivatives (I) prove to be full agonists, whereas the 1-deaza analogues (II) show affinities for the A1 receptor about 10-fold lower and the 2′-deoxy analogues (III), especially (IIIh)-(IIIm), bind to the A1 receptor with affinities in the high nanomolar range. Most of the latter ones are partial agonists. These results indicate that there is no simple linear relationship between receptor occupancy and activation and that a critical density of A1 adenosine receptors in the high-affinity state is required for G protein activation.
