Skip to main content
SpringerLink
Log in

Effect of picrotoxinin on benzodiazepine receptor binding

  • Original Articles
  • Published:
Neurochemical Research Aims and scope Submit manuscript

Abstract

The effect of picrotoxinin on [3H]flunitrazepam binding to benzodiazepine receptors was investigated. In mouse forebrain membranes, picrotoxinin inhibited basal, GABA- and pentobarbital-stimulated [3H]flunitrazepam binding; this inhibitory activity was temperature- and chloride ion-dependent. Scatchard analysis of the data indicates that picrotoxinin decreases the number of binding sites without alterating binding affinity. In cerebellar membranes, picrotoxinin did not alter [3H]flunitrazepam receptor binding.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Leeb-Lundberg, F., Napias, C., andR. W. Olsen, 1981. Dihydropicrotoxinin binding sites in mammalian brain: Interaction with convulsant and depressant benzodiazepines. Brain Res. 216:399–408.

    Google Scholar 

  2. Ticku, M. K. 1980. Is the picrotoxinin binding site at the GABA synapse a site of action for barbiturates. Brain Res. Bull. 5 (suppl. 2):919–923.

    Google Scholar 

  3. Leeb-LUNDBERG,F, Snowman, A., andOlsen, R. W. 1980. Barbiturate receptor sites are coupled to benzodiazepine receptors. Proc. Natl. Acad. Sci. USA. 77:7468–7472.

    Google Scholar 

  4. Squires, R. F., andBraestrup, C. 1977. Benzodiazepine receptors in rat brain. Nature 266:732–734.

    Google Scholar 

  5. Skerritt, J. H., andJohnston, A. R. 1983. Interactions of some anesthetic, convulsant, and anticonvulsant drugs at GABA-benzodiazepine receptor-ionophore complexes in rat brain synaptosomal membranes. Neurochem. Res. 8:1351–1362.

    Google Scholar 

  6. Karobath, M., Drexlen, G., andSupavilai, P. 1981. Modulation by picrotoxin and IPTBO of3H-flunitrazepam binding to the GABA/benzodiazepine receptor complex of rat cerebellum. Life Sci. 28:307–313.

    Google Scholar 

  7. Fujimoto, M. andOkabayashi, T. 1981. Effect of picrotoxin on benzodiazepine receptors and GABA receptors with reference to the effect of C1− ion. Life Sci. 28:895–901.

    Google Scholar 

  8. Marangos, P. J., andMartino, A. M. 1981. Studies on the relationship of γ-aminobutyric acid-stimulated diazepam binding and the γ-aminobutyric acid receptor. Mol. Pharmacol. 20:16–21.

    Google Scholar 

  9. Oyama, V. I., andEagle, H. 1956. Measurement of cell growth in tissue culture with a phenol reagent (Folin-ciocalteau). Proc. Soc. Exp. Biol. Med. 91:305–307.

    Google Scholar 

  10. Chweh, A. Y., Swinyard, A. E., andWolf, H. H. 1983. Pentylenetetrazol may discriminate between different types of benzodiazepine receptors. J. Neurochem. 41:830–833.

    Google Scholar 

  11. Ticku, M. K., andOlsen, R. W. 1977. γ-Aminobutyric acid-stimulated chloride permeability in crayfish muscle. Biochim. Biophys. Acta 464:519–529.

    Google Scholar 

  12. Lippa, A. S., Klepner, C. A., Benson, D. I., Critchett, D. J., Sano, M. C., andBeer, B. 1980. The role of GABA in mediating the anticonvulsant properties of benzodiazepines. Brain Res. Bull. 5 (Suppl. 2):861–865.

    Google Scholar 

  13. Braestrup, C., andNielsen, M. 1981. [3H]Propyl-β-carboline-3-carboxylate as a selective radioligand for the BZ1 benzodiazepine receptor subclass. J. Neurochem. 37:333–341.

    Google Scholar 

  14. Niehoff, D. L., Marshal, R. D., Horst, W. D., O'Brien, R. A., Palacios, J. M., andKuhar, M. J. 1982. Binding of a radiolabeled triazolopyridazine to a subtype of benzodiazepine receptor in the cat cerebellum. J. Pharmacol. Exp. Ther. 221:670–675.

    Google Scholar 

  15. Supavilai, P., Mannonen, A., Collins, J. F., andKarobath, M. 1982. Anion-dependent modulation of [3H]muscimol binding and of GABA-stimulated [3H]flunitrazepam binding by picrotoxin and related CNS convulsants. Eur. J. Pharmacol. 81:687–691.

    Google Scholar 

  16. Ramanjaneyulu, R. andTicku, M. K. 1984. Interactions of pentylenetetrazole and tetrazole analogues with the picrotoxinin site of the benzodiazepine-GABA receptorionophore complex. Eur. J. Pharmacol. 98:337–345.

    Google Scholar 

  17. Squires, R. F., Saederup, E., Crawley, J. N., Skolnick, P., andPaul, S. M. 1984. Convulsant potencies of tetrazoles are highly correlated with actions on GABA/benzodiazepine/picrotoxin receptor complexes in brain. Life Sci. 35:1439–1444.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Biochemical Pharmacology and Toxicology College of Pharmacy, University of Utah, 84112, Salt Lake City, Utah

    Andrew Y. Chweh, Rafael A. Ulloque, Ewart A. Swinyard & Harold H. Wolf

Authors
  1. Andrew Y. Chweh
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Rafael A. Ulloque
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Ewart A. Swinyard
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Harold H. Wolf
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Chweh, A.Y., Ulloque, R.A., Swinyard, E.A. et al. Effect of picrotoxinin on benzodiazepine receptor binding. Neurochem Res 10, 871–877 (1985). https://doi.org/10.1007/BF00964624

Download citation

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00964624

Keywords

Search

Navigation