EVIDENCE FOR SPECIFIC ADENOSINE RECEPTORS AT CHOLINERGIC NERVE ENDINGS
- 1 January 1980
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 71 (1), 191-194
- https://doi.org/10.1111/j.1476-5381.1980.tb10925.x
Abstract
1 An electrophysiological study was made to determine if adenosine and adenine nucleotides affect cholinergic nerve endings to frog skeletal muscle through relatively non-specific nucleotide receptors or through specific adenosine receptors. 2 Non-hydrolysable derivatives of adenosine triphosphate failed to alter the mean number of acetylcholine (ACh) quanta released by the nerve impulse (m) or the miniature endplate potential frequency (m.e.p.p.f) but N6-methyladenosine and 2-chloroadenosine, two adenosine analogues with an unsubstituted ribose moiety (R-site agonists), produced marked reductions in m and m.e.p.p.f. 3 In contrast, 2'-deoxyadenosine, a derivative with an unsubstituted purine ring (P-site agonist), generally produced increases in m and m.e.p.p.f, which further increased after removing the drug. Other P-site agonists such as 5'-deoxyadenosine (in the presence of theophylline) and 9-beta-D-arabinofuranosyl adenine also increased m and m.e.p.p.f. 4 The results suggest that two types of adenosine receptors may be present at cholinergic nerve endings, one type (R-site) mediating depression and the other type (P-site) producing enhancement of ACh release.Keywords
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