Skip to main content
PMC home page
Biochemical Journal logoLink to Biochemical Journal
. 1989 Jun 15;260(3):923–926. doi: 10.1042/bj2600923

MK-801 is a potent nematocidal agent. Characterization of MK-801 binding sites in Caenorhabditis elegans.

J M Schaeffer 1, A R Bergstrom 1, M J Turner 1
PMCID: PMC1138764  PMID: 2669739

Abstract

MK-801, an N-methyl-D-aspartate antagonist in mammalian brain tissue, is a potent nematocidal agent. Specific MK-801 binding sites have been identified and characterized in a membrane fraction prepared from the free-living nematode Caenorhabditis elegans. The high-affinity MK-801 binding site has an apparent dissociation constant, Kd, of 225 nM. Unlike the MK-801 binding site in mammalian tissues, the C. elegans binding site is not effected by glutamate or glycine, and polyamines are potent inhibitors of specific MK-801 binding.

Full text

PDF

Selected References

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

  1. Adams M. E., Carney R. L., Enderlin F. E., Fu E. T., Jarema M. A., Li J. P., Miller C. A., Schooley D. A., Shapiro M. J., Venema V. J. Structures and biological activities of three synaptic antagonists from orb weaver spider venom. Biochem Biophys Res Commun. 1987 Oct 29;148(2):678–683. doi: 10.1016/0006-291x(87)90930-2. [DOI] [PubMed] [Google Scholar]
  2. Bradford M. M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem. 1976 May 7;72:248–254. doi: 10.1006/abio.1976.9999. [DOI] [PubMed] [Google Scholar]
  3. Brenner S. The genetics of Caenorhabditis elegans. Genetics. 1974 May;77(1):71–94. doi: 10.1093/genetics/77.1.71. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Davies J., Watkins J. C. Selective antagonism of amino acid-induced and synaptic excitation in the cat spinal cord. J Physiol. 1979 Dec;297(0):621–635. doi: 10.1113/jphysiol.1979.sp013060. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Foster A. C., Wong E. H. The novel anticonvulsant MK-801 binds to the activated state of the N-methyl-D-aspartate receptor in rat brain. Br J Pharmacol. 1987 Jun;91(2):403–409. doi: 10.1111/j.1476-5381.1987.tb10295.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Huettner J. E., Bean B. P. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988 Feb;85(4):1307–1311. doi: 10.1073/pnas.85.4.1307. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. LOWRY O. H., ROSEBROUGH N. J., FARR A. L., RANDALL R. J. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951 Nov;193(1):265–275. [PubMed] [Google Scholar]
  8. MacDermott A. B., Mayer M. L., Westbrook G. L., Smith S. J., Barker J. L. NMDA-receptor activation increases cytoplasmic calcium concentration in cultured spinal cord neurones. 1986 May 29-Jun 4Nature. 321(6069):519–522. doi: 10.1038/321519a0. [DOI] [PubMed] [Google Scholar]
  9. Nowak L., Bregestovski P., Ascher P., Herbet A., Prochiantz A. Magnesium gates glutamate-activated channels in mouse central neurones. Nature. 1984 Feb 2;307(5950):462–465. doi: 10.1038/307462a0. [DOI] [PubMed] [Google Scholar]
  10. Ransom R. W., Stec N. L. Cooperative modulation of [3H]MK-801 binding to the N-methyl-D-aspartate receptor-ion channel complex by L-glutamate, glycine, and polyamines. J Neurochem. 1988 Sep;51(3):830–836. doi: 10.1111/j.1471-4159.1988.tb01818.x. [DOI] [PubMed] [Google Scholar]
  11. Reynolds I. J., Murphy S. N., Miller R. J. 3H-labeled MK-801 binding to the excitatory amino acid receptor complex from rat brain is enhanced by glycine. Proc Natl Acad Sci U S A. 1987 Nov;84(21):7744–7748. doi: 10.1073/pnas.84.21.7744. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Shaw G. G., Pateman A. J. The regional distribution of the polyamines spermidine and spermine in brain. J Neurochem. 1973 Apr;20(4):1225–1230. doi: 10.1111/j.1471-4159.1973.tb00091.x. [DOI] [PubMed] [Google Scholar]
  13. Wong E. H., Kemp J. A., Priestley T., Knight A. R., Woodruff G. N., Iversen L. L. The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104–7108. doi: 10.1073/pnas.83.18.7104. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Wong E. H., Knight A. R., Ransom R. Glycine modulates [3H]MK-801 binding to the NMDA receptor in rat brain. Eur J Pharmacol. 1987 Oct 27;142(3):487–488. doi: 10.1016/0014-2999(87)90095-1. [DOI] [PubMed] [Google Scholar]
  15. Wong E. H., Knight A. R., Woodruff G. N. [3H]MK-801 labels a site on the N-methyl-D-aspartate receptor channel complex in rat brain membranes. J Neurochem. 1988 Jan;50(1):274–281. doi: 10.1111/j.1471-4159.1988.tb13260.x. [DOI] [PubMed] [Google Scholar]

Articles from Biochemical Journal are provided here courtesy of The Biochemical Society

RESOURCES