Abstract
Periodate oxidation of eight N 6-substituted adenosine derivatives was performed with the aim of oxidizing the vicinal 2′ and 3′ hydroxyl groups of the ribose moiety. A thermodynamical and pharmacological characterization of the products of this transformation allowed us to verify that oxidized adenosine analogues act as agonists at adenosine A 1 receptors. The dependence of their association constants on temperature indicates that their binding is entropy driven, a feature typical of adenosine A 1 receptor agonists; moreover all synthesized compounds were able to fully inhibit the forskolin induced c-AMP accumulation in rat isolated adipocytes. This is the first report suggesting that the presence of an intact ribose moiety is not necessary for agonistic activity at adenosine A 1 receptor. In fact periodate oxidation of the ribose moiety yields a dialdehyde and it is recognized that nucleoside dialdehydes are complex equilibrium mixtures of cyclic and acyclic hydrates and hemiacetals.
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Schedule a callMore From: Biochimica et Biophysica Acta (BBA) - Molecular Cell Research
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