Adenosine A1 receptor mediated inhibition of nerve stimulation-induced contractions of the rabbit portal vein.
The aim of this study was to determine whether the adenosine receptor that inhibits adrenergic neurotransmission in the rabbit portal vein is of the A1 or the A2 subtype. Isometric contractions of the isolated vein were evoked by electrical field stimulation and by exogenous noradrenaline. Low concentrations of adenosine, and a number of analogues inhibited the response evoked by field stimulation but had no effect on those evoked by noradrenaline. The order of inhibitory potency was: L-N6-phenylisopropyladenosine (L-PIA) = N6-cyclohexyladenosine (CHA) = 5'-N-cyclopropylcarboxamide adenosine (NCPCA) greater than or equal to 5'-N-ethylcarboxamide adenosine (NECA) = 2-chloroadenosine greater than adenosine greater than D-PIA. The difference in potency between the stereoisomers L- and D-PIA was about 60 fold. The purine transport inhibitor dipyridamole potentiated the inhibitory effect of adenosine but not that of its analogues. The inhibitory responses evoked by adenosine and its' analogues were attenuated by the adenosine antagonist theophylline. These results indicate that adenosine selectively inhibits contractions of the rabbit portal vein evoked by adrenergic nerve stimulation via activation of an adenosine A1 receptor.
D000241:Adenosine / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D003042:Cocaine / Q000494:pharmacology; D003913:Dextroamphetamine / Q000494:pharmacology; D004176:Dipyridamole / Q000494:pharmacology; D004558:Electric Stimulation; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology*; D010660:Phenylisopropyladenosine / Q000494:pharmacology; D011169:Portal Vein; D011817:Rabbits; D011956:Receptors, Cell Surface / Q000502:physiology*; D011983:Receptors, Purinergic; D013806:Theophylline / Q000494:pharmacology
D011956:Receptors, Cell Surface; D011983:Receptors, Purinergic; D010660:Phenylisopropyladenosine; D004176:Dipyridamole; D013806:Theophylline; D003042:Cocaine; D000241:Adenosine; D003913:Dextroamphetamine