NMDA receptors play an important physiological role in regulating synaptic plasticity, learning and memory. GluN2A subunits are the most abundant functional subunits of NMDA receptors expressed in mature brain, and their dysfunction is related to various neurological diseases. According to subunit composition, GluN2A-containing NMDA receptors can be divided into two types: diheteromeric and triheteromeric receptors. In this review, the expression, functional and pharmacological properties of different kinds of GluN2A-containing NMDA receptors as well as selective GluN2A regulators were described to further understand this type of NMDA receptors.
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http://dx.doi.org/10.1007/s10571-021-01185-1 | DOI Listing |
Sheng Li Xue Bao
December 2024
State Key Laboratory of Medical Neurobiology, MOE Frontiers Center for Brain Science, Institutes of Brain Science, Fudan University, Shanghai 200032, China.
At present, the problem of drug addiction treatment mainly lies in the high relapse rate of drug addicts. Addictive drugs will bring users a strong sense of euphoria and promote drug seeking. Once the drug is withdrawn, there will be withdrawal symptoms such as strong negative emotions and uncomfortable physical reactions.
View Article and Find Full Text PDFJ Psychoactive Drugs
January 2025
Department of Mental Health, Psychiatric Service for Diagnosis and Treatment, San Luigi Gonzaga Hospital, University of Turin, Turin, Orbassano, Italy.
This study explores the psychotic-like experiences (PLEs) associated with recreational ketamine use among young adults. Ketamine, initially introduced as an anesthetic, is now widely used recreationally for its dissociative effects, raising concerns about its impact on mental health. Ten participants aged 18-24, who used ketamine recreationally multiple times a week, were assessed using the Community Assessment of Psychic Experiences (CAPE-42).
View Article and Find Full Text PDFAnesth Analg
November 2024
From the Department of Anesthesia Critical Care & Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts.
Background: R-Glabridin is a major flavonoid of licorice (Glycyrrhiza glabra) root and known to modulate GABAA receptors, which are targets of many clinical hypnotics. However, R-glabridin hypnotic activity has not been reported in animals.
Methods: Inverted photomotor responses (IPMRs) were used to assess the hypnotic effects of natural R-glabridin and synthetic R/S-glabridin in wild-type zebrafish larvae and transgenic larvae lacking functional GABAA receptor β3 subunits (β30/0).
Pharmaceuticals (Basel)
December 2024
School of Pharmacy, University of Reading, Whiteknights, Reading RG6 6AJ, UK.
Recent studies, typically using patient cerebrospinal fluid (CSF), have suggested that different autoantibodies (Aabs) acting on their respective receptors, may underlie neuropsychiatric disorders. The GluN1 (NR1) subunit of the N-methyl-D-aspartate receptor (NMDAR) has been identified as a target of anti-NMDAR Aabs in a number of central nervous system (CNS) diseases, including encephalitis and autoimmune epilepsy. However, the role or the nature of Aabs responsible for effects on neuronal excitability and synaptic plasticity is yet to be established fully.
View Article and Find Full Text PDFPharmaceuticals (Basel)
November 2024
Relmada Therapeutics, Inc., Coral Gables, FL 33134, USA.
Uncompetitive NMDAR (N-methyl-D-aspartate receptor) antagonists restore impaired neural plasticity, reverse depressive-like behavior in animal models, and relieve major depressive disorder (MDD) in humans. This review integrates recent findings from in silico, in vitro, in vivo, and human studies of uncompetitive NMDAR antagonists into the extensive body of knowledge on NMDARs and neural plasticity. Uncompetitive NMDAR antagonists are activity-dependent channel blockers that preferentially target hyperactive GluN2D subtypes because these subtypes are most sensitive to activation by low concentrations of extracellular glutamate and are more likely activated by certain pathological agonists and allosteric modulators.
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