Abstract
Arylazido aminopropionyl ATP (ANAPP 3), an ATP-receptor antagonist containing a photosensitive arylazido moiety coupled to the 3′ hydroxyl of ATP, inhibited the twitch response of electrically stimulated ileal longitudinal muscle strips in a dose-dependent manner. These agonist responses to ANAPP 3 were attenuated by the enzyme adenosine deaminase and antagonized by the adenosine receptor antagonist 8-phenyltheophylline. Schild analysis yielded similar pA 2 values for ANAPP 3 and adenosine suggesting a common receptor site. Several 3′-ribose-modified adenosine analogs were tested for agonist activity and found to be inactive. Results suggest that ANAPP 3 interacts at the presynaptic adenosine receptor of the ileum following its metabolism to adenosine, which explains the lack of antagonism at adenosine receptors of ileal smooth muscle following photolysis of ANAPP 3.
Published Version
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