| 词条 | Pyrazolam |
| 释义 |
| drug_name = | IUPAC_name = 8-Bromo-1-methyl-6-(pyridin-2-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine | image = Pyrazolam-skeletal.svg | width = 150 | tradename = | pregnancy_category= | legal_AU = S9 | legal_CA = Schedule IV | legal_status = | routes_of_administration = Oral, Sublingual, rectal | bioavailability = | protein_bound = | metabolism = | elimination_half-life = 17 hours | excretion = | CAS_number = 39243-02-2 | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 12562545 | ChemSpiderID = 15417688 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 8LH16383PK | ChEMBL = 3246831 | C=16 | H=12 | Br=1 | N=5 | smiles = CC1=NN=C2CN=C(C3=NC=CC=C3)C3=CC(Br)=CC=C3N12 | StdInChI = 1S/C16H12BrN5/c1-10-20-21-15-9-19-16(13-4-2-3-7-18-13)12-8-11(17)5-6-14(12)22(10)15/h2-8H,9H2,1H3 | StdInChIKey = BGRWSFIQQPVEML-UHFFFAOYSA-N }}Pyrazolam (SH-I-04)[1] is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s,[2] and subsequently "rediscovered" and sold as a designer drug starting in 2012.[3][4][5][6][7] Pyrazolam has structural similarities to alprazolam[8] and bromazepam. Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine.[3][9] It is most selective for the α2 and α3 subtypes of the GABAA receptor.[10] Legal StatusUnited KingdomIn the UK, pyrazolam has been classified as a Class C drug by section 5 of the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs.[11] See also
References1. ^Clayton T, et al. A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. Int J Med Chem. 2015; 2015: 430248. {{doi|10.1155/2015/430248}} {{pmid|26682068}} {{Benzodiazepines}}{{GABAAR PAMs}}2. ^{{Cite patent | country=US |number= 3954728 | title =Preparation of triazolo benzodiazepines and novel compounds}} 3. ^1 {{cite journal | date=July 2013 | first1=B. | first2=M. | first4=S. | last1=Moosmann | title=Characterization of the designer benzodiazepine pyrazolam and its detectability in human serum and urine | last2=Hutter | last3=Huppertz | first3=L. M. | last4=Ferlaino | last5=Redlingshöfer | first5=L. | last6=Auwärter | first6=V. | journal=Forensic Toxicology | volume=31 | issue=2 | pages=263–271 | doi=10.1007/s11419-013-0187-4}} 4. ^{{cite journal | author1=Bjoern Moosmann | title=Designer benzodiazepines: A new challenge | date=June 2015 | author2=Leslie A King | author3=Volker Auwärter | journal=World Psychiatry | volume=14 | issue=2 | pages=248 | doi=10.1002/wps.20236 | pmid=26043347 | pmc=4471986}} 5. ^{{cite journal | title=Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays |author1=Madeleine Pettersson Bergstrand |author2=Anders Helander |author3=Therese Hansson |author4=Olof Beck | journal=Drug Testing and Analysis | volume=9 | issue=4 | pages=640–645 | date=2016 | doi=10.1002/dta.2003 | pmid=27366870}} 6. ^{{cite journal|first1=Gudrun|last1=Høiseth|first2=Silja Skogstad|last2=Tuv|first3=Ritva|last3=Karinen|title=Blood concentrations of new designer benzodiazepines in forensic cases|url=http://www.sciencedirect.com/science/article/pii/S0379073816304121|journal=Forensic Science International|doi=10.1016/j.forsciint.2016.09.006|date=2016|volume=268|pages=35–38|pmid=27685473}} 7. ^{{cite journal|first1=Kieran R.|last1=Manchester|first2=Peter D.|last2=Maskell|first3=Laura|last3=Waters|title=Experimental versus theoretical log D7.4, pKa and plasma protein binding values for benzodiazepines appearing as new psychoactive substances|journal=Drug Testing and Analysis|volume=10|issue=8|pages=1258–1269|issn=1942-7611|doi=10.1002/dta.2387|pmid=29582576|date=2018}} 8. ^{{cite journal | author1=Hester Jr | first1=J. B. | title=6-Phenyl-4H-s-triazolo[4,3-a][l,4]benzodiazepines Which Have Central Nervous System Depressant Activity | last2=Rudzik | first2=A. D. | last3=Kamdar | first3=B. V. | journal=J. Med. Chem. | date=November 1971 | volume=14 | issue=11 | pages=1078–1081 | doi=10.1021/jm00293a015 | pmid=5165540}} 9. ^[https://www.uniklinik-freiburg.de/fileadmin/mediapool/08_institute/rechtsmedizin/pdf/Poster2013/Mossmann_DPHG2013.pdf Characterization of the designer benzodiazepines pyrazolam and flubromazepam and study on their detectability in human serum and urine samples], B. Moosmann, M. Hutter, L. M. Huppertz and V. Auwärter 10. ^{{cite journal | title=6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity | journal=Journal of Medicinal Chemistry | date=November 1979 | volume=22 | issue=11 | pages=1390–1398 | doi=10.1021/jm00197a021 | first1=J. B. | last1=Hester | last2=von Voigtlander | first2=P. | pmid=42799}} 11. ^{{Cite web|url=http://www.legislation.gov.uk/uksi/2017/634/contents/made|title=The Misuse of Drugs Act 1971 (Amendment) Order 2017|last=|first=|date=|website=|archive-url=|archive-date=|dead-url=|access-date=}} 5 : Triazolobenzodiazepines|GABAA receptor positive allosteric modulators|Designer drugs|Pyridines|Bromoarenes |
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