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. 1980 Oct;70(2):313–321. doi: 10.1111/j.1476-5381.1980.tb07938.x

The selective anti-muscarinic action of stercuronium

CK Li, F Mitchelson
PMCID: PMC2044327  PMID: 6893558

Abstract

1 The antimuscarinic activity of stercuronium, a competitive neuromuscular blocking drug, has been compared in the anaesthetized guinea-pig, guinea-pig atria, bladder and ileum, rabbit atria and the sympathetically innervated rabbit ear artery preparation using carbachol (CCh) as agonist.

2 In the anaesthetized guinea-pig, stercuronium (0.2 and 2.0 μmol/kg) produced significantly greater inhibition (P < 0.05) of the bradycardia than of the vasodepressor response produced by CCh, the difference being 2 fold at the low dose and 5.8 fold at the higher dose.

3 In guinea-pig atria the negative chronotropic response to CCh was inhibited to a similar degree to the negative inotropic response by stercuronium, whereas in bladder and ileum stercuronium was 17 fold less active as an antimuscarinic drug.

4 The affinity of stercuronium for the prejunctional muscarinic receptor on sympathetic nerve endings in the rabbit ear artery was similar to that for the muscarinic receptor mediating negative inotropic responses to CCh in the rabbit left atrium, and 2.3 fold less than the affinity for the muscarinic receptors in guinea-pig atria.

5 A similar trend was observed with gallamine, another neuromuscular blocking drug, when results obtained in the rabbit ear artery preparation were compared to previously reported data. Also, the affinity of gallamine for muscarinic receptors mediating relaxation of the cat anococcygeus muscle was found to be similar to that for prejunctional muscarinic receptors in the rabbit ear artery.

6 It is suggested that stercuronium and gallamine have a greater affinity for cardiac receptors and the inhibitory muscarinic receptors on sympathetic nerve endings than for muscarinic receptors mediating contraction of bladder and ileum.

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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. Barlow R. B., Berry K. J., Glenton P. A., Nilolaou N. M., Soh K. S. A comparison of affinity constants for muscarine-sensitive acetylcholine receptors in guinea-pig atrial pacemaker cells at 29 degrees C and in ileum at 29 degrees C and 37 degrees C. Br J Pharmacol. 1976 Dec;58(4):613–620. doi: 10.1111/j.1476-5381.1976.tb08631.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Carrier G. O., Ahlquist R. P. The influence of extracellular calcium on muscarinic receptors in vascular smooth muscle. Arch Int Pharmacodyn Ther. 1976 Oct;223(2):223–230. [PubMed] [Google Scholar]
  4. Clark A. L., Mitchelson F. The inhibitory effect of gallamine on muscarinic receptors. Br J Pharmacol. 1976 Nov;58(3):323–331. doi: 10.1111/j.1476-5381.1976.tb07708.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. De la Lande I. S., Rand M. J. A simple isolated nerve-blood vessel preparation. Aust J Exp Biol Med Sci. 1965 Oct;43(5):639–656. doi: 10.1038/icb.1965.48. [DOI] [PubMed] [Google Scholar]
  6. Fozard J. R., Muscholl E. Effects of several muscarinic agonists on cardiac performance and the release of noradrenaline from sympathetic nerves of the perfused rabbit heart. Br J Pharmacol. 1972 Aug;45(4):616–629. doi: 10.1111/j.1476-5381.1972.tb08119.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Gardier R. W., Tsevdos E. J., Jackson D. B. The effect of pancuronium and gallamine on muscarinic transmission in the superior cervical ganglion. J Pharmacol Exp Ther. 1978 Jan;204(1):46–53. [PubMed] [Google Scholar]
  8. Gillespie J. S., McGrath J. C. The response of the cat anococcygeus muscle to nerve or drug stimulation and a comparison with the rat anococcygeus. Br J Pharmacol. 1974 Jan;50(1):109–118. doi: 10.1111/j.1476-5381.1974.tb09597.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Li C. K., Mitchelson F. Effect of variations in temperature on antimuscarinic activity in guinea-pig atria. Experientia. 1978 May 15;34(5):641–643. doi: 10.1007/BF01937009. [DOI] [PubMed] [Google Scholar]
  10. Li C. K., Mitchelson F. The effect of stercuronium on cardiac muscarinic receptors. Eur J Pharmacol. 1978 Oct 1;51(3):251–259. [PubMed] [Google Scholar]
  11. MCEWEN L. M. The effect on the isolated rabbit heart of vagal stimulation and its modification by cocaine, hexamethonium and ouabain. J Physiol. 1956 Mar 28;131(3):678–689. doi: 10.1113/jphysiol.1956.sp005493. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Madden J., Mitchelson F. The interaction of hemicholinium-3 (HC-3) with cholinomimetics and atropine. Eur J Pharmacol. 1975 May;32(1):17–29. doi: 10.1016/0014-2999(75)90318-0. [DOI] [PubMed] [Google Scholar]
  13. Marshall I. G. The ganglion blocking and vagolytic actions of three short-acting neuromuscular blocking drugs in the cat. J Pharm Pharmacol. 1973 Jul;25(7):530–536. doi: 10.1111/j.2042-7158.1973.tb09152.x. [DOI] [PubMed] [Google Scholar]
  14. Paton W. D., Zar M. A. The origin of acetylcholine released from guinea-pig intestine and longitudinal muscle strips. J Physiol. 1968 Jan;194(1):13–33. doi: 10.1113/jphysiol.1968.sp008392. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. RIKER W. F., Jr, WESCOE W. C. The pharmacology of Flaxedil, with observations on certain analogs. Ann N Y Acad Sci. 1951 Oct;54(3):373–394. doi: 10.1111/j.1749-6632.1951.tb39932.x. [DOI] [PubMed] [Google Scholar]
  16. Rathbun F. J., Hamilton J. T. Effect of gallamine on cholinergic receptors. Can Anaesth Soc J. 1970 Nov;17(6):574–590. doi: 10.1007/BF03004717. [DOI] [PubMed] [Google Scholar]
  17. Saxena P. R., Bonta I. L. Mechanism of selective cardiac vagolytic action of pancuronium bromide. Specific blockade of cardiac muscarinic receptors. Eur J Pharmacol. 1970;11(3):332–341. doi: 10.1016/0014-2999(70)90009-9. [DOI] [PubMed] [Google Scholar]
  18. Steinsland O. S., Furchgott R. F., Kirpekar S. M. Inhibition of adrenergic neurotransmission by parasympathomimetics in the rabbit ear artery. J Pharmacol Exp Ther. 1973 Feb;184(2):346–356. [PubMed] [Google Scholar]
  19. Steinsland O. S., Furchgott R. F. Vasoconstriction of the isolated rabbit ear artery caused by nicotinic agonists acting on adrenergic neurons. J Pharmacol Exp Ther. 1975 Apr;193(1):128–137. [PubMed] [Google Scholar]
  20. Vanhoutee P. M., Verbeuren T. J. Inhibition by acetylcholine of the norepinephrine release evoked by potassium in canine saphenous veins. Circ Res. 1976 Aug;39(2):263–269. doi: 10.1161/01.res.39.2.263. [DOI] [PubMed] [Google Scholar]

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