Cooperative Modulation of ( 3 H)MK‐801 Binding to the N ‐Methyl‐d‐Aspartate Receptor‐Ion Channel Complex by l‐Glutamate, Glycine, and Polyamines

Cooperative Modulation of ( 3 H)MK‐801 Binding to the N ‐Methyl‐d‐Aspartate... Abstract: In extensively washed rat cortical membranes (3 H)(+)‐ 5 ‐ methyl ‐ 10,11 ‐ dihydro ‐ 5 H‐ dibenzo (a,d)cyclohepten‐5,10‐imine ((3H)MK‐801) labeled a homogeneous set of sites (Bmax=1.86 pmol/mg protein) with relatively low affinity (KD= 45 nM). l‐Glutamate, glycine. and spermidine produced concentration‐dependent increases in specific (3H)MK‐801 binding due to a reduction in the Kd of the radioligand. In the presence of high concentrations of l‐glutamate, glycine, or spermidine, the KD values for (3H)MK‐801 were reduced to 11 nM, 18 nM, and 15 nM, respectively. Maximally effective concentrations of combinations of the three compounds further increased (3H)MK‐801 binding affinity as follows: l‐glutamate + glycine, KD= 6.2 nM; l‐glutamate + spermidine, KD= 2.2 nM: http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Neurochemistry Wiley

Cooperative Modulation of ( 3 H)MK‐801 Binding to the N ‐Methyl‐d‐Aspartate Receptor‐Ion Channel Complex by l‐Glutamate, Glycine, and Polyamines

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Publisher
Wiley
Copyright
Copyright © 1988 Wiley Subscription Services, Inc., A Wiley Company
ISSN
0022-3042
eISSN
1471-4159
D.O.I.
10.1111/j.1471-4159.1988.tb01818.x
Publisher site
See Article on Publisher Site

Abstract

Abstract: In extensively washed rat cortical membranes (3 H)(+)‐ 5 ‐ methyl ‐ 10,11 ‐ dihydro ‐ 5 H‐ dibenzo (a,d)cyclohepten‐5,10‐imine ((3H)MK‐801) labeled a homogeneous set of sites (Bmax=1.86 pmol/mg protein) with relatively low affinity (KD= 45 nM). l‐Glutamate, glycine. and spermidine produced concentration‐dependent increases in specific (3H)MK‐801 binding due to a reduction in the Kd of the radioligand. In the presence of high concentrations of l‐glutamate, glycine, or spermidine, the KD values for (3H)MK‐801 were reduced to 11 nM, 18 nM, and 15 nM, respectively. Maximally effective concentrations of combinations of the three compounds further increased (3H)MK‐801 binding affinity as follows: l‐glutamate + glycine, KD= 6.2 nM; l‐glutamate + spermidine, KD= 2.2 nM:

Journal

Journal of NeurochemistryWiley

Published: Sep 1, 1988

References

  • The novel anticonvulsant MK‐801 binds to the activated state of the N ‐methyl‐d‐aspartate receptor in rat brain
    Foster, Foster; Wong, Wong
  • GABA‐benzodiazepine‐barbiturate receptor interactions
    Olsen, Olsen
  • The attractions of proteins for small molecules and ions
    Scatchard, Scatchard
  • The regional distribution of the polyamines spermidine and spermine in brain
    Shaw, Shaw; Pateman, Pateman
  • ( 3 H)MK‐801 labels a site on the N ‐methyl‐d‐aspartate receptor channel complex in rat brain membranes
    Wong, Wong; Knight, Knight; Woodruff, Woodruff

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