Starting from Ro-25-6981 as a lead compound, highly potent and selective NR1/2B subtype selective NMDA receptor antagonists, with low activity at alpha(1) adrenergic receptors were developed.
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Antibodies to AMPA receptors in Rasmussen's encephalitis.
Eur J Paediatr Neurol
March 2016
Nuffield Department of Clinical Neurosciences, University of Oxford, John Radcliffe Hospital, Oxford, UK. Electronic address:
Rasmussen's encephalitis is a rare progressive childhood disorder characterized by frequent severe seizures, hemiparesis, encephalitis and mental deterioration, and associated with severe unilateral neuroinflammation. Autoantibodies, particularly to the GluA3 subtype of the alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propinonic acid receptor (AMPAR) were reported in the 1990s but not always confirmed. To explore further, sera from 52 patients with Rasmussen's encephalitis were tested by cell-based assays for antibodies to AMPAR GluA1/2/3, N-methyl-d-aspartate (NMDA NR1/2b), γ-aminobutyric acid type A and B (GABAAR α1/γ2/β2 and GABABR b1/b2) receptors, for potassium channel complex proteins, and for binding to live cortical and hippocampal neuronal cultures.
View Article and Find Full Text PDFMg2+ imparts NMDA receptor subtype selectivity to the Alzheimer's drug memantine.
J Neurosci
March 2009
Department of Neuroscience and Center for Neuroscience, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA.
Article Synopsis
- N-methyl-D-aspartate receptors (NMDARs) are crucial for neuron communication and are involved in many brain functions and disorders, with memantine being a key drug for treating Alzheimer's by blocking NMDAR channels.
- Memantine's effectiveness is significantly influenced by external magnesium ions (Mg(2+)(o)), which greatly reduce its inhibition of the NR1/2A and NR1/2B receptor subtypes but only mildly affect NR1/2C and NR1/2D subtypes.
- This finding suggests that existing theories about how memantine and other related drugs like ketamine function should be re-evaluated, highlighting a potentially greater importance of NR1/2C and NR1/
Effect of oestrogen receptor alpha and beta agonists on brain N-methyl-D-aspartate receptors.
J Neuroendocrinol
August 2008
Molecular Endocrinology and Oncology Research Center, CHUQ, CHUL Pavillon, Quebec and Faculty of Pharmacy, Laval University, Quebec, Canada.
Article Synopsis
- Previous studies demonstrate that oestradiol affects NMDA receptors with NR1/2B subunits in the brain, but the role of specific oestrogen receptor subtypes in this modulation is unclear.
- Experiments conducted on ovariectomised rats treated with oestradiol or its receptor-specific agonists (PPT for ER alpha and DPN for ER beta) reveal that oestradiol and PPT restore NMDA receptor binding and subunit mRNA levels, while DPN does not have a similar effect.
- The findings suggest that while oestradiol modulates NMDA receptors in certain brain areas, the contribution of oestrogen receptors might vary depending on the specific brain region involved.
Permeant ion effects on external Mg2+ block of NR1/2D NMDA receptors.
J Neurosci
October 2006
Department of Neuroscience, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA.
Voltage-dependent channel block by external Mg2+ (Mg2+(o)) of NMDA receptors is an essential determinant of synaptic function. The resulting Mg2+(o) inhibition of NMDA responses depends strongly on receptor subunit composition: NR1/2A and NR1/2B receptors are more strongly inhibited by Mg2+(o) than are NR1/2C or NR1/2D receptors. Previous work showed that permeant ions have profound effects on Mg2+(o) block of NMDA receptors composed of NR1, NR2A, and NR2B subunits.
View Article and Find Full Text PDFNMDA receptor NR2 subunit dependence of the slow component of magnesium unblock.
J Neurosci
May 2006
Department of Neuroscience, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA.
Article Synopsis
- NMDA receptors are crucial for various brain functions and are made up of different subunits, primarily NR1 and NR2 (with four types of NR2: A, B, C, and D).
- The properties and behaviors of these receptors, including how they interact with magnesium ions (Mg(o)2+), depend on which NR2 subunit is present.
- Research shows that NR1/2A and NR1/2B receptors unblock slower from Mg(o)2+ compared to NR1/2C and NR1/2D, which can impact how quickly the receptors respond during neuronal activities like action potentials.
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