Data di Pubblicazione:
1983
Citazione:
Beta-adrenoceptor desensitization in rat lung: functional and biochemical aspects / M. P. Abbracchio, F. Cattabeni, E. Coen, Y. Torres-Hernandez, C. Omini. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 89:1-2(1983), pp. 35-42. [10.1016/0014-2999(83)90605-2]
Abstract:
Rat lung parenchymal strips were used to study β-adrenoceptor desensitization from both a functional and a biochemical point of view. Prolonged 'in vitro' exposure of rat lung to theβ-agonist isoproterenol (10-6 M for 20 min) markedly reduced the antagonistic activity of isoproterenol on carbachol-induced contractions. The loss of responsiveness to isoproterenol was associated with a 33% decrease of the β-receptor number with concomitant reduction of isoproterenol-stimulated adenylate cyclase activity, whereas the enzyme response to NaF was identical in control and in desensitized rat lung. On the basis of these results obtained by comparing the functional and biochemical aspects of the desensitization process, we suggest that the marked reduction of pharmacological activity of isoproterenol after desensitization was primarily due to the decrease in the number of binding sites. The possible molecular mechanisms underlying desensitization are also discussed.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Adenylate cyclase; Desensitization; Rat lung; β-Adrenoceptor
Elenco autori:
M. P. Abbracchio, F. Cattabeni, E. Coen, Y. Torres-Hernandez, C. Omini
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