Structure-activity relationships for amino acid transmitter candidates acting at N-methyl-D-aspartate and quisqualate receptors

QUICK SEARCH:

[advanced]

	Author:		Keyword(s):
Year:		Vol:		Page:

HOME | SEARCH | ARCHIVE | SUBSCRIBE | CONTACT | HELP

This Article

Full Text (PDF)

Submit an eLetter

Alert me when this article is cited

Alert me when eLetters are posted

Alert me if a correction is posted

Citation Map

Services

Email this article to a friend

Similar articles in this journal

Similar articles in PubMed

Alert me to new issues of the journal

Download to citation manager

Citing Articles

Citing Articles via HighWire

Citing Articles via Google Scholar

Google Scholar

Articles by Patneau, D. K.

Articles by Mayer, M. L.

Search for Related Content

PubMed

PubMed Citation

Articles by Patneau, D. K.

Articles by Mayer, M. L.

Previous Article | Next Article

Journal of Neuroscience, Vol 10, 2385-2399, Copyright © 1990 by Society for Neuroscience

ARTICLE

Structure-activity relationships for amino acid transmitter candidates acting at N-methyl-D-aspartate and quisqualate receptors

DK Patneau and ML Mayer
Unit of Neurophysiology and Biophysics, NICHD, National Institutes of Health, Bethesda, Maryland 20892.
Dose-response curves for activation of excitatory amino acid receptors on mouse embryonic hippocampal neurons in culture were recorded for 15 excitatory amino acids, including the L-isomers of glutamate, aspartate, and a family of endogenous sulfur amino acids. In the presence of 3 microM glycine, with no extracellular Mg, micromolar concentrations of 11 of these amino acids produced selective activation of N-methyl-D-aspartate (NMDA) receptors. L-Glutamate was the most potent NMDA agonist (EC50 2.3 microM) and quinolinic acid the least potent (EC50 2.3 mM). Dose-response curves were well fit by the logistic equation, or by a model with 2 independent agonist binding sites. The mean limiting slope of log-log plots of NMDA receptor current versus agonist concentration (1.93) suggests that a 2-site model is appropriate. There was excellent correlation between agonist EC50S determined in voltage clamp experiments and KdS determined for NMDA receptor binding (Olverman et al., 1988). With no added glycine, and 1 mM extracellular Mg, responses to NMDA were completely blocked; responses to kainate and quisqualate were unchanged. Under these conditions, glutamate and the sulfur amino acids activated a rapidly desensitizing response, similar to that evoked by micromolar concentrations of quisqualate and AMPA, but mM concentrations of L- aspartate, homoquinolinic acid, and quinolinic acid failed to elicit a non-NMDA receptor-mediated response. Except for L-glutamate (EC50 480 microM), the low potency of the sulfur amino acids prevented the study of complete dose-response curves for the rapidly desensitizing response at quisqualate receptors. Small-amplitude nondesensitizing quisqualate receptor responses were activated by much lower concentrations of all quisqualate receptor agonists. Full dose-response curves for the nondesensitizing response were obtained for 9 amino acids; L-glutamate was the most potent endogenous agonist (EC50 19 microM). Domoate (EC50 13 microM) and kainate (EC50 143 microM) activated large-amplitude, nondesensitizing responses.

This article has been cited by other articles:

D. Atasoy, M. Ertunc, K. L. Moulder, J. Blackwell, C. Chung, J. Su, and E. T. Kavalali
Spontaneous and Evoked Glutamate Release Activates Two Populations of NMDA Receptors with Limited Overlap
J. Neurosci., October 1, 2008; 28(40): 10151 - 10166.
[Abstract] [Full Text] [PDF]

T. Miyaji, N. Echigo, M. Hiasa, S. Senoh, H. Omote, and Y. Moriyama
Identification of a vesicular aspartate transporter
PNAS, August 19, 2008; 105(33): 11720 - 11724.
[Abstract] [Full Text] [PDF]

G. Major, A. Polsky, W. Denk, J. Schiller, and D. W. Tank
Spatiotemporally Graded NMDA Spike/Plateau Potentials in Basal Dendrites of Neocortical Pyramidal Neurons
J Neurophysiol, May 1, 2008; 99(5): 2584 - 2601.
[Abstract] [Full Text] [PDF]

P. J. Sjostrom, E. A. Rancz, A. Roth, and M. Hausser
Dendritic Excitability and Synaptic Plasticity
Physiol Rev, April 1, 2008; 88(2): 769 - 840.
[Abstract] [Full Text] [PDF]

D. E. Featherstone and S. A. Shippy
Regulation of Synaptic Transmission by Ambient Extracellular Glutamate
Neuroscientist, April 1, 2008; 14(2): 171 - 181.
[Abstract] [PDF]

G. Busetto, M. J. Higley, and B. L. Sabatini
Developmental presence and disappearance of postsynaptically silent synapses on dendritic spines of rat layer 2/3 pyramidal neurons
J. Physiol., March 15, 2008; 586(6): 1519 - 1527.
[Abstract] [Full Text] [PDF]

K. Erreger, M. T. Geballe, A. Kristensen, P. E. Chen, K. B. Hansen, C. J. Lee, H. Yuan, P. Le, P. N. Lyuboslavsky, N. Micale, et al.
Subunit-Specific Agonist Activity at NR2A-, NR2B-, NR2C-, and NR2D-Containing N-Methyl-D-aspartate Glutamate Receptors
Mol. Pharmacol., October 1, 2007; 72(4): 907 - 920.
[Abstract] [Full Text] [PDF]

M. A. Herman and C. E. Jahr
Extracellular Glutamate Concentration in Hippocampal Slice
J. Neurosci., September 5, 2007; 27(36): 9736 - 9741.
[Abstract] [Full Text] [PDF]

E. J. Schwartz, T. Blackmer, T. Gerachshenko, and S. Alford
Presynaptic G-Protein-Coupled Receptors Regulate Synaptic Cleft Glutamate via Transient Vesicle Fusion
J. Neurosci., May 30, 2007; 27(22): 5857 - 5868.
[Abstract] [Full Text] [PDF]

K. L. Meur, M. Galante, M. C. Angulo, and E. Audinat
Tonic activation of NMDA receptors by ambient glutamate of non-synaptic origin in the rat hippocampus
J. Physiol., April 15, 2007; 580(2): 373 - 383.
[Abstract] [Full Text] [PDF]

S. Moriguchi, M. Nishi, S. Komazaki, H. Sakagami, T. Miyazaki, H. Masumiya, S.-y. Saito, M. Watanabe, H. Kondo, H. Yawo, et al.
Functional uncoupling between Ca2+ release and afterhyperpolarization in mutant hippocampal neurons lacking junctophilins
PNAS, July 11, 2006; 103(28): 10811 - 10816.
[Abstract] [Full Text] [PDF]

M. Ennis, M. Zhu, T. Heinbockel, and A. Hayar
Olfactory Nerve-Evoked, Metabotropic Glutamate Receptor-Mediated Synaptic Responses in Rat Olfactory Bulb Mitral Cells
J Neurophysiol, April 1, 2006; 95(4): 2233 - 2241.
[Abstract] [Full Text] [PDF]

J. M. Christie and G. L. Westbrook
Lateral excitation within the olfactory bulb.
J. Neurosci., February 22, 2006; 26(8): 2269 - 2277.
[Abstract] [Full Text] [PDF]

C. M. McDermott, M. N. Hardy, N. G. Bazan, and J. C. Magee
Sleep deprivation-induced alterations in excitatory synaptic transmission in the CA1 region of the rat hippocampus
J. Physiol., February 1, 2006; 570(3): 553 - 565.
[Abstract] [Full Text] [PDF]

V. F. Safiulina, G. Fattorini, F. Conti, and E. Cherubini
GABAergic Signaling at Mossy Fiber Synapses in Neonatal Rat Hippocampus
J. Neurosci., January 11, 2006; 26(2): 597 - 608.
[Abstract] [Full Text] [PDF]

J. M. Christie and C. E. Jahr
Multivesicular Release at Schaffer Collateral-CA1 Hippocampal Synapses
J. Neurosci., January 4, 2006; 26(1): 210 - 216.
[Abstract] [Full Text] [PDF]

P. Cavelier and D. Attwell
Tonic release of glutamate by a DIDS-sensitive mechanism in rat hippocampal slices
J. Physiol., April 15, 2005; 564(2): 397 - 410.
[Abstract] [Full Text] [PDF]

H. Katsuki, M. Nonaka, H. Shirakawa, T. Kume, and A. Akaike
Endogenous D-Serine Is Involved in Induction of Neuronal Death by N-Methyl-D-aspartate and Simulated Ischemia in Rat Cerebrocortical Slices
J. Pharmacol. Exp. Ther., November 1, 2004; 311(2): 836 - 844.
[Abstract] [Full Text] [PDF]

L. Maggi, E. Sola, F. Minneci, C. Le Magueresse, J. P. Changeux, and E. Cherubini
Persistent decrease in synaptic efficacy induced by nicotine at Schaffer collateral-CA1 synapses in the immature rat hippocampus
J. Physiol., September 15, 2004; 559(3): 863 - 874.
[Abstract] [Full Text] [PDF]

M. Vargas-Caballero and H. P. C. Robinson
Fast and Slow Voltage-Dependent Dynamics of Magnesium Block in the NMDA Receptor: The Asymmetric Trapping Block Model
J. Neurosci., July 7, 2004; 24(27): 6171 - 6180.
[Abstract] [Full Text] [PDF]

G. Popescu and A. Auerbach
The NMDA Receptor Gating Machine: Lessons from Single Channels
Neuroscientist, June 1, 2004; 10(3): 192 - 198.
[Abstract] [PDF]

R. M. Klein and J. R. Howe
Effects of the Lurcher Mutation on GluR1 Desensitization and Activation Kinetics
J. Neurosci., May 26, 2004; 24(21): 4941 - 4951.
[Abstract] [Full Text] [PDF]

T. A. Simeone, R. M. Sanchez, and J. M. Rho
Molecular Biology and Ontogeny of Glutamate Receptors in the Mammalian Central Nervous System
J Child Neurol, May 1, 2004; 19(5): 343 - 360.
[Abstract] [PDF]

C.-C. Kuo, B.-J. Lin, H.-R. Chang, and C.-P. Hsieh
Use-Dependent Inhibition of the N-Methyl-D-aspartate Currents by Felbamate: a Gating Modifier with Selective Binding to the Desensitized Channels
Mol. Pharmacol., February 1, 2004; 65(2): 370 - 380.
[Abstract] [Full Text] [PDF]

A. O. Komendantov, O. G. Komendantova, S. W. Johnson, and C. C. Canavier
A Modeling Study Suggests Complementary Roles for GABAA and NMDA Receptors and the SK Channel in Regulating the Firing Pattern in Midbrain Dopamine Neurons
J Neurophysiol, January 1, 2004; 91(1): 346 - 357.
[Abstract] [Full Text]

G. Lowe
Flash Photolysis Reveals a Diversity of Ionotropic Glutamate Receptors on the Mitral Cell Somatodendritic Membrane
J Neurophysiol, September 1, 2003; 90(3): 1737 - 1746.
[Abstract] [Full Text] [PDF]

M. Vargas-Caballero and H. P. C. Robinson
A Slow Fraction of Mg2+ Unblock of NMDA Receptors Limits Their Contribution to Spike Generation in Cortical Pyramidal Neurons
J Neurophysiol, May 1, 2003; 89(5): 2778 - 2783.
[Abstract] [Full Text] [PDF]

M.-L. He, H. Zemkova, and S. S. Stojilkovic
Dependence of Purinergic P2X Receptor Activity on Ectodomain Structure
J. Biol. Chem., March 14, 2003; 278(12): 10182 - 10188.
[Abstract] [Full Text] [PDF]

K. M. Franks, T. M. Bartol Jr., and T. J. Sejnowski
A Monte Carlo Model Reveals Independent Signaling at Central Glutamatergic Synapses
Biophys. J., November 1, 2002; 83(5): 2333 - 2348.
[Abstract] [Full Text] [PDF]

M.-L. He, T.-a. Koshimizu, M. Tomic', and S. S. Stojilkovic
Purinergic P2X2 Receptor Desensitization Depends on Coupling between Ectodomain and C-Terminal Domain
Mol. Pharmacol., November 1, 2002; 62(5): 1187 - 1197.
[Abstract] [Full Text] [PDF]

A. Araque, E. D. Martin, G. Perea, J. I. Arellano, and W. Buno
Synaptically Released Acetylcholine Evokes Ca2+ Elevations in Astrocytes in Hippocampal Slices
J. Neurosci., April 1, 2002; 22(7): 2443 - 2450.
[Abstract] [Full Text] [PDF]

G. Losi, K. Prybylowski, Z. Fu, J. H. Luo, and S. Vicini
Silent Synapses in Developing Cerebellar Granule Neurons
J Neurophysiol, March 1, 2002; 87(3): 1263 - 1270.
[Abstract] [Full Text] [PDF]

K. Matsui, J. Hasegawa, and M. Tachibana
Modulation of Excitatory Synaptic Transmission by GABAC Receptor-Mediated Feedback in the Mouse Inner Retina
J Neurophysiol, November 1, 2001; 86(5): 2285 - 2298.
[Abstract] [Full Text] [PDF]

A. Bal-Price and G. C. Brown
Inflammatory Neurodegeneration Mediated by Nitric Oxide from Activated Glia-Inhibiting Neuronal Respiration, Causing Glutamate Release and Excitotoxicity
J. Neurosci., September 1, 2001; 21(17): 6480 - 6491.
[Abstract] [Full Text] [PDF]

E. C. Ihle and D. K. Patneau
Modulation of alpha -Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptor Desensitization by Extracellular Protons
Mol. Pharmacol., April 13, 2001; 58(6): 1204 - 1212.
[Abstract] [Full Text]

N. Chen, J. Ren, L. A. Raymond, and T. H. Murphy
Changes in Agonist Concentration Dependence That Are a Function of Duration of Exposure Suggest N-Methyl-D-aspartate Receptor Nonsaturation during Synaptic Stimulation
Mol. Pharmacol., February 1, 2001; 59(2): 212 - 219.
[Abstract] [Full Text]

A. Meini, A. Benocci, M. Frosini, G. Sgaragli, G. Pessina, C. Aldinucci, G. T. Youmbi, and M. Palmi
Nitric Oxide Modulation of Interleukin-1{beta}-Evoked Intracellular Ca2+ Release in Human Astrocytoma U-373 MG Cells and Brain Striatal Slices
J. Neurosci., December 15, 2000; 20(24): 8980 - 8986.
[Abstract] [Full Text] [PDF]

C. D. Hohnke, S. Oray, and M. Sur
Activity-Dependent Patterning of Retinogeniculate Axons Proceeds with a Constant Contribution from AMPA and NMDA Receptors
J. Neurosci., November 1, 2000; 20(21): 8051 - 8060.
[Abstract] [Full Text] [PDF]

J. R. Cottrell, G. R. Dube, C. Egles, and G. Liu
Distribution, Density, and Clustering of Functional Glutamate Receptors Before and After Synaptogenesis in Hippocampal Neurons
J Neurophysiol, September 1, 2000; 84(3): 1573 - 1587.
[Abstract] [Full Text] [PDF]

S. Gasparini, C. Saviane, L. L. Voronin, and E. Cherubini
Silent synapses in the developing hippocampus: Lack of functional AMPA receptors or low probability of glutamate release?
PNAS, August 6, 2000; (2000) 170032297.
[Abstract] [Full Text]

D. Friedman and B. W. Strowbridge
Functional Role of NMDA Autoreceptors in Olfactory Mitral Cells
J Neurophysiol, July 1, 2000; 84(1): 39 - 50.
[Abstract] [Full Text] [PDF]

A. G. Carter and W. G. Regehr
Prolonged Synaptic Currents and Glutamate Spillover at the Parallel Fiber to Stellate Cell Synapse
J. Neurosci., June 15, 2000; 20(12): 4423 - 4434.
[Abstract] [Full Text] [PDF]

T. C. Smith, L.-Y. Wang, and J. R. Howe
Heterogeneous Conductance Levels of Native AMPA Receptors
J. Neurosci., March 15, 2000; 20(6): 2073 - 2085.
[Abstract] [Full Text] [PDF]

L. L. Thio, M. Wong, and K. A. Yamada
Ketone bodies do not directly alter excitatory or inhibitory hippocampal synaptic transmission
Neurology, January 25, 2000; 54(2): 325 - 325.
[Abstract] [Full Text] [PDF]

R. Nahum-Levy, L. H. Fossom, P. Skolnick, and M. Benveniste
Putative Partial Agonist 1-Aminocyclopropanecarboxylic Acid Acts Concurrently as a Glycine-Site Agonist and a Glutamate-Site Antagonist at N-Methyl-D-aspartate Receptors
Mol. Pharmacol., December 1, 1999; 56(6): 1207 - 1218.
[Abstract] [Full Text]

M. Yuzaki and J. A. Connor
Characterization of L-Homocysteate-Induced Currents in Purkinje Cells From Wild-Type and NMDA Receptor Knockout Mice
J Neurophysiol, November 1, 1999; 82(5): 2820 - 2826.
[Abstract] [Full Text] [PDF]

S. Mennerick, W. Shen, W. Xu, A. Benz, K. Tanaka, K. Shimamoto, K. E. Isenberg, J. E. Krause, and C. F. Zorumski
Substrate Turnover by Transporters Curtails Synaptic Glutamate Transients
J. Neurosci., November 1, 1999; 19(21): 9242 - 9251.
[Abstract] [Full Text] [PDF]

L. S. Overstreet, G. A. Kinney, Y.-B. Liu, D. Billups, and N. T. Slater
Glutamate Transporters Contribute to the Time Course of Synaptic Transmission in Cerebellar Granule Cells
J. Neurosci., November 1, 1999; 19(21): 9663 - 9673.
[Abstract] [Full Text] [PDF]

L. M. Hawkins, P. L. Chazot, and F. A. Stephenson
Biochemical Evidence for the Co-association of Three N-Methyl-D-aspartate (NMDA) R2 Subunits in Recombinant NMDA Receptors
J. Biol. Chem., September 17, 1999; 274(38): 27211 - 27218.
[Abstract] [Full Text] [PDF]

M. G. Espey, R. J. Ellis, R. K. Heaton, and A. S. Basile
Relevance of glutamate levels in the CSF of patients with HIV-1-associated dementia complex
Neurology, September 1, 1999; 53(5): 1144 - 1144.
[Abstract] [Full Text]

K. Matsui, N. Hosoi, and M. Tachibana
Active Role of Glutamate Uptake in the Synaptic Transmission from Retinal Nonspiking Neurons
J. Neurosci., August 15, 1999; 19(16): 6755 - 6766.
[Abstract] [Full Text] [PDF]

V. Aroniadou-Anderjaska, M. Ennis, and M. T. Shipley
Dendrodendritic Recurrent Excitation in Mitral Cells of the Rat Olfactory Bulb
J Neurophysiol, July 1, 1999; 82(1): 489 - 494.
[Abstract] [Full Text] [PDF]

Y. Yamada, Y. Chochi, K. Takamiya, K. Sobue, and M. Inui
Modulation of the Channel Activity of the epsilon 2/zeta 1-Subtype N-Methyl D-Aspartate Receptor by PSD-95
J. Biol. Chem., March 5, 1999; 274(10): 6647 - 6652.
[Abstract] [Full Text] [PDF]

R. Dingledine, K. Borges, D. Bowie, and S. F. Traynelis
The Glutamate Receptor Ion Channels
Pharmacol. Rev., March 1, 1999; 51(1): 7 - 62.
[Abstract] [Full Text] [PDF]

Y.-X. Li, Y. Zhang, H. A. Lester, E. M. Schuman, and N. Davidson
Enhancement of Neurotransmitter Release Induced by Brain-Derived Neurotrophic Factor in Cultured Hippocampal Neurons
J. Neurosci., December 15, 1998; 18(24): 10231 - 10240.
[Abstract] [Full Text] [PDF]

R. Rao-Mirotznik, G. Buchsbaum, and P. Sterling
Transmitter Concentration at a Three-Dimensional Synapse
J Neurophysiol, December 1, 1998; 80(6): 3163 - 3172.
[Abstract] [Full Text] [PDF]

W. Danysz and C. G. Parsons
Glycine and N-Methyl-D-Aspartate Receptors: Physiological Significance and Possible Therapeutic Applications
Pharmacol. Rev., December 1, 1998; 50(4): 597 - 664.
[Abstract] [Full Text] [PDF]

P. Saltiel, M. C. Tresch, and E. Bizzi
Spinal Cord Modular Organization and Rhythm Generation: An NMDA Iontophoretic Study in the Frog
J Neurophysiol, November 1, 1998; 80(5): 2323 - 2339.
[Abstract] [Full Text] [PDF]

S. Rumpel, H. Hatt, and K. Gottmann
Silent Synapses in the Developing Rat Visual Cortex: Evidence for Postsynaptic Expression of Synaptic Plasticity
J. Neurosci., November 1, 1998; 18(21): 8863 - 8874.
[Abstract] [Full Text] [PDF]

P. Q. Trombley
Selective Modulation of GABAA Receptors by Aluminum
J Neurophysiol, August 1, 1998; 80(2): 755 - 761.
[Abstract] [Full Text] [PDF]