Skip to main content
PMC home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1984 Apr;81(4):611–615. doi: 10.1111/j.1476-5381.1984.tb16125.x

Classification of beta-adrenoceptors in human isolated bronchus.

R G Goldie, J W Paterson, D Spina, J L Wale
PMCID: PMC1986912  PMID: 6144342

Abstract

(+/-)-Isoprenaline (Iso), (-)-adrenaline (Ad), (-)-noradrenaline (NA), (+/-)-phenylephrine (Phe) and the beta 2-selective adrenoceptor agonist (+/-)-fenoterol (Fen) caused a concentration-dependent relaxation of human isolated bronchial preparations. Iso, Ad and NA caused complete relaxation of both spontaneous and carbachol-induced bronchial tone. Fen, which was only tested in preparations where tone was induced with carbachol, also caused complete relaxation. However, Phe was a partial agonist in all preparations tested. When relaxation responses to these amines were calculated as a % of their maximal effects, comparison of EC50 values showed that the order of potency was Iso greater than Ad = Fen greater than NA greater than Phe (92:27:25:1:0.2) in preparations with carbachol-induced tone and Iso greater than Ad greater than NA greater than Phe (112:38:1:0.3) in preparations with spontaneous tone. pA2 values determined for the beta-adrenoceptor antagonists propranolol (non-selective), atenolol (beta-selective) and ICI-118, 551 (beta 2-selective), using Iso as an agonist were, 9.3, 5.3 and 9.1 respectively. These results indicate that beta 2-adrenoceptors mediate relaxation of human isolated bronchus to sympathomimetic amines in preparations obtained 4-14 h post-mortem from non-diseased lung. alpha-Adrenoceptors were apparently sparse or absent in this tissue.

Full text

PDF
612

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Bristow M., Sherrod T. R., Green R. D. Analysis of beta receptor drug interactions in isolated rabbit atrium, aorta, stomach and trachea. J Pharmacol Exp Ther. 1970 Jan;171(1):52–61. [PubMed] [Google Scholar]
  2. Goldie R. G., Paterson J. W., Wale J. L. Classification of beta-adrenoceptors in isolated bronchus of the pig. Br J Pharmacol. 1983 May;79(1):177–180. doi: 10.1111/j.1476-5381.1983.tb10510.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Goldie R. G., Paterson J. W., Wale J. L. Pharmacological responses of human and porcine lung parenchyma, bronchus and pulmonary artery. Br J Pharmacol. 1982 Aug;76(4):515–521. doi: 10.1111/j.1476-5381.1982.tb09248.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Harms H. H. Isoproterenol antagonism of cardioselective beta adrenergic receptor blocking agents: a comparative study of human and guinea-pig cardiac and bronchial beta adrenergic receptors. J Pharmacol Exp Ther. 1976 Nov;199(2):329–335. [PubMed] [Google Scholar]
  5. Larsson S., Svedmyr N. Bronchodilating effect and side effects of beta2- adrenoceptor stimulants by different modes of administration (tablets, metered aerosol, and combinations thereof). A study with salbutamol in asthmatics. Am Rev Respir Dis. 1977 Nov;116(5):861–869. doi: 10.1164/arrd.1977.116.5.861. [DOI] [PubMed] [Google Scholar]
  6. Lulich K. M., Mitchell H. W., Sparrow M. P. The cat lung strip as an in vitro preparation of peripheral airways: a comparison of beta-adrenoceptor agonists, autacoids and anaphylactic challenge on the lung strip and trachea. Br J Pharmacol. 1976 Sep;58(1):71–79. doi: 10.1111/j.1476-5381.1976.tb07694.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Madsen B. W., Tandon M. K., Paterson J. W. Cross-over study of the efficacy of four beta 2-sympathomimetic bronchodilator aerosols. Br J Clin Pharmacol. 1979 Jul;8(1):75–82. doi: 10.1111/j.1365-2125.1979.tb05912.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Mathé A. A., Aström A., Persson N. A. Some bronchoconstricting and bronchodilating responses of human isolated bronchi: evidence for the existence of -adrenoceptors. J Pharm Pharmacol. 1971 Dec;23(12):905–910. doi: 10.1111/j.2042-7158.1971.tb09891.x. [DOI] [PubMed] [Google Scholar]
  9. O'Donnell S. R. A selective beta-adrenoreceptor stimulant (Th1165a) related to orciprenaline. Eur J Pharmacol. 1970 Sep 1;12(1):35–43. doi: 10.1016/0014-2999(70)90026-9. [DOI] [PubMed] [Google Scholar]
  10. O'Donnell S. R. An examination of some -adrenoreceptor stimulants for selectivity using the isolated trachea and atria of the guinea pig. Eur J Pharmacol. 1972 Sep;19(3):371–379. doi: 10.1016/0014-2999(72)90104-5. [DOI] [PubMed] [Google Scholar]
  11. O'Donnell S. R., Wanstall J. C. Evidence that ICI 118, 551 is a potent, highly Beta 2-selective adrenoceptor antagonist and can be used to characterize Beta-adrenoceptor populations in tissues. Life Sci. 1980 Aug 25;27(8):671–677. doi: 10.1016/0024-3205(80)90008-9. [DOI] [PubMed] [Google Scholar]
  12. O'Donnell S. R., Wanstall J. C. Relaxation of cat trachea by beta-adrenoceptor agonists can be mediated by both beta1- and beta2-adrenoceptors and potentiated by inhibitors of extraneuronal uptake. Br J Pharmacol. 1983 Feb;78(2):417–424. doi: 10.1111/j.1476-5381.1983.tb09406.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. O'Donnell S. R., Wanstall J. C. The importance of choice of agonist in studies designed to predict beta 2 : beta 1 adrenoceptor selectivity of antagonists from pA2 values on guinea-pig trachea and atria. Naunyn Schmiedebergs Arch Pharmacol. 1979 Sep;308(3):183–190. doi: 10.1007/BF00501381. [DOI] [PubMed] [Google Scholar]
  14. Paterson J. W., Woolcock A. J., Shenfield G. M. Bronchodilator drugs. Am Rev Respir Dis. 1979 Nov;120(5):1149–1188. doi: 10.1164/arrd.1979.120.5.1149. [DOI] [PubMed] [Google Scholar]
  15. Simonsson B. G., Svedmyr N., Skoogh B. E., Andersson R., Bergh N. P. In vivo and in vitro studies on alpha-receptors in human airways. Potentiation with bacterial endotoxin. Scand J Respir Dis. 1972;53(4):227–236. [PubMed] [Google Scholar]
  16. Toda N., Hayashi S., Hatano Y., Okunishi H., Miyazaki M. Selectivity and steric effects of metoprolol isomers on isolated rabbit atria, arteries and tracheal muscles. J Pharmacol Exp Ther. 1978 Nov;207(2):311–319. [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology are provided here courtesy of The British Pharmacological Society

RESOURCES