| 词条 | Desmethylflunitrazepam |
| 释义 |
| IUPAC_name = 5-(2-Fluorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one | image = Desmethylflunitrazepam.svg | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_CA = Schedule IV | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 2558-30-7 | ATC_prefix = | ATC_suffix = | PubChem = 520217 | ChemSpiderID = 453770 | ChEMBL = 87369 | UNII = 055XLQ0YQ6 | C=15 | H=10 | F=1 | N=3 | O=3 | molecular_weight = | melting_point = | smiles = FC1=C(C=CC=C1)C2=NCC(NC3=C2C=C(C=C3)[N+](=O)[O-])=O | StdInChI = 1S/C15H10FN3O3/c16-12-4-2-1-3-10(12)15-11-7-9(19(21)22)5-6-13(11)18-14(20)8-17-15/h1-7H,8H2,(H,18,20) | StdInChIKey = KNGIGRDYBQPXKQ-UHFFFAOYSA-N }}Desmethylflunitrazepam (also known as norflunitrazepam, Ro05-4435 and fonazepam) is a benzodiazepine that is a metabolite of flunitrazepam[1][2][3] and has been sold online as a designer drug.[4][5] It has an IC50 value of 1.499 nM for the GABAA receptor.[6][7] See also{{colbegin}}
References1. ^{{cite journal|first1=Ruud W.|last1=Busker|first2=Gerard M. J. Beijersbergen|last2=van Henegouwen|first3=Brigitta M. C.|last3=Kwee|first4=Jos H. M.|last4=Winkens|title=Photobinding of flunitrazepam and its major photo-decomposition product N-desmethylflunitrazepam|url=http://www.sciencedirect.com/science/article/pii/0378517387901451|journal=International Journal of Pharmaceutics|date=May 1987|pages=113–120|volume=36|issue=2–3|via=ScienceDirect|doi=10.1016/0378-5173(87)90145-1}} {{Benzodiazepines}}{{Hypnotics and sedatives}}{{GABAAR PAMs}}{{Glycinergics}}{{pharma-stub}}2. ^{{cite journal|first1=Janet K|last1=Coller|first2=Andrew A|last2=Somogyi|first3=Felix|last3=Bochner|title=Quantification of flunitrazepam's oxidative metabolites, 3-hydroxyflunitrazepam and desmethylflunitrazepam, in hepatic microsomal incubations by high-performance liquid chromatography|url=http://www.sciencedirect.com/science/article/pii/S0378434798003831|journal=Journal of Chromatography B|date=20 November 1998|pages=87–92|volume=719|issue=1–2|via=ScienceDirect|doi=10.1016/S0378-4347(98)00383-1|pmid=9869368}} 3. ^{{cite journal|first1=Tansel|last1=Kilicarslan|first2=Robert L.|last2=Haining|first3=Allan E.|last3=Rettie|first4=Usanda|last4=Busto|title=Flunitrazepam Metabolism by Cytochrome P450s 2C19 and 3A4|url=http://dmd.aspetjournals.org/content/29/4/460.long|journal=Drug Metabolism and Disposition|date=1 April 2001|issn=1521-009X|pages=460–465|volume=29|issue=4|via=dmd.aspetjournals.org|first5=Rachel F.|last5=Tyndale|first6=Edward M.|last6=Sellers|pmid=11259331}} 4. ^{{cite journal|first1=Bjoern|last1=Moosmann|first2=Philippe|last2=Bisel|first3=Florian|last3=Franz|first4=Laura M.|last4=Huppertz|title=Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines – an update comprising adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, metizolam, and nitrazolam|journal=Journal of Mass Spectrometry|date=2016|issn=1096-9888|volume=51|issue=11|pages=1080–1089|doi=10.1002/jms.3840|pmid=27535017|first5=Volker|last5=Auwärter}} 5. ^{{cite journal|first1=Maria|last1=Katselou|first2=Ioannis|last2=Papoutsis|first3=Panagiota|last3=Nikolaou|first4=Chara|last4=Spiliopoulou|title=Metabolites replace the parent drug in the drug arena. The cases of fonazepam and nifoxipam|journal=Forensic Toxicology|volume=35|issue=1|pages=1–10|date=2016|issn=1860-8973|doi=10.1007/s11419-016-0338-5|pmid=28127407|pmc=5214877|first5=Sotiris|last5=Athanaselis}} 6. ^{{cite journal|first1=Desmond J.|last1=Maddalena|first2=Graham A. R.|last2=Johnston|title=Prediction of Receptor Properties and Binding Affinity of Ligands to Benzodiazepine/GABAA Receptors Using Artificial Neural Networks|journal=Journal of Medicinal Chemistry|date=February 1995|pages=715–724|volume=38|issue=4|doi=10.1021/jm00004a017|pmid=7861419}} 7. ^{{cite journal|first1=Sung-Sau|last1=So|first2=Martin|last2=Karplus|title=Genetic Neural Networks for Quantitative Structure−Activity Relationships: Improvements and Application of Benzodiazepine Affinity for Benzodiazepine/GABAA Receptors|journal=Journal of Medicinal Chemistry|date=20 December 1996|pages=5246–5256|volume=39|issue=26|doi=10.1021/jm960536o|pmid=8978853}} 6 : Designer drugs|Fluoroarenes|GABAA receptor positive allosteric modulators|Glycine receptor antagonists|Lactams|Nitrobenzodiazepines |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。