Skip to main content
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1982 Nov;77(3):525–529. doi: 10.1111/j.1476-5381.1982.tb09327.x

Anticonvulsant actions of the putative gamma-aminobutyric acid (GABA)-mimetic, ethylenediamine.

P F Morgan, T W Stone
PMCID: PMC2044634  PMID: 6814559

Abstract

1 Ethylenediamine, 31.6-1000 mg/kg intraperitoneally, inhibited the convulsive effects of pentylenetetrazol, 100 mg/kg (i.p.) in mice. 2 Ethylenediamine, 100-1000 mg/kg (i.p.) increased the convulsion threshold to the intravenous infusion of three convulsants in the order pentylenetetrazol greater than bicuculline greater than strychnine. 3 The benzodiazepine antagonist R0 15-1788, 10 mg/kg (i.p.), significantly inhibited the anticonvulsant action of diazepam, 50 micrograms/kg, but not ethylenediamine, 1000 mg/kg. 4 These results clearly indicate that ethylenediamine has anticonvulsant properties and are consistent with the hypothesis that ethylenediamine is a gamma-aminobutyric acid (GABA)-mimetic.

Full text

PDF
525

Selected References

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

  1. Baraldi M., Grandison L., Guidotti A. Distribution and metabolism of muscimol in the brain and other tissues of the rat. Neuropharmacology. 1979 Jan;18(1):57–62. doi: 10.1016/0028-3908(79)90009-1. [DOI] [PubMed] [Google Scholar]
  2. Briley M. S., Langer S. Z. Influence of GABA receptor agonists and antagonists on the binding of 3H-diazepam to the benzodiazepine receptor. Eur J Pharmacol. 1978 Nov 1;52(1):129–132. doi: 10.1016/0014-2999(78)90031-6. [DOI] [PubMed] [Google Scholar]
  3. Costa E., Guidotti A., Mao C. C., Suria A. New concepts on the mechanism of action of benzodiazepines. Life Sci. 1975 Jul 15;17(2):167–185. doi: 10.1016/0024-3205(75)90501-9. [DOI] [PubMed] [Google Scholar]
  4. Haefely W., Kulcsár A., Möhler H., Pieri L., Polc P., Schaffner R. Possible involvement of GABA in the central actions of benzodiazepines. Adv Biochem Psychopharmacol. 1975;(14):131–151. [PubMed] [Google Scholar]
  5. Hunkeler W., Möhler H., Pieri L., Polc P., Bonetti E. P., Cumin R., Schaffner R., Haefely W. Selective antagonists of benzodiazepines. Nature. 1981 Apr 9;290(5806):514–516. doi: 10.1038/290514a0. [DOI] [PubMed] [Google Scholar]
  6. Iversen L. L. GABA and benzodiazepine receptors. Nature. 1978 Oct 12;275(5680):477–477. doi: 10.1038/275477a0. [DOI] [PubMed] [Google Scholar]
  7. Iverson L. L. The present state of tranquility. Nature. 1980 May 29;285(5763):285–286. doi: 10.1038/285285a0. [DOI] [PubMed] [Google Scholar]
  8. LEWIN J., ESPLIN D. W. Analysis of the spinal excitatory action of pentylenetetrazol. J Pharmacol Exp Ther. 1961 May;132:245–250. [PubMed] [Google Scholar]
  9. Lloyd H. G., Perkins M. N., Gaitonde M. K., Stone T. W. Uptake and calcium-dependent release of ethylenediamine (1,2-diaminoethane) by rat brain slices. J Neurochem. 1982 Apr;38(4):1118–1122. doi: 10.1111/j.1471-4159.1982.tb05356.x. [DOI] [PubMed] [Google Scholar]
  10. Lloyd H. G., Perkins M. N., Stone T. W. Ethylenediamine as a specific releasing agent of gamma-aminobutyric acid in rat striatal slices. J Neurochem. 1982 Apr;38(4):1168–1169. doi: 10.1111/j.1471-4159.1982.tb05366.x. [DOI] [PubMed] [Google Scholar]
  11. Maggi A., Enna S. J. Characteristics of muscimol accumulation in mouse brain after systemic administration. Neuropharmacology. 1979 Apr;18(4):361–366. doi: 10.1016/0028-3908(79)90143-6. [DOI] [PubMed] [Google Scholar]
  12. Martin I. L., Candy J. M. Facilitation of benzodiazepine binding by sodium chloride and GABA. Neuropharmacology. 1978 Nov;17(11):993–998. doi: 10.1016/0028-3908(78)90145-4. [DOI] [PubMed] [Google Scholar]
  13. Naik S. R., Guidotti A., Costa E. Central GABA receptor agonists: comparison of muscimol and baclofen. Neuropharmacology. 1976 Aug;15(8):479–484. doi: 10.1016/0028-3908(76)90058-7. [DOI] [PubMed] [Google Scholar]
  14. Nicoll R. A., Padjen A. Pentylenetetrazol: an antagonist of GABA at primary afferents of the isolated frog spinal cord. Neuropharmacology. 1976 Jan;15(1):69–71. doi: 10.1016/0028-3908(76)90099-x. [DOI] [PubMed] [Google Scholar]
  15. Nutt D. J., Cowen P. J., Little H. J. Unusual interactions of benzodiazepine receptor antagonists. Nature. 1982 Feb 4;295(5848):436–438. doi: 10.1038/295436a0. [DOI] [PubMed] [Google Scholar]
  16. Olsen R. W., Ban M., Miller T., Johnston G. A. Chemical instability of the GABA antagonist bicuculline under physiological conditions. Brain Res. 1975 Nov 14;98(2):383–387. doi: 10.1016/0006-8993(75)90019-0. [DOI] [PubMed] [Google Scholar]
  17. Pellmar T. C., Wilson W. A. Synaptic mechanism of pentylenetetrazole: selectivity for chloride conductance. Science. 1977 Aug 26;197(4306):912–914. doi: 10.1126/science.887932. [DOI] [PubMed] [Google Scholar]
  18. Perkins M. N., Bowery N. G., Hill D. R., Stone T. W. Neuronal responses to ethylenediamine: preferential blockade by bicuculline. Neurosci Lett. 1981 May 29;23(3):325–327. doi: 10.1016/0304-3940(81)90019-7. [DOI] [PubMed] [Google Scholar]
  19. Tallman J. F., Paul S. M., Skolnick P., Gallager D. W. Receptors for the age of anxiety: pharmacology of the benzodiazepines. Science. 1980 Jan 18;207(4428):274–281. doi: 10.1126/science.6101294. [DOI] [PubMed] [Google Scholar]
  20. Tallman J. F., Thomas J. W., Gallager D. W. GABAergic modulation of benzodiazepine binding site sensitivity. Nature. 1978 Jul 27;274(5669):383–385. doi: 10.1038/274383a0. [DOI] [PubMed] [Google Scholar]
  21. Unnerstall J. R., Pizzi W. J. Muscimol and gamma-hydroxybutyrate: similar interactions with convulsant agents. Life Sci. 1981 Jul 27;29(4):337–344. doi: 10.1016/0024-3205(81)90326-x. [DOI] [PubMed] [Google Scholar]
  22. Worms P., Depoortere H., Lloyd K. G. Neuropharmacological spectrum of muscimol. Life Sci. 1979 Aug 13;25(7):607–614. doi: 10.1016/0024-3205(79)90555-1. [DOI] [PubMed] [Google Scholar]

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

RESOURCES