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. 1985 Jan;84(1):227–235.

Responses to the beta 2-selective agonist procaterol of vascular and atrial preparations with different functional beta-adrenoceptor populations.

S R O'Donnell, J C Wanstall
PMCID: PMC1987226  PMID: 2858232

Abstract

Relaxant responses to the beta-adrenoceptor agonist, procaterol, have been examined on preparations of guinea-pig pulmonary artery (beta 2-adrenoceptors only), rat and rabbit pulmonary artery and rat aorta (beta 2 greater than beta 1), and these responses have been compared with responses of dog left circumflex coronary artery (beta 1 only). Low concentrations of procaterol (3 nM to 100 nM) relaxed KC1-contracted preparations of rat aorta and pulmonary artery from rat, rabbit and guinea-pig whereas high concentrations (greater than 1 microM) were required to relax preparations of the dog left circumflex coronary artery. The dissociation constant (KP value) for procaterol on beta 1-adrenoceptors was 4.9 microM (determined on dog coronary artery) and on beta 2-adrenoceptors was 0.008 microM (rabbit pulmonary artery). Procaterol therefore had a beta 2:beta 1 selectivity value of 612. KP values obtained on guinea-pig atria for procaterol, on which the concentration-response curve was biphasic, confirmed that both beta 2- and beta 1-adrenoceptors mediate responses of this tissue. The KP values were 0.009 microM (data from the first phase of the control concentration-response curve) and 3.5 microM (data from the concentration-response curve in the presence of the beta 2-selective antagonist, ICI 118,551, 10 nM). Data obtained on rat atria indicated that chronotropic responses of preparations from some rats, but not others, involved a minor population of beta 2-adrenoceptors, but the beta 2-adrenoceptors, when present, were less important than in guinea-pig atria.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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  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. Bryan L. J., Cole J. J., O'Donnell S. R., Wanstall J. C. A study designed to explore the hypothesis that beta-1 adrenoceptors are "innervated" receptors and beta-2 adrenoceptors are "hormonal" receptors. J Pharmacol Exp Ther. 1981 Feb;216(2):395–400. [PubMed] [Google Scholar]
  3. Costin B. I., O'Donnell S. R., Wanstall J. C. Chronotropic responses of rabbit isolated atria to beta-adrenoceptor agonists are mediated by only beta 1-adrenoceptors. J Pharm Pharmacol. 1983 Nov;35(11):752–754. doi: 10.1111/j.2042-7158.1983.tb02886.x. [DOI] [PubMed] [Google Scholar]
  4. Dickinson K. E., Nahorski S. R. Atypical characteristics of frog and chick erythrocyte beta-adrenoceptors. Eur J Pharmacol. 1981 Aug 27;74(1):43–52. doi: 10.1016/0014-2999(81)90321-6. [DOI] [PubMed] [Google Scholar]
  5. Hedberg A., Minneman K. P., Molinoff P. B. Differential distribution of beta-1 and beta-2 adrenergic receptors in cat and guinea-pig heart. J Pharmacol Exp Ther. 1980 Mar;212(3):503–508. [PubMed] [Google Scholar]
  6. Johansson L. H., Persson H. Beta 2-adrenoceptors in guinea-pig atria. J Pharm Pharmacol. 1983 Dec;35(12):804–807. doi: 10.1111/j.2042-7158.1983.tb02900.x. [DOI] [PubMed] [Google Scholar]
  7. Kenakin T. P., Beek D. Is prenalterol (H133/80) really a selective beta 1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships. J Pharmacol Exp Ther. 1980 May;213(2):406–413. [PubMed] [Google Scholar]
  8. Kenakin T. P. Theoretical and practical problems with the assessment of intrinsic efficacy of agonists: efficacy of reputed beta-1 selective adrenoceptor agonists for beta-2 adrenoceptors. J Pharmacol Exp Ther. 1982 Nov;223(2):416–423. [PubMed] [Google Scholar]
  9. Krstew E., Malta E., Raper C. Comparison of guinea pig uterine and rat vas deferens preparations for assessment of beta 2-adrenoceptor-mediated activity. J Pharmacol Methods. 1982 Dec;8(4):279–289. doi: 10.1016/0160-5402(82)90045-6. [DOI] [PubMed] [Google Scholar]
  10. MacKay D. How should values of pA2 and affinity constants for pharmacological competitive antagonists be estimated? J Pharm Pharmacol. 1978 May;30(5):312–313. doi: 10.1111/j.2042-7158.1978.tb13237.x. [DOI] [PubMed] [Google Scholar]
  11. Minneman K. P., Hedberg A., Molinoff P. B. Comparison of beta adrenergic receptor subtypes in mammalian tissues. J Pharmacol Exp Ther. 1979 Dec;211(3):502–508. [PubMed] [Google Scholar]
  12. O'Donnell S. R., Wanstall J. C. Beta-1 and beta-2 adrenoceptor-mediated responses in preparations of pulmonary artery and aorta from young and aged rats. J Pharmacol Exp Ther. 1984 Mar;228(3):733–738. [PubMed] [Google Scholar]
  13. O'Donnell S. R., Wanstall J. C. Demonstration of both beta 1- and beta 2-adrenoceptors mediating relaxation of isolated ring preparations of rat pulmonary artery. Br J Pharmacol. 1981 Nov;74(3):547–552. doi: 10.1111/j.1476-5381.1981.tb10463.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. 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]
  15. O'Donnell S. R., Wanstall J. C. Pharmacological approaches to the characterization of beta-adrenoreceptor populations in tissues. J Auton Pharmacol. 1981 Sep;1(4):305–312. doi: 10.1111/j.1474-8673.1981.tb00460.x. [DOI] [PubMed] [Google Scholar]
  16. 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]
  17. O'Donnell S. R., Wanstall J. C. The classification of beta-adrenoceptors in isolated ring preparations of canine coronary arteries. Br J Pharmacol. 1984 Apr;81(4):637–644. doi: 10.1111/j.1476-5381.1984.tb16129.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  18. Yabuuchi Y. The beta-adrenoceptor stimulant properties of OPC-2009 on guinea-pig isolated tracheal, right atrial and left atrial preparations. Br J Pharmacol. 1977 Dec;61(4):513–521. doi: 10.1111/j.1476-5381.1977.tb07543.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

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