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NMDA receptor antagonist

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NMDA receptor antagonists are a class of anesthetics that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor (NMDAR). [1]

134 relations: Ageing, Agmatine, Agonist, Alcoholic drink, Alkaloid, Allosteric regulation, Alpha-2 adrenergic receptor, Alzheimer's disease, Amantadine, Amino acid, Amnesia, Analgesic, Anesthesia, Anesthetic, Anticholinergic, AP-7 (drug), AP5, Apimostinel, Apocynaceae, Aptiganel, Ataxia, Atomoxetine, Attention, Barbiturate, Biochemical Pharmacology (journal), Bipolar disorder, Catalepsy, Catatonia, Chloroform, Clonidine, Confusion, Cough medicine, Delucemine, Delusional disorder, Dexanabinol, Dexoxadrol, Dextrallorphan, Dextromethorphan, Dextropropoxyphene, Dextrorphan, Diabetic neuropathy, Diazepam, Diphenidine, Dissociative, Dizocilpine, Drug tolerance, Eliprodil, Ethanol, Eticyclidine, Etiology, ..., Etoxadrol, Euphoria, Excitotoxicity, Gabapentin, Gacyclidine, Glutamate hypothesis of schizophrenia, Glutamatergic, Glutamic acid, Glycine, Guanfacine, Hallucination, Hallucinogen, HU-210, Huntington's disease, Huperzine A, Ibogaine, IC50, Influenza, Intrinsic activity, Ketamine, Ketobemidone, Kynurenic acid, Lanicemine, Learning, Levorphanol, Ligand-gated ion channel, List of investigational antidepressants, Liver, Magnesium, Memantine, Memory, Metabolism, Metabolite, Methadone, Methoxetamine, Methoxphenidine, Midafotel, Minocycline, Mood (psychology), Muscimol, N-Methyl-D-aspartic acid, NEFA (drug), Neramexane, Neurodegeneration, Neurotransmitter, Nightmare, Nitromemantine, Nitrous oxide, NMDA receptor, Olney's lesions, Parkinson's disease, PD-137889, Pethidine, Phencyclidine, Phenylalanine, Physiology & Behavior, Prodrug, Psychomotor agitation, Psychosis, Psychotomimetic, Rapastinel, Receptor antagonist, Recreational drug use, Remacemide, Rhynchophylline, Rolicyclidine, Schizophrenia, Selfotel, Serotonin receptor agonist, Stroke, Tenocyclidine, Tiletamine, Tramadol, Traumatic brain injury, Treatment-resistant depression, Vacuolization, WMS-2539, Xenon, 1-Aminocyclopropane-1-carboxylic acid, 4-Chlorokynurenine, 4-MeO-PCP, 5,7-Dichlorokynurenic acid, 7-Chlorokynurenic acid, 8A-PDHQ. Expand index (84 more) »

Ageing

Ageing or aging (see spelling differences) is the process of becoming older.

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Agmatine

Agmatine, also known as (4-aminobutyl)guanidine, is an aminoguanidine that was discovered in 1910 by Albrecht Kossel.

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Agonist

An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.

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Alcoholic drink

An alcoholic drink (or alcoholic beverage) is a drink that contains ethanol, a type of alcohol produced by fermentation of grains, fruits, or other sources of sugar.

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Alkaloid

Alkaloids are a class of naturally occurring chemical compounds that mostly contain basic nitrogen atoms.

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Allosteric regulation

In biochemistry, allosteric regulation (or allosteric control) is the regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site.

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Alpha-2 adrenergic receptor

The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein.

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Alzheimer's disease

Alzheimer's disease (AD), also referred to simply as Alzheimer's, is a chronic neurodegenerative disease that usually starts slowly and worsens over time.

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Amantadine

Amantadine (trade name Symmetrel, by Endo Pharmaceuticals) is a medication that has U.S. Food and Drug Administration approval for use both as an antiviral and an antiparkinsonian medication.

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Amino acid

Amino acids are organic compounds containing amine (-NH2) and carboxyl (-COOH) functional groups, along with a side chain (R group) specific to each amino acid.

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Amnesia

Amnesia is a deficit in memory caused by brain damage, disease, or psychological trauma.

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Analgesic

An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain.

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Anesthesia

In the practice of medicine (especially surgery and dentistry), anesthesia or anaesthesia (from Greek "without sensation") is a state of temporary induced loss of sensation or awareness.

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Anesthetic

An anesthetic (or anaesthetic) is a drug to prevent pain during surgery, completely blocking any feeling as opposed to an analgesic.

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Anticholinergic

An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system.

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AP-7 (drug)

AP-7 is a selective NMDA receptor (NMDAR) antagonist that competitively inhibits the glutamate binding site and thus activation of NMDAR.

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AP5

AP5 or APV ((2R)-amino-5-phosphonovaleric acid; (2R)-amino-5-phosphonopentanoate) is a selective NMDA receptor antagonist that competitively inhibits the ligand (glutamate) binding site of NMDA receptors.

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Apimostinel

Apimostinel (former developmental code name NRX-1074) is an antidepressant, acting as a selective partial agonist of an allosteric site of the glycine site of the NMDA receptor complex, which is under investigation by Naurex and Allergan for the treatment of major depressive disorder (MDD).

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Apocynaceae

Apocynaceae is a family of flowering plants that includes trees, shrubs, herbs, stem succulents, and vines, commonly known as the dogbane family, (Greek for "away from dog" since some taxa were used as dog poison).

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Aptiganel

Aptiganel (Cerestat; CNS-1102) is an unsuccessful drug candidate which acts as a noncompetitive NMDA antagonist, and that was under development by Cambridge Neuroscience, Inc as a treatment for stroke.

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Ataxia

Ataxia is a neurological sign consisting of lack of voluntary coordination of muscle movements that includes gait abnormality.

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Atomoxetine

Atomoxetine, sold under the brand name Strattera among others, is a norepinephrine (noradrenaline) reuptake inhibitor which is approved for the treatment of attention deficit hyperactivity disorder (ADHD).

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Attention

Attention, also referred to as enthrallment, is the behavioral and cognitive process of selectively concentrating on a discrete aspect of information, whether deemed subjective or objective, while ignoring other perceivable information.

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Barbiturate

A barbiturate is a drug that acts as a central nervous system depressant, and can therefore produce a wide spectrum of effects, from mild sedation to death.

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Biochemical Pharmacology (journal)

Biochemical Pharmacology is a peer-reviewed medical journal published by Elsevier.

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Bipolar disorder

Bipolar disorder, previously known as manic depression, is a mental disorder that causes periods of depression and periods of abnormally elevated mood.

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Catalepsy

Catalepsy (from Greek κατάληψις "seizing, grasping") is a nervous condition characterized by muscular rigidity and fixity of posture regardless of external stimuli, as well as decreased sensitivity to pain.

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Catatonia

Catatonia is a state of psycho-motor immobility and behavioral abnormality manifested by stupor.

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Chloroform

Chloroform, or trichloromethane, is an organic compound with formula CHCl3.

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Christmas

Christmas is an annual festival commemorating the birth of Jesus Christ,Martindale, Cyril Charles.

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Christmas and holiday season

The Christmas season, also called the festive season, or the holiday season (mainly in the U.S. and Canada; often simply called the holidays),, is an annually recurring period recognized in many Western and Western-influenced countries that is generally considered to run from late November to early January.

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Christmas Eve

Christmas Eve is the evening or entire day before Christmas Day, the festival commemorating the birth of Jesus.

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Christmas traditions

Christmas traditions vary from country to country.

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Clonidine

Clonidine (trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions.

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Confusion

Confusion (from Latin confusĭo, -ōnis, from confundere: "to pour together;" "to mingle together;" "to confuse") is the state of being bewildered or unclear in one’s mind about something.

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Cough medicine

Cough medicines are medications used in those with coughing and related conditions.

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Delucemine

Delucemine (NPS-1506) is a drug which acts as an NMDA antagonist and a serotonin reuptake inhibitor, and has neuroprotective effects.

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Delusional disorder

Delusional disorder is a generally rare mental illness in which the patient presents delusions, but with no accompanying prominent hallucinations, thought disorder, mood disorder, or significant flattening of affect.

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Dexanabinol

Dexanabinol (HU-211 or ETS2101) is a synthetic cannabinoid derivative in development by e-Therapeutics plc.

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Dexoxadrol

Dexoxadrol (Dioxadrol) is a dissociative anaesthetic drug which has been found to be an NMDA antagonist and produces similar effects to PCP in animals.

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Dextrallorphan

Dextrallorphan (DXA) is an opioid derivative chemical of the morphinan class that is used in scientific research.

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Dextromethorphan

Dextromethorphan (DXM or DM) is a drug of the morphinan class with sedative, dissociative, and stimulant properties (at higher doses).

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Dextropropoxyphene

Dextropropoxyphene is an analgesic in the opioid category, patented in 1955 and manufactured by Eli Lilly and Company.

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Dextrorphan

Dextrorphan (DXO) is a psychoactive drug of the morphinan class which acts as an antitussive or cough suppressant and dissociative hallucinogen.

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Diabetic neuropathy

Diabetic neuropathies are nerve damaging disorders associated with diabetes mellitus.

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Diazepam

Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that typically produces a calming effect.

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Diphenidine

Diphenidine (1,2-DEP, DPD, DND) is a dissociative anesthetic that has been sold as a designer drug.

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Dissociative

Dissociatives are a class of hallucinogen, which distort perceptions of sight and sound and produce feelings of detachment – dissociation – from the environment and self.

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Dizocilpine

Dizocilpine (INN), also known as MK-801, is a noncompetitive antagonist of the ''N''-Methyl-D-aspartate (NMDA) receptor, a glutamate receptor, discovered by a team at Merck in 1982.

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Drug tolerance

Drug tolerance is a pharmacological concept describing subjects' reduced reaction to a drug following its repeated use.

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Eliprodil

Eliprodil (codenamed SL-82.0715) is a NMDA antagonist drug candidate that failed a Phase III clinical trial for the treatment of acute ischemic stroke in 1996, sponsored by Synthélabo Recherche.

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Ethanol

Ethanol, also called alcohol, ethyl alcohol, grain alcohol, and drinking alcohol, is a chemical compound, a simple alcohol with the chemical formula.

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Eticyclidine

Eticyclidine (PCE, CI-400) is a dissociative anesthetic drug with hallucinogenic effects.

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Etiology

Etiology (alternatively aetiology or ætiology) is the study of causation, or origination.

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Etoxadrol

Etoxadrol (CL-1848C) is a dissociative anaesthetic drug that has been found to be an NMDA antagonist and produce similar effects to PCP in animals.

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Euphoria

Euphoria is an affective state in which a person experiences pleasure or excitement and intense feelings of well-being and happiness.

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Excitotoxicity

Excitotoxicity is the pathological process by which nerve cells are damaged or killed by excessive stimulation by neurotransmitters such as glutamate and similar substances.

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Gabapentin

Gabapentin, sold under the brand name Neurontin among others, is a medication which is used to treat epilepsy (specifically partial seizures), neuropathic pain, hot flashes, and restless legs syndrome.

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Gacyclidine

Gacyclidine (GK-11) is a psychoactive drug which acts as a dissociative via functioning as a non-competitive NMDA receptor antagonist.

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Glutamate hypothesis of schizophrenia

The glutamate hypothesis of schizophrenia models the subset of pathologic mechanisms linked to glutamatergic signaling.

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Glutamatergic

Glutamatergic means "related to glutamate".

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Glutamic acid

Glutamic acid (symbol Glu or E) is an α-amino acid with formula.

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Glycine

Glycine (symbol Gly or G) is the amino acid that has a single hydrogen atom as its side chain.

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Guanfacine

Guanfacine (trade names Estulic, Tenex, and, in extended release form, Intuniv) is a sympatholytic drug used to treat hypertension and attention deficit hyperactivity disorder (ADHD).

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Hallucination

A hallucination is a perception in the absence of external stimulus that has qualities of real perception.

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Hallucinogen

A hallucinogen is a psychoactive agent which can cause hallucinations, perceptual anomalies, and other substantial subjective changes in thoughts, emotion, and consciousness.

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HU-210

HU-210 is a synthetic cannabinoid that was first synthesized in 1988 from (1R,5S)-myrtenol by a group led by Professor Raphael Mechoulam at the Hebrew University.

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Huntington's disease

Huntington's disease (HD), also known as Huntington's chorea, is an inherited disorder that results in death of brain cells.

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Huperzine A

Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata and in varying quantities in other Huperzia species, including H. elmeri, H. carinat, and H. aqualupian.

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Ibogaine

Ibogaine is a naturally occurring psychoactive substance found in plants in the Apocynaceae family such as Tabernanthe iboga, Voacanga africana and Tabernaemontana undulata.

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IC50

The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function.

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Influenza

Influenza, commonly known as "the flu", is an infectious disease caused by an influenza virus.

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Intrinsic activity

Intrinsic activity (IA) or efficacy refers to the relative ability of a drug-receptor complex to produce a maximum functional response.

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Ketamine

Ketamine, sold under the brand name Ketalar among others, is a medication mainly used for starting and maintaining anesthesia.

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Ketobemidone

Ketobemidone, sold under the brand name Ketogan among others, is a powerful opioid painkiller.

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Kynurenic acid

Kynurenic acid (KYNA or KYN) is a product of the normal metabolism of amino acid L-tryptophan.

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Lanicemine

Lanicemine (AZD6765) is a low-trapping NMDA receptor antagonist that was under development by AstraZeneca for the management of severe and treatment-resistant depression.

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Learning

Learning is the process of acquiring new or modifying existing knowledge, behaviors, skills, values, or preferences.

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Levorphanol

Levorphanol (INN; brand name Levo-Dromoran) is an opioid medication used to treat moderate to severe pain.

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Ligand-gated ion channel

Ligand-gated ion channels (LICs, LGIC), also commonly referred as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand), such as a neurotransmitter.

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List of investigational antidepressants

This is a list of investigational antidepressants, or antidepressants that are currently under development for clinical use in the treatment of mood disorders but are not yet approved.

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Liver

The liver, an organ only found in vertebrates, detoxifies various metabolites, synthesizes proteins, and produces biochemicals necessary for digestion.

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Magnesium

Magnesium is a chemical element with symbol Mg and atomic number 12.

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Memantine

Memantine is used to treat moderate to severe Alzheimer's disease. It acts on the glutamatergic system by blocking NMDA receptors. It was first synthesized by Eli Lilly and Company in 1968 as a potential agent to treat diabetes; the NMDA activity was discovered in the 1980s.

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Memory

Memory is the faculty of the mind by which information is encoded, stored, and retrieved.

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Metabolism

Metabolism (from μεταβολή metabolē, "change") is the set of life-sustaining chemical transformations within the cells of organisms.

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Metabolite

A metabolite is the intermediate end product of metabolism.

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Methadone

Methadone, sold under the brand name Dolophine among others, is an opioid used to treat pain and as maintenance therapy or to help with tapering in people with opioid dependence.

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Methoxetamine

Methoxetamine, abbreviated as MXE, is a dissociative hallucinogen that has been sold as a designer drug.

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Methoxphenidine

Methoxphenidine (methoxydiphenidine, 2-MeO-Diphenidine, MXP) is a dissociative of the diarylethylamine class that has been sold online as a designer drug.

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Midafotel

Midafotel (CPPene; SDZ EAA 494) is a potent, competitive antagonist at the NMDA receptor.

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Minocycline

Minocycline is a broad-spectrum tetracycline antibiotic, and has a broader spectrum than the other members of the group.

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Mood (psychology)

In psychology, a mood is an emotional state.

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Muscimol

Muscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of Amanita muscaria and related species of mushroom.

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N-Methyl-D-aspartic acid

N-Methyl-D-aspartic acid or N-Methyl-D-aspartate (NMDA) is an amino acid derivative that acts as a specific agonist at the NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.

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NEFA (drug)

NEFA is a moderate affinity NMDA antagonist (IC50.

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Neramexane

Neramexane is a drug related to memantine, which acts as an NMDA antagonist and has neuroprotective effects.

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Neurodegeneration

Neurodegeneration is the progressive loss of structure or function of neurons, including death of neurons.

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Neurotransmitter

Neurotransmitters are endogenous chemicals that enable neurotransmission.

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New Year

New Year is the time or day at which a new calendar year begins and the calendar's year count increments by one.

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New Year's Day

New Year's Day, also called simply New Year's or New Year, is observed on January 1, the first day of the year on the modern Gregorian calendar as well as the Julian calendar.

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New Year's Eve

In the Gregorian calendar, New Year's Eve (also known as Old Year's Day or Saint Sylvester's Day in many countries), the last day of the year, is on 31 December which is the seventh day of Christmastide.

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Nightmare

A nightmare, also called a bad dream, Retrieved July 11, 2016.

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Nitromemantine

Nitromemantine (developmental code name YQW-36) is a derivative of memantine developed in 2006 for the treatment of Alzheimer's disease.

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Nitrous oxide

Nitrous oxide, commonly known as laughing gas or nitrous, is a chemical compound, an oxide of nitrogen with the formula.

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NMDA receptor

The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel protein found in nerve cells.

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Olney's lesions

Olney's lesions, also known as NMDA receptor antagonist neurotoxicity (NAN), are a potential form of brain damage due to drugs that have been studied experimentally and have produced neuronal damage, yet are administered by doctors to humans in the settings of pharmacotherapy and of anesthesia.

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Parkinson's disease

Parkinson's disease (PD) is a long-term degenerative disorder of the central nervous system that mainly affects the motor system.

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PD-137889

PD-137889 (N-methylhexahydrofluorenamine) is a chemical compound that is active as an NMDA receptor antagonist in the central nervous system at roughly 30 times the potency of the "flagship" of its class, ketamine, and substitutes for phencyclidine in animal studies.

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Pethidine

Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a synthetic opioid pain medication of the phenylpiperidine class.

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Phencyclidine

Phencyclidine (PCP), also known as angel dust among other names, is a drug used for its mind altering effects.

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Phenylalanine

Phenylalanine (symbol Phe or F) is an α-amino acid with the formula.

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Physiology & Behavior

Physiology & Behavior is a peer-reviewed scientific journal published by Elsevier.

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Prodrug

A prodrug is a medication or compound that, after administration, is metabolized (i.e., converted within the body) into a pharmacologically active drug.

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Psychomotor agitation

Psychomotor agitation is a set of signs and symptoms that stem from mental tension and anxiety.

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Psychosis

Psychosis is an abnormal condition of the mind that results in difficulties telling what is real and what is not.

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Psychotomimetic

A drug with psychotomimetic (also known as psychotogenic) actions mimics the symptoms of psychosis, including delusions and/or delirium, as opposed to just hallucinations.

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Rapastinel

Rapastinel (former developmental code names GLYX-13, BV-102) is a novel antidepressant that is under development by Allergan (previously Naurex) as an adjunctive therapy for the treatment of treatment-resistant major depressive disorder.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.

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Recreational drug use

Recreational drug use is the use of a psychoactive drug to induce an altered state of consciousness for pleasure, by modifying the perceptions, feelings, and emotions of the user.

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Remacemide

Remacemide is a drug which acts as a low-affinity NMDA antagonist with sodium channel blocking properties.

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Rhynchophylline

Rhynchophylline is an alkaloid found in certain Uncaria species (Rubiaceae), notably Uncaria rhynchophylla and Uncaria tomentosa.

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Rolicyclidine

Rolicyclidine (PCPy) is a dissociative anesthetic drug with hallucinogenic and sedative effects.

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Schizophrenia

Schizophrenia is a mental disorder characterized by abnormal social behavior and failure to understand reality.

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Selfotel

Selfotel (CGS-19755) is a drug which acts as a competitive NMDA antagonist, directly competing with glutamate for binding to the receptor.

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Serotonin receptor agonist

A serotonin receptor agonist is an agonist of one or more serotonin receptors.

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Stroke

A stroke is a medical condition in which poor blood flow to the brain results in cell death.

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Tenocyclidine

Tenocyclidine (TCP) was discovered by a team at Parke-Davis in the late 1950s.

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Tiletamine

Tiletamine is a dissociative anesthetic and pharmacologically classified as an NMDA receptor antagonist.

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Tramadol

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain.

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Traumatic brain injury

Traumatic brain injury (TBI), also known as intracranial injury, occurs when an external force injures the brain.

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Treatment-resistant depression

Treatment-resistant depression (TRD) or treatment-refractory depression is a term used in clinical psychiatry to describe cases of major depressive disorder (MDD) that do not respond adequately to appropriate courses of at least two antidepressants.

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Vacuolization

Vacuolization is the formation of vacuoles within or adjacent to cells, and, in dermatopathology, often refers to the basal cell-basement membrane zone area.

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WMS-2539

WMS-2539 is a fluorinated derivative of dexoxadrol and a potent uncompetitive NMDA receptor antagonist.

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Xenon

Xenon is a chemical element with symbol Xe and atomic number 54.

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1-Aminocyclopropane-1-carboxylic acid

1-Aminocyclopropane-1-carboxylic acid (ACC) is a disubstituted cyclic α-amino acid in which a three-membered cyclopropane ring is fused to the Cα atom of the amino acid.

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2018

2018 has been designated as the third International Year of the Reef by the International Coral Reef Initiative.

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2019

2019 (MMXIX) will be a common year starting on Tuesday of the Gregorian calendar, the 2019th year of the Common Era (CE) and Anno Domini (AD) designations, the 19th year of the 3rd millennium, the 19th year of the 21st century, and the 10th and last year of the 2010s decade.

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4-Chlorokynurenine

L-4-Chlorokynurenine (4-Cl-KYN; developmental code name AV-101) is an orally active small molecule prodrug of 7-chlorokynurenic acid, a NMDA receptor antagonist.

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4-MeO-PCP

4-Methoxyphencyclidine (methoxydine, 4-MeO-PCP) is a dissociative anesthetic drug that has been sold online as a research chemical.

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5,7-Dichlorokynurenic acid

5,7-Dichlorokynurenic acid (DCKA) is a selective NMDA receptor antagonist acting at the glycine site of the NMDA receptor complex.

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7-Chlorokynurenic acid

7-Chlorokynurenic acid (7-CKA) is a tool compound that acts as a potent and selective noncompetitive antagonist of the glycine site of the NMDA receptor.

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8A-PDHQ

8a-Phenyldecahydroquinoline (8A-PDHQ) is a high affinity NMDA antagonist developed by a team at Parke Davis in the 1950s.

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N-methyl-D-aspartate receptor antagonist, NMDA Receptor Antagonist, NMDA Receptor Antagonists, NMDA antagonist, NMDA antagonists, NMDA blocker, NMDA receptor antagonists, NMDA receptor blocker, NMDAR antagonist, NMDAR blocker, Nmda receptor antagonist.

References

[1] https://en.wikipedia.org/wiki/NMDA_receptor_antagonist

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