Several adenosine analogs were evaluated for their effects on rate and contractility in guinea pig isolated atria. Among adenosine agonists, (-)-N-(1-methyl-2-phenylethyl) adenosine (l-phenylisopropyladenosine; l-PIA) and N-cyclohexyladenosine (CHA), decreased rate and force at nanomolar concentrations, whereas 2-chloroadenosine, N,N-dimethyladenosine (N6-dimethyladenosine) and (+)-N-(1-methyl-2-phenylethyl)adenosine (d-phenylisopropyladenosine; d-PIA) were less potent cardiac depressants. The degree and order of potency of these agonists suggest that the cardiac depressant effects of adenosine are mediated via A1-receptors. The cardiac depressant effects of CHA and l-PIA were antagonized by theophylline and 1,3-diethyl-8-phenylxanthine (DPX).
D B Evans, J A Schenden, J A Bristol. Adenosine receptors mediating cardiac depression. Life sciences. 1982 Nov 29;31(22):2425-32
PMID: 7154843
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