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We have used the autoradiographic technique to localize the distribution of adenosine receptors and adenosine kinase in rat lung. A selective antagonist of the A2b adenosine receptor, PSB-1115 [(2, 8-dicyclopentyl-7-methyl-2-propyl-1,3-dipropylxanthine)3-(N-ethyl-3-iodo-2-propynyl)1,3-dipropylxanthine] and a selective inhibitor of the A2a adenosine receptor, CSC [2- (4-cyclopentyl-4(1-homopiperidinyl) pyridyl)-9(1H-pyrazolo [1,5-a]pyrimidin-4-yl-)] were used to determine the localization of the A2a and A2b receptor subtypes, respectively. The distribution of A2a and A2b receptors was similar with no significant differences in the density of adenosine receptors occurring in the trachea, bronchi or bronchioles. Adenosine kinase activity was also found in association with the alveolar epithelium and type II pneumocytes. alpha-Difluoromethylornithine (DFMO) administration significantly reduced A2b receptor density in the lung and resulted in an increase in the density of A2a receptors, a decrease in A1 receptor density and an increase in adenosine kinase activity. These results indicate that there are a number of adenosine receptors in the lung which appear to have different distributions suggesting different roles in the pulmonary regulation of adenosine receptors.
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