Matches in DBpedia 2016-04 for { <http://dbpedia.org/resource/Arketamine> ?p ?o }
- Arketamine abstract "Arketamine, also (R)-ketamine or R(–)-ketamine, is the (R)-(–) enantiomer of ketamine. Unlike racemic ketamine and esketamine, the S(+) enantiomer of ketamine, arketamine is less potent pharmacologically and has never been approved or marketed as an enantiopure drug for clinical use. Arketamine is active in its own right but is inferior to esketamine at all receptors targeted for anesthetic use, with its only superior affinity being for the dopamine transporter, which is considered an antitarget in anesthetic applications due to its association with an increase in adverse psychiatric effects (such as those which occur following administration of the related recreational anesthetic phencyclidine).Relative to esketamine, arketamine possesses 4–5 times lower affinity for the PCP site of the NMDA receptor. In accordance, arketamine is significantly less potent than racemic ketamine and especially esketamine in terms of anesthetic, analgesic, and sedative-hypnotic effects. Racemic ketamine has weak affinity for the sigma receptor, where it acts as an agonist, whereas esketamine binds negligibly to this receptor, and so the sigma receptor activity of racemic ketamine lies in arketamine. It has been suggested that this action of arketamine may play a role in the hallucinogenic effects of racemic ketamine and that it may be responsible for the lowering of the seizure threshold seen with racemic ketamine. Esketamine inhibits the dopamine transporter about 8-fold more potently than does arketamine, and so is about 8 times more potent as a dopamine reuptake inhibitor. Arketamine and esketamine possess similar potency for interaction with the muscarinic acetylcholine receptors.Paradoxically, arketamine shows greater and longer-lasting rapid antidepressant effects in animal models of depression relative to esketamine. It has been suggested that this difference may have due to with the possibility of different activity of arketamine and esketamine and their respective metabolites at the α7-nicotinic receptor, as norketamine and hydroxynorketamine are potent antagonists of this receptor and markers of potential rapid antidepressant effects (specifically, increased mammalian target of rapamycin function) correlate closely with their affinity for it. The picture is unclear however, and other mechanisms have also been implicated.In rodent studies, esketamine produced hyperlocomotion, prepulse inhibition deficits, and rewarding effects, while arketamine did not, indicating that arketamine may have a lower propensity for producing psychotomimetic effects and a lower abuse potential in addition to superior antidepressant efficacy.".
- Arketamine atcPrefix "None".
- Arketamine casNumber "33643-49-1".
- Arketamine iupacName "(R)-2-(2-Chlorophenyl)-2-(methylamino)cyclohexanone".
- Arketamine pubchem "644025".
- Arketamine thumbnail Arketamine.svg?width=300.
- Arketamine wikiPageID "46929392".
- Arketamine wikiPageLength "9584".
- Arketamine wikiPageOutDegree "53".
- Arketamine wikiPageRevisionID "708202088".
- Arketamine wikiPageWikiLink Agonist.
- Arketamine wikiPageWikiLink Alpha-7_nicotinic_receptor.
- Arketamine wikiPageWikiLink Analgesic.
- Arketamine wikiPageWikiLink Anesthetic.
- Arketamine wikiPageWikiLink Antidepressant.
- Arketamine wikiPageWikiLink Antitarget.
- Arketamine wikiPageWikiLink Biological_activity.
- Arketamine wikiPageWikiLink Category:Amines.
- Arketamine wikiPageWikiLink Category:Antidepressants.
- Arketamine wikiPageWikiLink Category:Dissociative_drugs.
- Arketamine wikiPageWikiLink Category:Dopamine_reuptake_inhibitors.
- Arketamine wikiPageWikiLink Category:Enantiopure_drugs.
- Arketamine wikiPageWikiLink Category:General_anesthetics.
- Arketamine wikiPageWikiLink Category:Ketones.
- Arketamine wikiPageWikiLink Category:Muscarinic_antagonists.
- Arketamine wikiPageWikiLink Category:NMDA_receptor_antagonists.
- Arketamine wikiPageWikiLink Category:Nicotinic_antagonists.
- Arketamine wikiPageWikiLink Category:Organochlorides.
- Arketamine wikiPageWikiLink Category:Sedatives.
- Arketamine wikiPageWikiLink Category:Sigma_agonists.
- Arketamine wikiPageWikiLink Clinic.
- Arketamine wikiPageWikiLink Depression_(mood).
- Arketamine wikiPageWikiLink Dopamine_reuptake_inhibitor.
- Arketamine wikiPageWikiLink Dopamine_transporter.
- Arketamine wikiPageWikiLink Drug.
- Arketamine wikiPageWikiLink Enantiomer.
- Arketamine wikiPageWikiLink Esketamine.
- Arketamine wikiPageWikiLink Hallucinogen.
- Arketamine wikiPageWikiLink Hydroxynorketamine.
- Arketamine wikiPageWikiLink Hyperlocomotion.
- Arketamine wikiPageWikiLink Ketamine.
- Arketamine wikiPageWikiLink Ligand_(biochemistry).
- Arketamine wikiPageWikiLink Mechanistic_target_of_rapamycin.
- Arketamine wikiPageWikiLink Metabolite.
- Arketamine wikiPageWikiLink Model_organism.
- Arketamine wikiPageWikiLink Muscarinic_acetylcholine_receptor.
- Arketamine wikiPageWikiLink NMDA_receptor.
- Arketamine wikiPageWikiLink Norketamine.
- Arketamine wikiPageWikiLink Pharmacology.
- Arketamine wikiPageWikiLink Phencyclidine.
- Arketamine wikiPageWikiLink Prepulse_inhibition.
- Arketamine wikiPageWikiLink Psychotomimetic.
- Arketamine wikiPageWikiLink Racemic_mixture.
- Arketamine wikiPageWikiLink Receptor_antagonist.
- Arketamine wikiPageWikiLink Reuptake_inhibitor.
- Arketamine wikiPageWikiLink Reward_system.
- Arketamine wikiPageWikiLink Sedative.
- Arketamine wikiPageWikiLink Seizure_threshold.
- Arketamine wikiPageWikiLink Sigma_receptor.
- Arketamine wikiPageWikiLink Substance_abuse.
- Arketamine wikiPageWikiLinkText "Arketamine".
- Arketamine wikiPageWikiLinkText "arketamine".
- Arketamine atcPrefix "None".
- Arketamine c "13".
- Arketamine casNumber "33643".
- Arketamine chemspiderid "559099".
- Arketamine cl "1".
- Arketamine h "16".
- Arketamine inchi "InChI=1S/C13H16ClNO/c1-15-1310-6-2-3-7-1114/h2-3,6-7,15H,4-5,8-9H2,1H3/t13-/m1/s1".
- Arketamine inchikey "YQEZLKZALYSWHR-CYBMUJFWSA-N".
- Arketamine iupacName "-2".
- Arketamine legalAu "S8".
- Arketamine legalCa "Schedule I".
- Arketamine legalUk "CD".
- Arketamine legalUn "Unscheduled".
- Arketamine legalUs "Schedule III".
- Arketamine molecularWeight "237.725".
- Arketamine n "1".
- Arketamine o "1".
- Arketamine pubchem "644025".
- Arketamine smiles "CNC1C2=CC=CC=C2Cl".
- Arketamine width "200".
- Arketamine wikiPageUsesTemplate Template:Antidepressants.
- Arketamine wikiPageUsesTemplate Template:Cholinergics.
- Arketamine wikiPageUsesTemplate Template:Dopaminergics.
- Arketamine wikiPageUsesTemplate Template:Drugbox.
- Arketamine wikiPageUsesTemplate Template:General_anesthetics.
- Arketamine wikiPageUsesTemplate Template:Glutamatergics.
- Arketamine wikiPageUsesTemplate Template:Hallucinogens.
- Arketamine wikiPageUsesTemplate Template:Nervous-system-drug-stub.
- Arketamine wikiPageUsesTemplate Template:Reflist.
- Arketamine wikiPageUsesTemplate Template:Sigmaergics.
- Arketamine subject Category:Amines.
- Arketamine subject Category:Antidepressants.
- Arketamine subject Category:Dissociative_drugs.
- Arketamine subject Category:Dopamine_reuptake_inhibitors.
- Arketamine subject Category:Enantiopure_drugs.
- Arketamine subject Category:General_anesthetics.
- Arketamine subject Category:Ketones.
- Arketamine subject Category:Muscarinic_antagonists.