Skip to main content
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1991 Jan;102(1):19–22. doi: 10.1111/j.1476-5381.1991.tb12125.x

Bicuculline blocks nicotinic acetylcholine response in isolated intermediate lobe cells of the pig.

Z W Zhang 1, P Feltz 1
PMCID: PMC1917877  PMID: 2043922

Abstract

1. The effect of bicuculline on nicotinic acetylcholine (ACh) responses in isolated intermediate lobe (IL) cells of the pig was investigated by use of patch-clamp techniques. Bicuculline was found to reduce ACh-evoked whole-cell currents (IACh) in all cells tested (n = 40). 2. The blocking effect of bicuculline on IACh was dose-dependent, the concentration producing half-maximal blockade being 43.8 microM. 3. The blockade of IACh by bicuculline was not voltage-dependent at membrane potentials above -60 mV, but a slight voltage-dependence was observed at holding potentials (HP) of -80 and -100 mV. 4. The inhibitory effect of bicuculline on IACh was partially competitive at a HP of -60 mV. 5. Neither SR 95531, a pyridazinyl gamma-aminobutyric acid derivative, nor t-butylbicyclophosphorothionate (TBPS) blocked IACh in IL cells. 6. It is concluded that bicuculline interacts directly with the ACh receptor-ionophore complex on porcine IL cells.

Full text

PDF
19

Selected References

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

  1. Benson J. A. Bicuculline blocks the response to acetylcholine and nicotine but not to muscarine or GABA in isolated insect neuronal somata. Brain Res. 1988 Aug 16;458(1):65–71. doi: 10.1016/0006-8993(88)90496-9. [DOI] [PubMed] [Google Scholar]
  2. Bormann J. Electrophysiology of GABAA and GABAB receptor subtypes. Trends Neurosci. 1988 Mar;11(3):112–116. doi: 10.1016/0166-2236(88)90156-7. [DOI] [PubMed] [Google Scholar]
  3. Breuker E., Johnston G. A. Inhibition of acetylcholinesterase by bicuculline and related alkaloids. J Neurochem. 1975 Dec;25(6):903–904. doi: 10.1111/j.1471-4159.1975.tb04427.x. [DOI] [PubMed] [Google Scholar]
  4. Davis M. D., Haas H. L., Lichtensteiger W. The hypothalamohypophyseal system in vitro: electrophysiology of the pars intermedia and evidence for both excitatory and inhibitory inputs. Brain Res. 1985 May 13;334(1):97–104. doi: 10.1016/0006-8993(85)90571-2. [DOI] [PubMed] [Google Scholar]
  5. Demeneix B. A., Desaulles E., Feltz P., Loeffler J. P. Dual population of GABAA and GABAB receptors in rat pars intermedia demonstrated by release of alpha MSH caused by barium ions. Br J Pharmacol. 1984 May;82(1):183–190. doi: 10.1111/j.1476-5381.1984.tb16457.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Demeneix B. A., Taleb O., Loeffler J. P., Feltz P. GABAA and GABAB receptors on porcine pars intermedia cells in primary culture: functional role in modulating peptide release. Neuroscience. 1986 Apr;17(4):1275–1285. doi: 10.1016/0306-4522(86)90094-1. [DOI] [PubMed] [Google Scholar]
  7. Earl J., Large W. A. Electrophysiological investigation of GABA-mediated inhibition at the hermit crab neuromuscular junction. J Physiol. 1974 Jan;236(1):113–127. doi: 10.1113/jphysiol.1974.sp010425. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Godfraind J. M., Krnjević K., Pumain R. Doubtful value of bicuculline as a specific antagonist of GABA. Nature. 1970 Nov 14;228(5272):675–676. doi: 10.1038/228675a0. [DOI] [PubMed] [Google Scholar]
  9. Hamann M., Desarmenien M., Desaulles E., Bader M. F., Feltz P. Quantitative evaluation of the properties of a pyridazinyl GABA derivative (SR 95531) as a GABAA competitive antagonist. An electrophysiological approach. Brain Res. 1988 Mar 1;442(2):287–296. doi: 10.1016/0006-8993(88)91514-4. [DOI] [PubMed] [Google Scholar]
  10. Hamill O. P., Marty A., Neher E., Sakmann B., Sigworth F. J. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch. 1981 Aug;391(2):85–100. doi: 10.1007/BF00656997. [DOI] [PubMed] [Google Scholar]
  11. Hill R. G., Simmonds M. A., Straughan D. W. A comparative study of some convulsant substances as gamma-aminobutyric acid antagonists in the feline cerebral cortex. Br J Pharmacol. 1973 Sep;49(1):37–51. doi: 10.1111/j.1476-5381.1973.tb08266.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Mann E., Enna S. J. Phylogenetic distribution of bicuculline-sensitive gamma-amino-butyric acid (GABA) receptor binding. Brain Res. 1980 Feb 24;184(2):367–373. doi: 10.1016/0006-8993(80)90805-7. [DOI] [PubMed] [Google Scholar]
  13. Mienville J. M., Vicini S. A pyridazinyl derivative of gamma-aminobutyric acid (GABA), SR 95531, is a potent antagonist of Cl- channel opening regulated by GABAA receptors. Neuropharmacology. 1987 Jul;26(7A):779–783. doi: 10.1016/0028-3908(87)90242-5. [DOI] [PubMed] [Google Scholar]
  14. Miller J. J., McLennan H. The action of bicuculline upon acetylcholine-induced excitations of central neurones. Neuropharmacology. 1974 Aug;13(8):785–787. doi: 10.1016/0028-3908(74)90025-2. [DOI] [PubMed] [Google Scholar]
  15. Nistri A., Constanti A. Pharmacological characterization of different types of GABA and glutamate receptors in vertebrates and invertebrates. Prog Neurobiol. 1979;13(2):117–235. doi: 10.1016/0301-0082(79)90016-9. [DOI] [PubMed] [Google Scholar]
  16. Olsen R. W., Ban M., Miller T. Studies on the neuropharmacological activity of bicuculline and related compounds. Brain Res. 1976 Feb 6;102(2):283–299. doi: 10.1016/0006-8993(76)90883-0. [DOI] [PubMed] [Google Scholar]
  17. Olsen R. W., Snowman A. M. [3H]bicuculline methochloride binding to low-affinity gamma-aminobutyric acid receptor sites. J Neurochem. 1983 Dec;41(6):1653–1663. doi: 10.1111/j.1471-4159.1983.tb00877.x. [DOI] [PubMed] [Google Scholar]
  18. Sadoshima J., Tokutomi N., Akaike N. Effects of neostigmine and physostigmine on the acetylcholine receptor-ionophore complex in frog isolated sympathetic neurones. Br J Pharmacol. 1988 Jun;94(2):620–624. doi: 10.1111/j.1476-5381.1988.tb11568.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  19. Shank R. P., Pong S. F., Freeman A. R., Graham L. T., Jr Bicuculline and picrotoxin as antagonists of gamma-aminobutyrate and neuromuscular inhibition in the lobster. Brain Res. 1974 May 31;72(1):71–78. doi: 10.1016/0006-8993(74)90651-9. [DOI] [PubMed] [Google Scholar]
  20. Slater N. T., Filbert M., Carpenter D. O. Multiple interactions of anticholinesterases with Aplysia acetylcholine responses. Brain Res. 1986 Jun 11;375(2):407–412. doi: 10.1016/0006-8993(86)90768-7. [DOI] [PubMed] [Google Scholar]
  21. Squires R. F., Casida J. E., Richardson M., Saederup E. [35S]t-butylbicyclophosphorothionate binds with high affinity to brain-specific sites coupled to gamma-aminobutyric acid-A and ion recognition sites. Mol Pharmacol. 1983 Mar;23(2):326–336. [PubMed] [Google Scholar]
  22. Straughan D. W., Neal M. J., Simmonds M. A., Collins G. G., Hill R. G. Evaluation of bicuculline as a GABA antagonist. Nature. 1971 Oct 1;233(5318):352–354. doi: 10.1038/233352a0. [DOI] [PubMed] [Google Scholar]
  23. Svenneby G., Roberts E. Bicuculline and N-methylbicuculline--competitive inhibitors of brain acetylcholinesterase. J Neurochem. 1973 Oct;21(4):1025–1026. doi: 10.1111/j.1471-4159.1973.tb07551.x. [DOI] [PubMed] [Google Scholar]
  24. Takeuchi A., Onodera K. Effect of bicuculline on the GABA receptor of the crayfish neuromuscular junction. Nat New Biol. 1972 Mar 15;236(63):55–56. doi: 10.1038/newbio236055a0. [DOI] [PubMed] [Google Scholar]
  25. Taraskevich P. S., Douglas W. W. GABA directly affects electrophysiological properties of pituitary pars intermedia cells. Nature. 1982 Oct 21;299(5885):733–734. doi: 10.1038/299733a0. [DOI] [PubMed] [Google Scholar]
  26. Williams P. J., MacVicar B. A., Pittman Q. J. A dopaminergic inhibitory postsynaptic potential mediated by an increased potassium conductance. Neuroscience. 1989;31(3):673–681. doi: 10.1016/0306-4522(89)90432-6. [DOI] [PubMed] [Google Scholar]
  27. Zhang Z. W., Feltz P. Nicotinic acetylcholine receptors in porcine hypophyseal intermediate lobe cells. J Physiol. 1990 Mar;422:83–101. doi: 10.1113/jphysiol.1990.sp017974. [DOI] [PMC free article] [PubMed] [Google Scholar]

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

RESOURCES