| 词条 | Nortilidine |
| 释义 |
| IUPAC_name = ethyl (1R,2S)-2-(methylamino)-1-phenylcyclohex-3-ene-1-carboxylate | image = Nortilidine.svg | width = | alt = | image2 = | width2 = | drug_name = | caption = | tradename = | licence_EU = | licence_US = | DailyMedID = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | dependency_liability = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 38677-94-0 | CAS_supplemental = | ATCvet = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 162321 | PubChemSubstance = | IUPHAR_ligand = | DrugBank = | ChemSpiderID = 142535 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 77839 | ChEMBL = 1614654 | UNII = 7145G6817J | synonyms = | C=16 | H=21 | N=1 | O=2 | molecular_weight = 259.3434 g/mol | SMILES = CCOC(=O)[C@]1(CCC=C[C@@H]1NC)C2=CC=CC=C2 | StdInChI = 1S/C16H21NO2/c1-3-19-15(18)16(13-9-5-4-6-10-13)12-8-7-11-14(16)17-2/h4-7,9-11,14,17H,3,8,12H2,1-2H3/t14-,16+/m0/s1 | StdInChIKey = PDJZPNKVLDWEKI-GOEBONIOSA-N | density = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | specific_rotation = | sec_combustion = }}Nortilidine[1] is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine[2] but virtually all of the opioid activity resides in the (1S,2R) isomer.[3] The (1R,2S) isomer has NMDA antagonist activity. The drug also acts as a dopamine reuptake inhibitor.[4] The reversed-ester of nortilidine is also known[5] which has almost identical properties to nortilidine.[6] See also
References1. ^US Patent 3792080 - Process for Substituted Cyclohexenes its Products {{Dopaminergics}}{{Glutamatergics}}{{Opioidergics}}{{analgesic-stub}}2. ^J Clin Pharmacol. 2002 Nov ;42 (11):1257-61 - Sequential first-pass metabolism of nortilidine: the active metabolite of the synthetic opioid drug tilidine 3. ^Opiates: George R. Lenz page 439, Table 9-30 (78) 4. ^{{cite journal|last1=Schifano|first1=Fabrizio|last2=Orsolini|first2=Laura|last3=Duccio Papanti|first3=G.|last4=Corkery|first4=John M.|title=Novel psychoactive substances of interest for psychiatry|journal=World Psychiatry|volume=14|issue=1|year=2015|pages=15–26|issn=1723-8617|doi=10.1002/wps.20174|pmc=4329884}} 5. ^US Patent 4291059 - Cycloaromatic compounds, analgesic Properties thereof and Method of use thereof as analgesic 6. ^Personal Communication with Derek P. Reynolds 4 : Opioids|Dopamine reuptake inhibitors|NMDA receptor antagonists|Cyclohexenes |
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