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GRIN2B
Glutamate MDAreceptor subunit epsilon-2, also known as ''N''-methyl D-aspartate receptor subtype 2B (NMDAR2B or NR2B), is a protein that in humans is encoded by the ''GRIN2B'' gene. NMDA receptors ''N''-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. The NMDA receptor channel has been shown to be involved in long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning. NMDA receptor channels are heterotetramers composed of two molecules of the key receptor subunit NMDAR1 (GRIN1) and two drawn from one or more of the four NMDAR2 subunits: NMDAR2A (GRIN2A), NMDAR2B (GRIN2B), NMDAR2C ( GRIN2C), and NMDAR2D ( GRIN2D). The NR2 subunit acts as the agonist binding site for glutamate, one of the predominant excitatory neurotransmitter receptors in the mammalian brain. Function NR2B has been associated with age- and visual-experience-dependent plasticity in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NMDA Receptor
The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA receptor, AMPA and kainate receptors. Depending on its subunit composition, its Ligand (biochemistry), ligands are Glutamate (neurotransmitter), glutamate and glycine (or D-Serine, D-serine). However, the binding of the ligands is typically not sufficient to open the channel as it may be blocked by Magnesium, Mg2+ ions which are only removed when the neuron is sufficiently depolarized. Thus, the channel acts as a "coincidence detector" and only once both of these conditions are met, the channel opens and it allows cation, positively charged ions (cations) to flow through the cell membrane. The NMDA receptor is thought to be very important for controlling synaptic plasticity and mediating learning and memory functions. The N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DLG4
PSD-95 (postsynaptic density protein 95) also known as SAP-90 (synapse-associated protein 90) is a protein that in humans is encoded by the ''DLG4'' (discs large homolog 4) gene. PSD-95 is a member of the membrane-associated guanylate kinase (MAGUK) family. With PSD-93 it is recruited into the same NMDA receptor and potassium channel clusters. These two MAGUK proteins may interact at postsynaptic sites to form a multimeric scaffold for the clustering of receptors, ion channels, and associated signaling proteins. PSD-95 is the best studied member of the MAGUK-family of PDZ domain-containing proteins. Like all MAGUK-family proteins, its basic structure includes three PDZ domains, an SH3 domain, and a guanylate kinase-like domain (GK) connected by disordered linker regions. It is almost exclusively located in the post synaptic density of neurons, and is involved in anchoring synaptic proteins. Its direct and indirect binding partners include neuroligin, NMDA receptors, AMPA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Felbamate
Felbamate (marketed under the brand name Felbatol by MedPointe) is an anticonvulsant used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox–Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drug's usage to severe refractory epilepsy. Mechanism of action Felbamate has been proposed to have a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptors, the relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain. Approva ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rislenemdaz
Rislenemdaz (developmental code names CERC-301, MK-0657) is an orally active, selective NMDA receptor subunit 2B (NR2B) antagonist which is under development by Cerecor in the United States as an adjunctive therapy for treatment-resistant depression (TRD). In November 2013, phase II clinical trials were initiated, and in the same month, rislenemdaz received Fast Track Designation from the Food and Drug Administration for TRD. A pilot study was published in 2012, and a phase II trial was completed in 2014, but was deemed insufficient. A second attempt at a phase II trial in 2016 also found that the drug failed to demonstrate efficacy against depression. Pharmacology Rislenemdaz is a small-molecule antagonist of the NMDA receptor. The NMDA receptor is composed of several subunits, but rislenemdaz is specific for the GluN2B subunits which are only seen in the spinal cord and forebrain. Rislenemdaz binds specifically to the GluN2B subunit in order to prevent endogenous glutamate f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ifenprodil
Ifenprodil, sold under the brand names Cerocral, Dilvax, and Vadilex, is a cerebral vasodilator that has been marketed in some countries, including in Japan, Hong Kong, and France. It is currently under development for treatment of a variety of additional indications. Ifenprodil has multiple known pharmacological actions. It is an inhibitor of the NMDA receptor, specifically of NMDA receptors containing GluN1 and GluN2B subunits, the "ifenprodil binding site". Additionally, ifenprodil inhibits GIRK channels and interacts with α1-adrenergic, serotonin, and sigma receptors. Chemically, ifenprodil is a substituted phenethylamine and β-hydroxyamphetamine derivative. It is used pharmaceutically as the tartrate salt. Research Ifenprodil has been studied as a possible medication to prevent tinnitus after acoustic trauma. It is currently in phase II trials for cough and idiopathic pulmonary fibrosis Idiopathic pulmonary fibrosis (IPF) synonymous with cryptogenic fibr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
STriatal-Enriched Protein Tyrosine Phosphatase
Protein tyrosine phosphatase non-receptor type 5 is an enzyme that in humans is encoded by the ''PTPN5'' gene. Protein tyrosine phosphatase ( PTP), non-receptor type 5, also known as STEP (STriatal-Enriched protein tyrosine Phosphatase), was the first brain-specific PTP discovered. The human STEP locus maps to chromosome 11p15.2-p15.1 and the murine STEP gene to chromosome 7B3-B5. The single STEP gene is alternatively spliced to produce several isoforms, the best characterized of which are the cytosolic STEP46 protein and the membrane-associated STEP61 protein. Substrates Seven known targets of STEP have been identified as of 2015, including ERK1/2, p38, Fyn, Pyk2, PTPα, and the glutamate receptor subunits GluN2B and GluA2. STEP dephosphorylation of the kinases (ERK1/2, p38, Fyn, and Pyk2) occurs at a regulatory tyrosine within the kinase activation loop and leads to their inactivation. Dephosphorylation of a regulatory tyrosine on PTPα prevents the translocation of PT ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CERC-301
Rislenemdaz (developmental code names CERC-301, MK-0657) is an orally active, selective NMDA receptor subunit 2B (NR2B) antagonist which is under development by Cerecor in the United States as an adjunctive therapy for treatment-resistant depression (TRD). In November 2013, phase II clinical trials were initiated, and in the same month, rislenemdaz received Fast Track Designation from the Food and Drug Administration for TRD. A pilot study was published in 2012, and a phase II trial was completed in 2014, but was deemed insufficient. A second attempt at a phase II trial in 2016 also found that the drug failed to demonstrate efficacy against depression. Pharmacology Rislenemdaz is a small-molecule antagonist of the NMDA receptor. The NMDA receptor is composed of several subunits, but rislenemdaz is specific for the GluN2B subunits which are only seen in the spinal cord and forebrain. Rislenemdaz binds specifically to the GluN2B subunit in order to prevent endogenous glutamate f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Besonprodil
Besonprodil (CI-1041) is a drug which acts as an NMDA antagonist, selective for the NR2B subunit. It is under development as a supplemental medication for Parkinson's disease, and has been shown in animals to be effective in counteracting the dyskinesias associated with long-term treatment with levodopa Levodopa, also known as L-DOPA and sold under many brand names, is a dopaminergic medication which is used in the treatment of Parkinson's disease (PD) and certain other conditions like dopamine-responsive dystonia and restless legs syndrome. ... and related drugs. References NMDA receptor antagonists 4-Fluorophenyl compounds Piperidines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EVT-101
EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist. The drug was first claimed by Roche in 2002. By 2017, EVT-101 was in phase II clinical trials for major depressive disorder; however, development of the drug was discontinued in 2021. See also * List of investigational antidepressants This is a list of investigational antidepressants, or drugs that are currently under development for clinical use in the treatment of depression but are not yet approved. Specific indications include major depressive disorder, treatment-resista ... References Experimental antidepressants Abandoned drugs Imidazoles NMDA receptor antagonists Organofluorides Pyridazines {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Actinin, Alpha 2
Alpha-actinin-2 is a protein which in humans is encoded by the ''ACTN2'' gene. This gene encodes an alpha-actinin isoform that is expressed in both skeletal and cardiac muscles and functions to anchor myofibrillar actin thin filaments and titin to Z-discs. Structure Alpha-actinin-2 is a 103.8 kDa protein composed of 894 amino acids. Each molecule is rod-shaped (35 nm in length) and it homodimerizes in an anti-parallel fashion. Each monomer has an N-terminal actin-binding region composed of two calponin homology domains, two C-terminal EF hand domains, and four tandem spectrin-like repeats form the rod domain in the central region of the molecule. The high-resolution crystal structure of human alpha-actinin 2 at 3.5 Å was recently resolved. Alpha actinins belong to the spectrin gene superfamily which represents a diverse group of actin-binding cytoskeletal proteins, including spectrin, dystrophin, utrophin and fimbrin. Skeletal, cardiac, and smooth muscle isoforms are loca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GRIN2D
Glutamate MDAreceptor subunit epsilon-4 is a protein that in humans is encoded by the ''GRIN2D'' gene. Function N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. NMDA channel has been shown to be involved in long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning. NMDA receptor channels are heteromers composed of the key receptor subunit NMDAR1 (GRIN1) and 1 or more of the 4 NMDAR2 subunits: NMDAR2A (GRIN2A), NMDAR2B (GRIN2B), NMDAR2C (GRIN2C), and NMDAR2D (GRIN2D). Interactions GRIN2D has been shown to interact with Interleukin 16. See also * Glutamate receptor * NMDA receptor The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other ... Refere ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GRIN2C
Glutamate MDAreceptor subunit epsilon-3 is a protein that in humans is encoded by the ''GRIN2C'' gene. Function N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. NMDA channel has been shown to be involved in long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning. NMDA receptor channels are heteromers composed of the key receptor subunit NMDAR1 (GRIN1) and 1 or more of the 4 NMDAR2 subunits: NMDAR2A (GRIN2A), NMDAR2B (GRIN2B), NMDAR2C (GRIN2C), and NMDAR2D ( GRIN2D). Interactions GRIN2C has been shown to interact with DLG4 and DLG3. See also * Glutamate receptor * NMDA receptor The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other ... Referen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
