Abstract
1 Four β-adrenoceptor blocking agents, (±)- and (+)-propranolol, practolol and oxprenolol, were found to antagonize, apparently competitively, the responses of both the rat isolated stomach and uterus to 5-hydroxytryptamine (5-HT).
2 The pA2 values for each of these agents as antagonists of the contractile action of 5-HT on the rat stomach were found to be: (±)-propranolol, 6.08; (+)-propranolol, 4.94; practolol, 3.43; and oxprenolol, 5.99. These values were very similar to the corresponding figures for antagonism of 5-HT-induced contractions of the uterus.
3 pA2 values for antagonism of adrenaline-induced relaxations by the four blocking agents on the rat stomach and uterus did not differ from the values for 5-HT blockade.
4 To antagonize contractile responses to acetylcholine of the rat stomach it was necessary to give 100 times more (±)-propranolol than was needed to antagonize responses to 5-HT.
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- ARIENS E. J., VAN ROSSUM J. M. pDx, pAx and pDx values in the analysis of pharmacodynamics. Arch Int Pharmacodyn Ther. 1957 Apr 1;110(2-3):275–299. [PubMed] [Google Scholar]
- ARMITAGE A. K., VANE J. R. A SENSITIVE METHOD FOR THE ASSAY OF CATECHOL AMINES. Br J Pharmacol Chemother. 1964 Feb;22:204–210. doi: 10.1111/j.1476-5381.1964.tb01560.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- ASTROEM A. INFLUENCE OF SOME LOCAL ANESTHETICS UPON THE ADRENALINE CONTRACTION OF ISOLATED STRIPS OF RABBIT AORTA. Acta Physiol Scand. 1964 Jan-Feb;60:30–38. doi: 10.1111/j.1748-1716.1964.tb02866.x. [DOI] [PubMed] [Google Scholar]
- Brunner H., Hedwall P. R., Maier R., Meier M. Pharmacological aspects of oxprenolol. Postgrad Med J. 1970 Nov;(Suppl):5–14. [PubMed] [Google Scholar]
- Dunlop D., Shanks R. G. Selective blockade of adrenoceptive beta receptors in the heart. Br J Pharmacol Chemother. 1968 Jan;32(1):201–218. doi: 10.1111/j.1476-5381.1968.tb00444.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- ERSPAMER V. Pharmacological studies on enteramine (5-hydroxytryptamine) IX. Influence of sympathomimetic and sympatholytic drugs on the physiological and pharmacological actions of enteramine. Arch Int Pharmacodyn Ther. 1953 Apr;93(3-4):293–316. [PubMed] [Google Scholar]
- GYERMEK L. 5-hydroxytryptamine antagonists. Pharmacol Rev. 1961 Sep;13:399–439. [PubMed] [Google Scholar]
- Gay W. S., Rand M. J., Wilson J. Mechanism of the vasoconstrictor action of isoprenaline on an isolated artery preparation. J Pharm Pharmacol. 1967 Jul;19(7):468–473. doi: 10.1111/j.2042-7158.1967.tb08111.x. [DOI] [PubMed] [Google Scholar]
- 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]
- INNES I. R. An action of 5-hydroxytryptamine on adrenaline receptors. Br J Pharmacol Chemother. 1962 Dec;19:427–441. doi: 10.1111/j.1476-5381.1962.tb01447.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Jester J., Horst W. D. Influence of serotonin on adrenergic mechanisms. Biochem Pharmacol. 1972 Feb 1;21(3):333–338. doi: 10.1016/0006-2952(72)90344-9. [DOI] [PubMed] [Google Scholar]
- VANE J. R. A sensitive method for the assay of 5-hydroxytryptamine. Br J Pharmacol Chemother. 1957 Sep;12(3):344–349. doi: 10.1111/j.1476-5381.1957.tb00146.x. [DOI] [PMC free article] [PubMed] [Google Scholar]