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NMDA receptor antagonist information


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 (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.

Several synthetic opioids function additionally as NMDAR-antagonists, such as pethidine, levorphanol, methadone, dextropropoxyphene, tramadol, and ketobemidone.

Some NMDA receptor antagonists, such as ketamine, dextromethorphan (DXM), phencyclidine (PCP), methoxetamine (MXE), and nitrous oxide (N2O), are sometimes used as recreational drugs, for their dissociative, hallucinogenic, and euphoriant properties. When used recreationally, they are classified as dissociative drugs.

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NMDA receptor antagonist

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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...

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NMDA receptor

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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...

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Receptor antagonist

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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...

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Phencyclidine

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pharmacologically, it is a dissociative anesthetic. PCP works primarily as an NMDA receptor antagonist. PCP is most commonly used in the United States. While usage peaked...

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Dizocilpine

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Dizocilpine (INN), also known as MK-801, is a pore blocker of the NMDA receptor, a glutamate receptor, discovered by a team at Merck in 1982. Glutamate is the...

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Norketamine

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CYP3A4. Similarly to ketamine, norketamine acts as a noncompetitive NMDA receptor antagonist, but is about 3–5 times less potent as an anesthetic in comparison...

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List of investigational antidepressants

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4-Chlorokynurenine (AV-101) – NMDA receptor glycine site antagonist Apimostinel (GATE-202, NRX-1074) – NMDA receptor modulator Arketamine (PCN-101, HR-071603)...

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Memantine

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low-affinity voltage-dependent uncompetitive antagonist at glutamatergic NMDA receptors. By binding to the NMDA receptor with a higher affinity than Mg2+ ions...

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GRIN2B

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Glutamate [NMDA] receptor subunit epsilon-2, also known as N-methyl D-aspartate receptor subtype 2B (NMDAR2B or NR2B), is a protein that in humans is...

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Ketamine

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high doses of ketamine for recreational purposes. Ketamine is an NMDA receptor antagonist, accounting for most of its psychoactive effects. Ketamine was...

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List of antidepressants

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non-competitive NMDA receptor antagonist, other actions Gepirone (Exxua) – 5-HT1A receptor partial agonist and α2-adrenergic receptor antagonist Opipramol (Insidon)...

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AP5

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selective NMDA receptor antagonist that competitively inhibits the ligand (glutamate) binding site of NMDA receptors. AP5 blocks NMDA receptors in micromolar...

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Orphenadrine

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effectively manage pain of various types. H1 receptor antagonist (antihistamine) NMDA receptor antagonist (Ki value of 6.0 ± 0.7 μM, one hundred times...

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Levorphanol

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receptor (MOR), but is also an agonist of the δ-opioid receptor (DOR), κ-opioid receptor (KOR), and the nociceptin receptor (NOP), as well as an NMDA...

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Antidepressant

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and seem to work via blockade of the ionotropic glutamate NMDA receptor. Other NMDA antagonists may also play a role in treating depression. The combination...

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Tenocyclidine

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used in research into NMDA receptors. TCP acts primarily as an NMDA receptor antagonist which blocks the activity of the NMDA receptor, however its increased...

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General anaesthetic

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and barbiturates (sodium thiopental, methohexital). Ketamine, an NMDA receptor antagonist, is used primarily for its analgesic effects and in an off-label...

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H2 receptor antagonist

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at the histamine H2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H2 antagonists can be used in the treatment...

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Esketamine

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problems. Esketamine acts primarily as a N-methyl-D-aspartate (NMDA) receptor antagonist but also has other actions. In the form of racemic ketamine, esketamine...

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Metabotropic glutamate receptor

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effects of the NMDA glutamate receptor antagonist, ketamine, on working memory by pretreatment with the group II metabotropic glutamate receptor agonist, LY354740...

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Angiotensin II receptor blocker

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Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin...

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Dextromethorphan

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cough and cold medicines. It affects serotonin, norepinephrine, NMDA, and sigma-1 receptors in the brain, all of which have been implicated in the pathophysiology...

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NMDA receptor modulator

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psychosis were lacking in glutamate transmission. (PCP is an NMDA receptor antagonist that blocks glutamate.) In giving glycine to people with PCP-induced...

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Promethazine

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shown that promethazine acts as a strong non-competitive selective NMDA receptor antagonist, with an EC50 of 20 μM; which might promote sedation in addition...

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Tramadol

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5-HT2C receptor antagonist M1 and M3 muscarinic acetylcholine receptor antagonist α7 nicotinic acetylcholine receptor antagonist NMDA receptor antagonist (very...

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Neramexane

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uncompetitive, fast, voltage-dependent, N-methyl-D-aspartate (NMDA) receptor antagonists--in vitro characterization". Journal of Neural Transmission. 114...

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Xenon

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high-affinity glycine-site NMDA receptor antagonist. However, xenon is different from certain other NMDA receptor antagonists in that it is not neurotoxic...

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