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Spermidine enhancement of [3H]MK-801 binding to the NMDA receptor complex in human cortical membranes.
Eur J Pharmacol. 1990 Sep 18; 189(2-3):195-200.EJ

Abstract

The effects of spermidine on the binding of [3H]MK-801 to the N-methyl-D-aspartate (NMDA) receptor complex was studied in human cerebral cortical membranes. [3H]MK-801 binding was increased from 56 +/- 5 fmol/mg protein (mean +/- S.E.M., n = 7) to 319 +/- 71 fmol/mg protein in the presence of 200 microM spermidine. The ED50 for spermidine stimulation of [3H]MK-801 binding was 89 +/- 22 microM (mean +/- S.E.M., n = 6). In the presence of glutamate (1 microM) plus glycine (1 microM) the ED50 was reduced to 5.5 +/- 0.7 microM. The increase in binding in the presence of spermidine was characterised by an increase in the rate of association of [3H]MK-801. In the presence of spermidine. [3H]MK-801 was inhibited by AP5. 7-chlorokynurenic acid and ifenprodil with IC50 values of 0.5 +/- 0.3 24 +/- 19 and 91 +/- 28 microM, respectively. None of these antagonists was a competitive inhibitor of the spermidine stimulation of [3H]MK-801 binding. Thus spermidine modulates the NMDA receptor complex in human brain, providing further evidence that the complex is similar in rat and human cortex.

Authors+Show Affiliations

Steele JE
Department of Neurochemistry, Institute of Neurology, London, U.K.
Bowen DM
No affiliation info available
Francis PT
No affiliation info available
Green AR
No affiliation info available
Cross AJ
No affiliation info available

MeSH

Adrenergic alpha-AntagonistsAgedAged, 80 and overCerebral CortexDizocilpine MaleateFemaleHumansIn Vitro TechniquesKynurenic AcidMaleMembranesPiperidinesRadioligand AssayReceptors, GlutamateReceptors, N-Methyl-D-AspartateReceptors, NeurotransmitterSpermidine

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1979277

Citation

Steele, J E., et al. "Spermidine Enhancement of [3H]MK-801 Binding to the NMDA Receptor Complex in Human Cortical Membranes." European Journal of Pharmacology, vol. 189, no. 2-3, 1990, pp. 195-200.
Steele JE, Bowen DM, Francis PT, et al. Spermidine enhancement of [3H]MK-801 binding to the NMDA receptor complex in human cortical membranes. Eur J Pharmacol. 1990;189(2-3):195-200.
Steele, J. E., Bowen, D. M., Francis, P. T., Green, A. R., & Cross, A. J. (1990). Spermidine enhancement of [3H]MK-801 binding to the NMDA receptor complex in human cortical membranes. European Journal of Pharmacology, 189(2-3), 195-200.
Steele JE, et al. Spermidine Enhancement of [3H]MK-801 Binding to the NMDA Receptor Complex in Human Cortical Membranes. Eur J Pharmacol. 1990 Sep 18;189(2-3):195-200. PubMed PMID: 1979277.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Spermidine enhancement of [3H]MK-801 binding to the NMDA receptor complex in human cortical membranes. AU - Steele,J E, AU - Bowen,D M, AU - Francis,P T, AU - Green,A R, AU - Cross,A J, PY - 1990/9/18/pubmed PY - 1990/9/18/medline PY - 1990/9/18/entrez SP - 195 EP - 200 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 189 IS - 2-3 N2 - The effects of spermidine on the binding of [3H]MK-801 to the N-methyl-D-aspartate (NMDA) receptor complex was studied in human cerebral cortical membranes. [3H]MK-801 binding was increased from 56 +/- 5 fmol/mg protein (mean +/- S.E.M., n = 7) to 319 +/- 71 fmol/mg protein in the presence of 200 microM spermidine. The ED50 for spermidine stimulation of [3H]MK-801 binding was 89 +/- 22 microM (mean +/- S.E.M., n = 6). In the presence of glutamate (1 microM) plus glycine (1 microM) the ED50 was reduced to 5.5 +/- 0.7 microM. The increase in binding in the presence of spermidine was characterised by an increase in the rate of association of [3H]MK-801. In the presence of spermidine. [3H]MK-801 was inhibited by AP5. 7-chlorokynurenic acid and ifenprodil with IC50 values of 0.5 +/- 0.3 24 +/- 19 and 91 +/- 28 microM, respectively. None of these antagonists was a competitive inhibitor of the spermidine stimulation of [3H]MK-801 binding. Thus spermidine modulates the NMDA receptor complex in human brain, providing further evidence that the complex is similar in rat and human cortex. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/1979277/Spermidine_enhancement_of_[3H]MK_801_binding_to_the_NMDA_receptor_complex_in_human_cortical_membranes_ DB - PRIME DP - Unbound Medicine ER -