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. 1978 Jun;63(2):309–314. doi: 10.1111/j.1476-5381.1978.tb09762.x

Anatagonism of the inhibitory effects of adenosine 5'-triphosphate on the isolated taenia of the guinea-pig caecum: structure-activity relationships within a series of isatogen derivatives.

H E Foster, M Hooper, M Spedding, A J Sweetman, D F Weetman
PMCID: PMC1668415  PMID: 667422

Abstract

1 A series of eight isatogen derivatives was studied on isolated tissues taken from guinea-pigs. The ability of the compounds to relax the taenia, to inhibit adenosine 5'-diphosphate (ADP)-stimulated respiration in mitochondria and to antagonize the inhibitory effects of adenosine 5'-triphosphate (ATP) on smooth muscle was measured. 2 All the derivatives inhibited ADP-stimulated respiration in mitochondria and relaxed the smooth muscle. These two effects were found to be significantly correlated. 3 Only half the compounds blocked the inhibitory effects of ATP, and all of these had a chemically reactive group (nitro, methoxy or pyridyl) in the 2'2-position. 2-2'-Pyridylisatogen was the most effective blocking agent. 4 The blockade of the inhibitory effects of ATP is not related to the other actions of the derivatives.

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Selected References

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

  1. BULBRING E., LULLMANN H. The effect of metabolic inhibitors on the electrical and mechanical activity of the smooth muscle of the guinea-pig's taenia coli. J Physiol. 1957 Apr 30;136(2):310–323. doi: 10.1113/jphysiol.1957.sp005762. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Bennett A., Posner J. Studies on prostaglandin antagonists. Br J Pharmacol. 1971 Aug;42(4):584–594. doi: 10.1111/j.1476-5381.1971.tb07142.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Bond C. C., Hooper M. Isatogens. VI. Synthesis of isatogens via tolan (diphenylacetylene) intermediates. J Chem Soc Perkin 1. 1969;18:2453–2460. doi: 10.1039/j39690002453. [DOI] [PubMed] [Google Scholar]
  4. CHUJYO N., HOLLAND W. C. Potassium-induced contracture and calcium exchange in the guinea pig's taenia coli. Am J Physiol. 1963 Jul;205:94–100. doi: 10.1152/ajplegacy.1963.205.1.94. [DOI] [PubMed] [Google Scholar]
  5. Eckenfels A., Vane J. R. Prostaglandins, oxygen tension and smooth muscle tone. Br J Pharmacol. 1972 Jul;45(3):451–462. doi: 10.1111/j.1476-5381.1972.tb08101.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Ferreira S. H., Herman A. G., Vane J. R. Prostaglandin production by rabbit isolated jejunum and its relationship to the inherent tone of the preparation. Br J Pharmacol. 1976 Apr;56(4):469–477. doi: 10.1111/j.1476-5381.1976.tb07459.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. 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]
  8. Spedding M., Sweetman A. J., Weetman D. F. Antagonism of adenosine 5'-triphosphate-induced relaxation by 2-2'-pyridylisatogen in the taenia of guinea-pig caecum. Br J Pharmacol. 1975 Apr;53(4):575–583. doi: 10.1111/j.1476-5381.1975.tb07397.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Splawinski J. A., Nies A. S., Sweetman B., Oates J. A. The effects of arachidonic acid, prostaglandin E2 and prostaglandin F2alpha on the longitudinal stomach strip of the rat. J Pharmacol Exp Ther. 1973 Dec;187(3):501–510. [PubMed] [Google Scholar]
  10. Sweetman A. J., Green A. P., Hooper M. The effect of 2-phenylisatogen on oxidative phosphorylation in rat liver mitochondria. FEBS Lett. 1971 May 20;14(5):306–308. doi: 10.1016/0014-5793(71)80286-7. [DOI] [PubMed] [Google Scholar]
  11. VAN ROSSUM J. M. Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters. Arch Int Pharmacodyn Ther. 1963;143:299–330. [PubMed] [Google Scholar]
  12. Weetman D. F., Turner N. The effects of inhibitors of adenosine 5'-triphosphate biosynthesis on the responses of the guinea-pig isolated bladder and some other preparations to nerve stimulation. Arch Int Pharmacodyn Ther. 1974 Jul;210(1):12–26. [PubMed] [Google Scholar]

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