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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receptor (also known as the NMDAreceptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDAreceptor is...
A receptorantagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than...
pharmacologically, it is a dissociative anesthetic. PCP works primarily as an NMDAreceptorantagonist. PCP is most commonly used in the United States. While usage peaked...
Dizocilpine (INN), also known as MK-801, is a pore blocker of the NMDAreceptor, a glutamate receptor, discovered by a team at Merck in 1982. Glutamate is the...
CYP3A4. Similarly to ketamine, norketamine acts as a noncompetitive NMDAreceptorantagonist, but is about 3–5 times less potent as an anesthetic in comparison...
low-affinity voltage-dependent uncompetitive antagonist at glutamatergic NMDAreceptors. By binding to the NMDAreceptor with a higher affinity than Mg2+ ions...
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...
high doses of ketamine for recreational purposes. Ketamine is an NMDAreceptorantagonist, accounting for most of its psychoactive effects. Ketamine was...
selective NMDAreceptorantagonist that competitively inhibits the ligand (glutamate) binding site of NMDAreceptors. AP5 blocks NMDAreceptors in micromolar...
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...
and seem to work via blockade of the ionotropic glutamate NMDAreceptor. Other NMDAantagonists may also play a role in treating depression. The combination...
used in research into NMDAreceptors. TCP acts primarily as an NMDAreceptorantagonist which blocks the activity of the NMDAreceptor, however its increased...
and barbiturates (sodium thiopental, methohexital). Ketamine, an NMDAreceptorantagonist, is used primarily for its analgesic effects and in an off-label...
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...
problems. Esketamine acts primarily as a N-methyl-D-aspartate (NMDA) receptorantagonist but also has other actions. In the form of racemic ketamine, esketamine...
effects of the NMDA glutamate receptorantagonist, ketamine, on working memory by pretreatment with the group II metabotropic glutamate receptor agonist, LY354740...
Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin...
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...
psychosis were lacking in glutamate transmission. (PCP is an NMDAreceptorantagonist that blocks glutamate.) In giving glycine to people with PCP-induced...
shown that promethazine acts as a strong non-competitive selective NMDAreceptorantagonist, with an EC50 of 20 μM; which might promote sedation in addition...
high-affinity glycine-site NMDAreceptorantagonist. However, xenon is different from certain other NMDAreceptorantagonists in that it is not neurotoxic...