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Cooperative Modulation of [3H]MK‐801 Binding to the N‐Methyl‐d‐Aspartate Receptor‐Ion Channel Complex by l‐Glutamate, Glycine, and Polyamines
Abstract
Abstract: In extensively washed rat cortical membranes [3 H](+)‐ 5 ‐ methyl ‐ 10,11 ‐ dihydro ‐ 5 H‐ dibenzo [a,d]cyclohepten‐5,10‐imine ([3 H]MK‐801) labeled a homogeneous set of sites (Bmax=1.86 pmol/mg protein) with relatively low affinity (KD= 45 n M). l‐Glutamate, glycine. and spermidine produced concentration‐dependent increases in specific [3 H]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 [3 H]MK‐801 were reduced to 11 n M, 18 n M, and 15 n M, respectively. Maximally effective concentrations of combinations of the three compounds further increased [3 H]MK‐801 binding affinity as follows: l‐glutamate + glycine, KD= 6.2 n M; l‐glutamate + spermidine, KD= 2.2 n M:
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Citations
Cited by
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Ionotropic and metabotropic glutamate receptor structure and pharmacology
Kew, J. N. C., & Kemp, J. A. (2005) · Psychopharmacology · doi:10.1007/s00213-005-2200-z · Cited by 788
Interactions of polyamines with ion channels
WILLIAMS, K. (1997) · Biochemical Journal · doi:10.1042/bj3250289 · Cited by 498
Beneyto, M., Kristiansen, L. V., Oni-Orisan, A., McCullumsmith, R. E., & Meador-Woodruff, J. H. (2007) · Neuropsychopharmacology · doi:10.1038/sj.npp.1301312 · Cited by 408
Control of Proton Sensitivity of the NMDA Receptor by RNA Splicing and Polyamines
Traynelis, S. F., Hartley, M., & Heinemann, S. F. (1995) · Science · doi:10.1126/science.7754371 · Cited by 406
Metadata
- Authors
- Ransom, R. W., & Stec, N. L.
- Venue
- Journal of Neurochemistry
- Publisher
- Wiley
- Published
- 1988-09
- Volume
- 51
- Issue
- 3
- Pages
- 830-836
- ISSN
- 0022-3042 (ISSN-L)
- 1471-4159
- OpenAlex
- W1964030958
- Cited by
- 750
- References
- 0
- FWCI
- 17.97
- Type
- journal article
- Language
- en
- Open access
- closed
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- Ransom, R. W., & Stec, N. L. (1988). Cooperative Modulation of [3H]MK‐801 Binding to the N‐Methyl‐d‐Aspartate Receptor‐Ion Channel Complex by l‐Glutamate, Glycine, and Polyamines. Journal of Neurochemistry. https://doi.org/10.1111/j.1471-4159.1988.tb01818.x
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