Effects on tracheal smooth muscle of adenosine and methylxanthines, and their interaction
- 1 December 1982
- journal article
- research article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 34 (12) , 788-793
- https://doi.org/10.1111/j.2042-7158.1982.tb06226.x
Abstract
The relaxant effects of xanthine and 15 different methylxanthines were studied in a guinea-pig isolated tracheal ring preparation. Substitution in the 3- and 1-positions of the xanthine molecule were found to be of greatest importance for improving tracheal relaxant potency. The unsubstituted xanthine and all 9-methylated xanthines were weakly active. Adenosine occasionally contracted (slightly) the tracheae but a concentration-dependent relaxation was always recorded. Endogenous adenosine did not seem to contribute to the tracheal tone. Xanthines methylated in the 1-position consistently antagonized the relaxant effect of adenosine and produced graded rightward shifts of the concentration-response line to adenosine (competitive antagonism). Xanthines with an unsubstituted 1-position or with comethylation in the 9-position were generally without antagonism. The results support our view that bronchodilating xanthine derivatives lacking universal adenosine antagonism can be produced.This publication has 24 references indexed in Scilit:
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