The Design of a Series of Highly A2 Selective Adenosine Agonists
The purine nucleoside, adenosine has been extensively studied as a modulator of cardiovascular function since it was shown to have potent hypotensive and bradycardic activity some 60 years ago (Drury et al., 1929). The hypotensive actions of adenosine occur via several mechanisms among which are direct regulation of blood flow via vasodilation of the peripheral vasculature, including the coronary arteries (Berne et al., 1983). Adenosine also produces sinus bradycardia and prolongation of impluse conduction in the atrioventricular node (Bellardinelli et al., 1983). In addition, adenosine has the ability to inhibit neurotransmitter release (Fredholm et al., 1988) and possesses potent central nervous system depressant and anticonvulsant activity (Dunwiddie, 1985).
KeywordsPotential Intracellular Action Adenosine Receptor Subtype Fold Selectivity Receptor Binding Profile Inhibit Neurotransmitter Release
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