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. 1983 May;79(1):177–180. doi: 10.1111/j.1476-5381.1983.tb10510.x

Classification of beta-adrenoceptors in isolated bronchus of the pig.

R G Goldie, J W Paterson, J L Wale
PMCID: PMC2044832  PMID: 6307451

Abstract

1 (+/-)-Isoprenaline (Iso), (-)-adrenaline (Ad), (-)-noradrenaline (NA), the beta 2-selective adrenoceptor agonist (+/-)-fenoterol (Fen) and the beta 1-selective adrenoceptor agonist (+/-)-RO363 caused concentration-dependent relaxation of preparations of pig bronchus pre-contracted with carbachol 40-ng/ml (0.22 microM). Iso, Ad, NA and Fen caused complete relaxation of carbachol-induced tone, but RO363 caused relaxation equivalent to only 59% of the maximal response to Iso. 2 When relaxation responses to these amines were plotted as a % of their maximal effects, comparison of EC50 values showed that the order of potency was RO363 greater than Iso greater than NA greater than Fen greater than Ad (14.4:4.6:1:0.4:0.3). 3 pA2 values determined for the beta-adrenoceptor antagonists propranolol (non-selective) and atenolol (beta 1-selective), or the partial agonist salbutamol (beta 2-selective) using Iso as agonist were 8.3, 7.3 and 4.4 respectively. The pA2 value for atenolol using RO363 as the agonist was 7.6. 4 These results indicate that porcine bronchus contains a homogeneous population of beta 1-adrenoceptors.

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Selected References

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

  1. ARUNLAKSHANA O., SCHILD H. O. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959 Mar;14(1):48–58. doi: 10.1111/j.1476-5381.1959.tb00928.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Foster R. W. A correlation between inhibition of the uptake of 3H from (+)-3H-noradrenaline and potentiation of the responses to (-)-noradrenaline in the guinea-pig isolated trachea. Br J Pharmacol Chemother. 1968 Jun;33(2):357–367. doi: 10.1111/j.1476-5381.1968.tb00996.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Foster R. W. An uptake of radioactivity from (plus or minus)-3H-isoprenaline and its inhibition by drugs which potentiate the responses to (minus)-isoprenaline in the guinea-pig isolated trachea. Br J Pharmacol. 1969 Mar;35(3):418–427. doi: 10.1111/j.1476-5381.1969.tb08283.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Foster R. W. The potentiation of the responses to noradrenaline and isoprenaline of the guinea-pig isolated tracheal chain preparation by desipramine, cocaine, phentolamine, phenoxybenzamine, guanethidine, metanephrine and cooling. Br J Pharmacol Chemother. 1967 Nov;31(3):466–482. doi: 10.1111/j.1476-5381.1967.tb00412.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Goldie R. G., Paterson J. W. Catecholamine transport in isolated lung parenchyma of pig. Br J Pharmacol. 1982 Aug;76(4):507–513. doi: 10.1111/j.1476-5381.1982.tb09247.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Goldie R. G., Paterson J. W., Wale J. L. A comparative study of beta-adrenoceptors in human and porcine lung parenchyma strip. Br J Pharmacol. 1982 Aug;76(4):523–526. doi: 10.1111/j.1476-5381.1982.tb09249.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. 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]
  8. 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]
  9. Iakovidis D., Malta E., McPherson G. A., Raper C. In vitro activity of RO363, a beta1-adrenoceptor selective agonist. Br J Pharmacol. 1980 Apr;68(4):677–685. doi: 10.1111/j.1476-5381.1980.tb10860.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Kenakin T. P. Errors in the measurement of agonist potency-ratios produced by uptake processes: a general model applied to beta-adrenoceptor agonists. Br J Pharmacol. 1980;71(2):407–417. doi: 10.1111/j.1476-5381.1980.tb10953.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Lands A. M., Arnold A., McAuliff J. P., Luduena F. P., Brown T. G., Jr Differentiation of receptor systems activated by sympathomimetic amines. Nature. 1967 May 6;214(5088):597–598. doi: 10.1038/214597a0. [DOI] [PubMed] [Google Scholar]
  12. 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]
  13. 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]
  14. 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]
  15. 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]
  16. O'Donnell S. R., Wanstall J. C. pA2 values of selective beta-adrenoceptor antagonists on isolated atria demonstrate a species difference in the beta-adrenoceptor populations mediating chronotropic responses in cat and guinea-pig. J Pharm Pharmacol. 1979 Oct;31(10):686–690. doi: 10.1111/j.2042-7158.1979.tb13629.x. [DOI] [PubMed] [Google Scholar]
  17. Raper C., McPherson G. A., Iakovidis D. A phenoxypropanolamine derivative (RO363) with selective beta1-receptor stimulant actions. Eur J Pharmacol. 1978 Nov 15;52(2):241–242. doi: 10.1016/0014-2999(78)90214-5. [DOI] [PubMed] [Google Scholar]

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