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N-methyl-D-aspartate receptors: different subunit requirements for binding of glutamate antagonists, glycine antagonists, and channel-blocking agents.
Mol Pharmacol. 1994 Mar; 45(3):540-5.MP

Abstract

Expression of the NR-1 subunit in Xenopus oocytes produces channels that respond to glutamate and are blocked by competitive and noncompetitive antagonists of the N-methyl-D-aspartate (NMDA) receptor. Ionic conductances through these channels are increased by coexpression with NR-2 receptor subunits. We have characterized the pharmacological properties of NMDA receptors assembled from combinations of subunits expressed in transfected cells, to determine the minimum subunit requirements for binding of competitive glutamate antagonists, glycine antagonists, and channel-blocking agents, as detected by ligand-binding experiments. Expression of NR-1a alone produced glycine antagonist binding, whereas the combination of NR-1a and NR-2A was needed to produce binding sites for glutamate antagonists and channel-blocking agents. These results suggest that functional NMDA receptors assemble from these subunits. However, differences in the pharmacological effects of NMDA and polyamines show that not all characteristics of native NMDA receptors are reproduced by this combination of subunits.

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Authors+Show Affiliations

Lynch DR
Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104.
Anegawa NJ
No affiliation info available
Verdoorn T
No affiliation info available
Pritchett DB
No affiliation info available

MeSH

Binding SitesCells, CulturedDizocilpine MaleateExcitatory Amino Acid AntagonistsGlutamatesGlutamic AcidGlycineHumansIon ChannelsKynurenic AcidReceptors, N-Methyl-D-AspartateTransfection

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

7511781

Citation

Lynch, D R., et al. "N-methyl-D-aspartate Receptors: Different Subunit Requirements for Binding of Glutamate Antagonists, Glycine Antagonists, and Channel-blocking Agents." Molecular Pharmacology, vol. 45, no. 3, 1994, pp. 540-5.
Lynch DR, Anegawa NJ, Verdoorn T, et al. N-methyl-D-aspartate receptors: different subunit requirements for binding of glutamate antagonists, glycine antagonists, and channel-blocking agents. Mol Pharmacol. 1994;45(3):540-5.
Lynch, D. R., Anegawa, N. J., Verdoorn, T., & Pritchett, D. B. (1994). N-methyl-D-aspartate receptors: different subunit requirements for binding of glutamate antagonists, glycine antagonists, and channel-blocking agents. Molecular Pharmacology, 45(3), 540-5.
Lynch DR, et al. N-methyl-D-aspartate Receptors: Different Subunit Requirements for Binding of Glutamate Antagonists, Glycine Antagonists, and Channel-blocking Agents. Mol Pharmacol. 1994;45(3):540-5. PubMed PMID: 7511781.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - N-methyl-D-aspartate receptors: different subunit requirements for binding of glutamate antagonists, glycine antagonists, and channel-blocking agents. AU - Lynch,D R, AU - Anegawa,N J, AU - Verdoorn,T, AU - Pritchett,D B, PY - 1994/3/1/pubmed PY - 1994/3/1/medline PY - 1994/3/1/entrez SP - 540 EP - 5 JF - Molecular pharmacology JO - Mol Pharmacol VL - 45 IS - 3 N2 - Expression of the NR-1 subunit in Xenopus oocytes produces channels that respond to glutamate and are blocked by competitive and noncompetitive antagonists of the N-methyl-D-aspartate (NMDA) receptor. Ionic conductances through these channels are increased by coexpression with NR-2 receptor subunits. We have characterized the pharmacological properties of NMDA receptors assembled from combinations of subunits expressed in transfected cells, to determine the minimum subunit requirements for binding of competitive glutamate antagonists, glycine antagonists, and channel-blocking agents, as detected by ligand-binding experiments. Expression of NR-1a alone produced glycine antagonist binding, whereas the combination of NR-1a and NR-2A was needed to produce binding sites for glutamate antagonists and channel-blocking agents. These results suggest that functional NMDA receptors assemble from these subunits. However, differences in the pharmacological effects of NMDA and polyamines show that not all characteristics of native NMDA receptors are reproduced by this combination of subunits. SN - 0026-895X UR - https://www.unboundmedicine.com/medline/citation/7511781/N_methyl_D_aspartate_receptors:_different_subunit_requirements_for_binding_of_glutamate_antagonists_glycine_antagonists_and_channel_blocking_agents_ L2 - http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=7511781 DB - PRIME DP - Unbound Medicine ER -