| 词条 | Dehydronorketamine |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 6-Amino-6-(2-chlorophenyl)cyclohex-2-en-1-one | image = 5,6-Dehydronorketamine.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 57683-62-2 | CAS_supplemental = | ATC_prefix = None | ATC_suffix = | PubChem = 162835 | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 142954 | C=12 | H=12 | Cl=1 | N=1 | O=1 | molecular_weight = 221.68278 g/mol | smiles = C1CC(C(=O)C=C1)(C2=CC=CC=C2Cl)N | StdInChI = 1S/C12H12ClNO/c13-10-6-2-1-5-9(10)12(14)8-4-3-7-11(12)15/h1-3,5-7H,4,8,14H2 | StdInChIKey = BXBPJMHHWPXBJL-UHFFFAOYSA-N | synonyms = }}Dehydronorketamine (DHNK), or 5,6-dehydronorketamine, is a minor metabolite of ketamine which is formed by dehydrogenation of its metabolite norketamine.[1][2] Though originally considered to be inactive,[1][2][3] DHNK has been found to act as a potent and selective negative allosteric modulator of the α7-nicotinic acetylcholine receptor (IC50 = 55 nM).[4][5] For this reason, similarly to hydroxynorketamine (HNK), it has been hypothesized that DHNK may have the capacity to produce rapid antidepressant effects.[6] However, unlike ketamine, norketamine, and HNK, DHNK has been found to be inactive in the forced swim test (FST) in mice at doses up to 50 mg/kg.[7] DHNK is inactive at the α3β4-nicotinic acetylcholine receptor (IC50 > 100 μM) and is only very weakly active at the NMDA receptor (Ki = 38.95 μM for (S)-(+)-DHNK).[4] It can be detected 7–10 days after a modest dose of ketamine, and because of this, is useful in drug detection assays.[8] See also
References1. ^1 {{cite book|author=Bruno Bissonnette|title=Pediatric Anesthesia|url=https://books.google.com/books?id=yq8tAwAAQBAJ&pg=PA366|date=14 May 2014|publisher=PMPH-USA|isbn=978-1-60795-213-8|pages=366–}} {{Nicotinic acetylcholine receptor modulators}}{{nervous-system-drug-stub}}2. ^1 {{cite book|author=J. John Mann|title=Clinical Handbook for the Management of Mood Disorders|url=https://books.google.com/books?id=3NPvLExs7X8C&pg=PA347|date=9 May 2013|publisher=Cambridge University Press|isbn=978-1-107-06744-8|pages=347–}} 3. ^{{cite book|title=The Neuropsychiatric Complications of Stimulant Abuse|url=https://books.google.com/books?id=qUSnBQAAQBAJ&pg=PA225|date=1 June 2015|publisher=Elsevier Science|isbn=978-0-12-803003-5|pages=225–}} 4. ^1 {{cite journal|last1=Moaddel|first1=Ruin|last2=Abdrakhmanova|first2=Galia|last3=Kozak|first3=Joanna|last4=Jozwiak|first4=Krzysztof|last5=Toll|first5=Lawrence|last6=Jimenez|first6=Lucita|last7=Rosenberg|first7=Avraham|last8=Tran|first8=Thao|last9=Xiao|first9=Yingxian|last10=Zarate|first10=Carlos A.|last11=Wainer|first11=Irving W.|title=Sub-anesthetic concentrations of (R,S)-ketamine metabolites inhibit acetylcholine-evoked currents in α7 nicotinic acetylcholine receptors|journal=European Journal of Pharmacology|volume=698|issue=1–3|year=2013|pages=228–234|issn=0014-2999|doi=10.1016/j.ejphar.2012.11.023|pmc=3534778}} 5. ^{{cite book|author=Robin A.J. Lester|title=Nicotinic Receptors|url=https://books.google.com/books?id=Y0BTBQAAQBAJ&pg=PA445|date=11 November 2014|publisher=Springer|isbn=978-1-4939-1167-7|pages=445–}} 6. ^{{cite journal|last1=Paul|first1=Rajib K.|last2=Singh|first2=Nagendra S.|last3=Khadeer|first3=Mohammed|last4=Moaddel|first4=Ruin|last5=Sanghvi|first5=Mitesh|last6=Green|first6=Carol E.|last7=O’Loughlin|first7=Kathleen|last8=Torjman|first8=Marc C.|last9=Bernier|first9=Michel|last10=Wainer|first10=Irving W.|title=(R,S)-Ketamine Metabolites (R,S)-norketamine and (2S,6S)-hydroxynorketamine Increase the Mammalian Target of Rapamycin Function|journal=Anesthesiology|volume=121|issue=1|year=2014|pages=149–159|issn=0003-3022|doi=10.1097/ALN.0000000000000285|pmid=24936922|pmc=4061505}} 7. ^{{vcite2 journal | vauthors = Sałat K, Siwek A, Starowicz G, Librowski T, Nowak G, Drabik U, Gajdosz R, Popik P | title = Antidepressant-like effects of ketamine, norketamine and dehydronorketamine in forced swim test: Role of activity at NMDA receptor | journal = Neuropharmacology | volume = 99| issue = | pages = 301–7| year = 2015 | pmid = 26240948 | doi = 10.1016/j.neuropharm.2015.07.037 | url = }} 8. ^{{cite book|author=Q. Alan Xu|title=Ultra-High Performance Liquid Chromatography and Its Applications|url=https://books.google.com/books?id=pl80RKCNkQ0C&pg=SA1-PA145|date=1 April 2013|publisher=John Wiley & Sons|isbn=978-1-118-53398-7|pages=1–}} 6 : Amines|Chloroarenes|Ketones|Nicotinic antagonists|Human drug metabolites|Cyclohexenes |
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