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   Is ketamine a non-competitive channel blocker of NMDA receptors?

   • This article has been updated Ketamine is a non-competitive channel blocker of N -methyl- d -aspartate (NMDA) receptors 1. A single sub-anaesthetic dose of ketamine produces rapid (within hours) and long-lasting antidepressant effects in patients who are resistant to other antidepressants 2, 3.

   Structural basis of ketamine action on human NMDA receptors

   www.nature.com/articles/s41586-021-03769-9

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   Which NMDA receptor is responsible for ketamine's more specific properties?

   • The antagonism of NMDA receptor is responsible for ketamine's more specific properties. Ketamine decreases the “wind up” phenomenon, and the antagonism is more important if the NMDA channel has been previously opened by the glutamate binding (“use dependence”).

   Ketamine Pharmacology: An Update (Pharmacodynamics and Molecular

   www.ncbi.nlm.nih.gov/pmc/articles/PMC6493357/

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   What are NMDA receptor antagonists?

   • NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the N -Methyl- D -aspartate receptor ( NMDAR ). They are commonly used as anesthetics for humans and non-human animals; the state of anesthesia they induce is referred to as dissociative anesthesia.

   NMDA receptor antagonist - Wikipedia

   en.wikipedia.org/wiki/NMDA_receptor_antagonist

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   How to trap NMDA receptors in the ketamine-bound state?

   • To trap the NMDA receptors in the ketamine-bound state, we pre-incubated the purified protein with glycine and glutamate (1 mM each) in the presence of S -ketamine (5 mM), which is 3–5 times more potent than R -ketamine 17. Next, we vitrified the protein and collected the structural data sets using cryo-EM.

   Structural basis of ketamine action on human NMDA receptors

   www.nature.com/articles/s41586-021-03769-9

   See all results for this question

2. en.wikipedia.org › wiki › NMDA_receptor_antagonistNMDA receptor antagonist - Wikipedia

   en.wikipedia.org › wiki › NMDA_receptor_antagonist

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   Ketamine, one of the most popular NMDA receptor antagonists. NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the N-Methyl-D-aspartate receptor . They are commonly used as anesthetics for humans and non-human animals; the state of anesthesia they induce is referred to as dissociative anesthesia.

3. www.nature.com › articles › s41586/021/03769-9Structural basis of ketamine action on human NMDA receptors

   www.nature.com › articles › s41586/021/03769-9

   Jul 28, 2021 · Ketamine is a non-competitive channel blocker of N -methyl- d -aspartate (NMDA) receptors 1. A single sub-anaesthetic dose of ketamine produces rapid (within hours) and...

   • Author: Youyi Zhang, Fei Ye, Tongtong Zhang, Shiyun Lv, Liping Zhou, Daohai Du, He Lin, Fei Guo, Cheng Luo, ...

   • Publish Year: 2021

4. www.ncbi.nlm.nih.gov › pmc › articlesKetamine: NMDA Receptors and Beyond - PMC

   www.ncbi.nlm.nih.gov › pmc › articles

   Nov 2, 2016 · Studies in the 1980s showed that ketamine is a noncompetitive (uncompetitive) NMDAR antagonist ( Anis et al., 1983) that acts by an open channel block mechanism ( MacDonald et al., 1987 ). Thus, ketamine does not bind closed NMDAR channels but rather requires channels to open to antagonize ( MacDonald et al., 1987 ).

   • Author: Charles F. Zorumski, Yukitoshi Izumi, Steven Mennerick

   • Publish Year: 2016

5. www.ncbi.nlm.nih.gov › books › NBK470357Ketamine - StatPearls - NCBI Bookshelf - National Center for ...

   www.ncbi.nlm.nih.gov › books › NBK470357

   Jan 30, 2024 · Objectives: Identify appropriate indications for ketamine use, recognizing its role in general anesthesia, pain management, and potential applications in psychiatry. Screen patients thoroughly, assessing their medical history and contraindications to determine suitability for ketamine administration.

   • Published: 2024/01/30

6. www.ncbi.nlm.nih.gov › pmc › articlesKetamine Pharmacology: An Update (Pharmacodynamics and ...

   www.ncbi.nlm.nih.gov › pmc › articles

   Apr 10, 2013 · The antagonism of NMDA receptor is responsible for ketamine's more specific properties. Ketamine decreases the “wind up” phenomenon, and the antagonism is more important if the NMDA channel has been previously opened by the glutamate binding (“use dependence”).

   • Author: Georges Mion, Thierry Villevieille
   • DOI: 10.1111/cns.12099

   • Publish Year: 2013
   • Publication: CNS Neurosci Ther. 2013 Jun; 19(6): 370-380.

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8. pubmed.ncbi.nlm.nih.gov › 34321660Structural basis of ketamine action on human NMDA receptors

   pubmed.ncbi.nlm.nih.gov › 34321660

   Ketamine is a non-competitive channel blocker of N-methyl-D-aspartate (NMDA) receptors 1. A single sub-anaesthetic dose of ketamine produces rapid (within hours) and long-lasting antidepressant effects in patients who are resistant to other antidepressants 2,3.

9. www.nature.com › articles › s41386/023/01629-wKetamine and rapid antidepressant action: new treatments and ...

   www.nature.com › articles › s41386/023/01629-w

   Jul 24, 2023 · Ketamine is an open channel blocker of ionotropic glutamatergic N -Methyl- D -Aspartate (NMDA) receptors. The discovery of its rapid antidepressant effects in patients with...