Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1975 Mar;53(3):393–401. doi: 10.1111/j.1476-5381.1975.tb07375.x

Action of beta-adrenoceptor antagonists on the response to isoprenaline in the oestrogen dominated rabbit uterus.

B I Nesheim
PMCID: PMC1666435  PMID: 236797

Abstract

1. Log dose-response curves to isoprenaline from spontaneously contracting muscle strips from rabbit uterus have been obtained. The effects of the alpha-adrenoceptor antagonists phentolamine and phenoxybenzamine, the beta- adrenoceptor antagonists propranolol and practolol, and (+)-propranolol on the log dose-response curves were studied. 2. Phentolamine 5.3 times 10- minus 7 M had a stimulating effect on the muscle strips, moving the log dose-response curve of isoprenaline to the right. Phenoxybenzamine 2.9 times 10- minus 5 M had no effect on the curves. 3. Propranolol 3.4 times 10- minus 6 M had no effect on the curves from circular muscle strips, with either phentolamine 5.4 times 10- minus 7 M or with phenoxybenzamine 2.9 times 10- minus 5 M as alpha-blocker. The curves from the longitudinal muscle strips were shifted somewhat to the right, the same shift, however, being obtained with (+)-propranolol 3.4 times 10- minus 6 M. 4. Practolol 3.8 times 10- minus 6, 3.8 times 10- minus 5 and 3.8 times 10- minus 4 M was without effect on the curves, either in the circular or in the longitudinal strips. 5. It is concluded that neither propranolol at 3.4 times 10- minus 6 M nor practolol act as beta-adrenoceptor antagonists in oestrogen dominated rabbit uterus. In all other tissues investigated, propranolol or practolol block the effect of isoprenaline. Whether the effect of isoprenaline in this tissue may be termed a beta-effect, is then a question of definition. In addition there is no evidence for any extraneuronal uptake mechanisms for isoprenaline. 6. Variations in sensitivity to beta-stimulation with the time of the year were observed, the sensitivity being greatest in the winter and lowest in the summer.

Full text

PDF
393

Selected References

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

  1. Andersson K. E., Ingemarsson I., Persson C. G. Relaxing effects of beta-receptor stimulators in isolated, gravid human myometrium. Life Sci. 1973 Aug 16;13(4):335–344. doi: 10.1016/0024-3205(73)90225-7. [DOI] [PubMed] [Google Scholar]
  2. 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]
  3. Diamond J., Brody T. M. Effect of catecholamines on smooth muscle motility and phosphorylase activity. J Pharmacol Exp Ther. 1966 May;152(2):202–211. [PubMed] [Google Scholar]
  4. 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]
  5. 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]
  6. Hellenbrecht D., Lemmer B., Wiethold G., Grobecker H. Measurement of hydrophobicity, surface activity, local anaesthesia, and myocardial conduction velocity as quantitative parameters of the non-specific membrane affinity of nine -adrenergic blocking agents. Naunyn Schmiedebergs Arch Pharmacol. 1973;277(2):211–226. doi: 10.1007/BF00501161. [DOI] [PubMed] [Google Scholar]
  7. Howe R., Shanks R. G. Optical isomers of propranolol. Nature. 1966 Jun 25;210(5043):1336–1338. doi: 10.1038/2101336a0. [DOI] [PubMed] [Google Scholar]
  8. LEVY B., TOZZI S. THE ADRENERGIC RECEPTIVE MECHANISM OF THE RAT UTERUS. J Pharmacol Exp Ther. 1963 Nov;142:178–184. [PubMed] [Google Scholar]
  9. Langslet A. Membrane stabilization and cardiac effects of d,1-propranolol, d-propranolol and chlorpromazine. Eur J Pharmacol. 1970;13(1):6–14. doi: 10.1016/0014-2999(70)90174-3. [DOI] [PubMed] [Google Scholar]
  10. Levy B. Practolol blockade of cardiac but not vascular or uterine beta-adrenergic receptors in the anesthetized cat. Arch Int Pharmacodyn Ther. 1973 Jul;204(1):143–146. [PubMed] [Google Scholar]
  11. Magaribuchi T., Osa T. Effects of catecholamines on electrical and mechanical activities of the pregnant mouse myometrium. Jpn J Physiol. 1971 Dec;21(6):627–643. doi: 10.2170/jjphysiol.21.627. [DOI] [PubMed] [Google Scholar]
  12. Marshall J. M. Adrenergic innervation of the female reproductive tract: anatomy, physiology and pharmacology. Ergeb Physiol. 1970;62:6–67. doi: 10.1007/BFb0111421. [DOI] [PubMed] [Google Scholar]
  13. Nesheim B. I. Effect of noradrenaline and isoprenaline on the circular and longitudinal muscle of the oestrogen dominated rabbit uterus. Acta Pharmacol Toxicol (Copenh) 1972;31(4):296–304. doi: 10.1111/j.1600-0773.1972.tb00685.x. [DOI] [PubMed] [Google Scholar]
  14. Nesheim B. I., Osnes J. B., Oye I. Role of cyclic adenosine 3',5'-monophosphate in the isoprenaline-induced relaxation of the oestrogen dominated rabbit uterus. Br J Pharmacol. 1975 Mar;53(3):403–407. doi: 10.1111/j.1476-5381.1975.tb07376.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Parker R. B., Waud D. R. Pharmacological estimation of drug-receptor dissociation constants. Statistical evaluation. I. Agonists. J Pharmacol Exp Ther. 1971 Apr;177(1):1–12. [PubMed] [Google Scholar]
  16. Stander R. W., Barden T. P. Adrenergic receptor activity of catecholamines in human gestational myometrium. Obstet Gynecol. 1966 Dec;28(6):768–774. [PubMed] [Google Scholar]
  17. Sullivan S. F., Marshall J. M. Quantitative evaluation of effects of exogenous amines on contractility of human myometrium in vitro. Am J Obstet Gynecol. 1970 May 1;107(1):139–149. doi: 10.1016/s0002-9378(16)33902-3. [DOI] [PubMed] [Google Scholar]
  18. Wasserman M. A., Levy B. Selective beta adrenergic receptor blockade in the rat. J Pharmacol Exp Ther. 1972 Aug;182(2):256–263. [PubMed] [Google Scholar]
  19. Waud D. R., Parker R. B. Pharmacological estimation of drug-receptor dissociation constants. Statistical evaluation. II. Competitive antagonists. J Pharmacol Exp Ther. 1971 Apr;177(1):13–24. [PubMed] [Google Scholar]
  20. Willems J. L., De Schaepdryver A. F. Adrenergic receptors in the oestradiol and allyl-oestrenol dominated rabbit uterus. Arch Int Pharmacodyn Ther. 1966 Jun;161(2):269–274. [PubMed] [Google Scholar]

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

RESOURCES