α1‐Adrenoceptor function and autoradiographic distribution in human asthmatic lung

Abstract 1. The autoradiographic distribution of alpha 1-adrenoceptors was investigated in non-diseased and asthmatic human lung by use of [3H]-prazosin (H-PZ). To validate binding and autoradiographic methods, H-PZ binding was also measured in rat heart. 2. Significant levels of specific H-PZ binding were detected in sections of rat heart. This binding was associated with a single class of non-interacting sites of high affinity (dissociation constant, Kd = 1.17 +/- 0.26 nM). The maximum binding capacity (Bmax) was 59.5 +/- 4.5 fmol mg-1 protein. 3. In sharp contrast, very low levels of specific H-PZ binding were found in both human nondiseased and asthmatic bronchus, although a high level of binding of [125I]-iodocyanopindolol (I-CYP, 50 pM) to beta-adrenoceptors was detected in these airways. Furthermore, very low levels of autoradiographic grains representing specific H-PZ binding were found in all airway structures in human non-diseased or asthmatic lung parenchyma. 4. Consistent with these data, the alpha-adrenoceptor agonist phenylephrine failed to induce significant increases in tone in bronchi isolated from either non-diseased or asthmatic human lung. Results indicate that asthma does not involve significant increases in airway alpha 1-adrenoceptor function.