Mechanisms of blockade of excitatory amino acid receptor channels
Abstract
Ion channels coupled to NMDA, kainate and AMPA receptors are the target of pharmacological regulation by a variety of drugs and ions. While these channels are all nonselectively permeated by Na+ and K+ ions, the NMDA receptor-channel complex contains a number of pharmacological sites distinct from those found on the others. For example, Mg2+ ions rapidly and reversibly block open NMDA channels in a highly voltage-dependent manner. Its extreme voltage dependence suggests that the Mg2+ binding site lies deep within the ion channel pore. By contrast the voltage-dependent block of activated channels by the dissociative anesthetic 'slow channel blockers' has unusual characteristics. In the fourth article in our series on excitatory amino acids, John MacDonald and Linda Nowak analyse the characteristics of these two types of block and describe the hypotheses that have been put forward to explain the mechanisms involved.
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Ketamine blocks NMDARs through an open-channel mechanism and acts as a non-competitive antagonist.
“Ketamine impacts the NMDAR via an open-channel block mechanism which makes it a non-competitive antagonist.”
From Mechanisms of ketamine and its metabolites as antidepressants (2022) · cites this paper as MacDonald & Nowak, 1990
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Ketamine: NMDA Receptors and Beyond
Zorumski, C. F., Izumi, Y., & Mennerick, S. (2016) · The Journal of Neuroscience · doi:10.1523/jneurosci.1547-16.2016 · Cited by 254 · see citing works
Subunit-specific mechanisms and proton sensitivity of NMDA receptor channel block
Dravid, S. M., Erreger, K., Yuan, H., Nicholson, K., Le, P., Lyuboslavsky, P., Almonte, A., Murray, E., Mosley, C., Barber, J., et al. (2007) · The Journal of Physiology · doi:10.1113/jphysiol.2006.124958 · Cited by 184 · see citing works
Mechanisms of ketamine and its metabolites as antidepressants
Hess, E. M., Riggs, L. M., Michaelides, M., & Gould, T. D. (2022) · Biochemical Pharmacology · doi:10.1016/j.bcp.2021.114892 · Cited by 169 · see citing works
The N-methyl-d-aspartate receptor, synaptic plasticity, and depressive disorder
Petrie, R. X. A., Reid, I. C., & Stewart, C. A. (2000) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(00)00063-2 · Cited by 129 · see citing works
Salami, M., Fathollahi, Y., Esteky, H., Motamedi, F., & Atapour, N. (2000) · European Journal of Pharmacology · doi:10.1016/s0014-2999(00)00034-0 · Cited by 15 · see citing works
- Authors
- MacDonald, J. F., & Nowak, L. M.
- Affiliations
- University of Toronto (CA)
- Cornell University (US)
- ORCID
- Nowak, Linda M.
- Venue
- Trends in Pharmacological Sciences
- Publisher
- Elsevier BV
- Published
- 1990-04
- Volume
- 11
- Issue
- 4
- Pages
- 167-172
- ISSN
- 0165-6147 (ISSN-L)
- OpenAlex
- W1993107827
- Cited by
- 198
- References
- 0
- Citations by year
- 2023: 1 · 2021: 1 · 2019: 2 · 2018: 2 · 2017: 1 · 2016: 4 · 2014: 3 · 2013: 2 · 2012: 2
- FWCI
- 2.09
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Trends in Pharmacological Sciences (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Keywords
- glutamate receptors, NMDA receptor, kainate receptors, AMPA receptors, ion channel blockade, magnesium block, dissociative anesthetics, voltage-dependent block, ion channel pore
- MeSH terms
- Animals, Electrophysiology, Humans, Ion Channels, Receptors, Cell Surface, Receptors, Amino Acid
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