| 词条 | Cinazepam |
| 释义 |
| IUPAC_name = 4[7-Bromo-5-(2-chlorophenyl)-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]oxy4-oxobutanoic acid | image = Cinazepam.svg | width = 266 | CAS_number = 172986-25-3 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = U4SS7UFXC7 | ATC_prefix = None | ATC_suffix = | PubChem = 629281 | DrugBank = | ChemSpiderID = 546502 | chemical_formula = | C=19 | H=14 | Br=1 | Cl=1 | N=2 | O=5 | molecular_weight = 465.682 g/mol | smiles = c1ccc(c(c1)C2=NC(C(=O)Nc3c2cc(cc3)Br)OC(=O)CCC(=O)O)Cl | StdInChI = 1S/C19H14BrClN2O5/c20-10-5-6-14-12(9-10)17(11-3-1-2-4-13(11)21)23-19(18(27)22-14)28-16(26)8-7-15(24)25/h1-6,9,19H,7-8H2,(H,22,27)(H,24,25) | StdInChIKey = NQTRBZXDWMDXAQ-UHFFFAOYSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = }}Cinazepam (BD-798, sold under brand name Levana) is an atypical benzodiazepine derivative.[1] It produces pronounced hypnotic, sedative, and anxiolytic effects with minimal myorelaxant side effects.[2][3][4] In addition, unlike many other benzodiazepine and nonbenzodiazepine hypnotics such as diazepam, flunitrazepam, and zopiclone, cinazepam does not violate sleep architecture, and the continuity of slow-wave sleep and REM sleep are proportionally increased.[2][3][4] As such, cinazepam produces a sleep state close to physiological, and for that reason, may be advantageous compared to other, related drugs in the treatment of insomnia and other sleep disorders.[2] Cinazepam has an order of magnitude lower affinity for the benzodiazepine receptor of the GABAA complex relative to other well-known hypnotic benzodiazepines such as nitrazepam and phenazepam.[2] Moreover, in mice, it is rapidly metabolized, with only 5% of the base compound remaining within 30 minutes of administration.[2] As such, cinazepam is considered to be a benzodiazepine prodrug; specifically, to 3-hydroxyphenazepam, as the main active metabolite.[2] See also
References1. ^{{cite book|title=Sleep Research|url=https://books.google.com/books?id=DWBQAAAAYAAJ|year=1997|publisher=Brain Information Service/Brain Research Institute, University of California.}} {{Hypnotics}}{{Benzodiazepines}}{{GABAAR PAMs}}{{sedative-stub}}2. ^1 2 3 4 5 {{cite journal |vauthors=Schukin SI, Zinkovsky VG, Zhuk OV | title = Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice | journal = Pharmacol Rep | volume = 63 | issue = 5 | pages = 1093–100 | year = 2011 | pmid = 22180351 | doi = 10.1016/s1734-1140(11)70628-4| url = http://www.if-pan.krakow.pl/pjp/pdf/2011/5_1093.pdf}} 3. ^1 {{cite journal|last1=Makan|first1=S. Yu.|last2=Boiko|first2=I. A.|last3=Smul’skii|first3=S. P.|last4=Andronati|first4=S. A.|title=Effect of cinazepam administration on the ligand affinity of neuromediator system receptors in rat brain|journal=Pharmaceutical Chemistry Journal|volume=41|issue=5|year=2007|pages=249–252|issn=0091-150X|doi=10.1007/s11094-007-0055-9}} 4. ^1 {{cite journal|last1=Andronati|first1=S. A.|last2=Makan|first2=S. Yu.|last3=Neshchadin|first3=D. P.|last4=Yakubovskaya|first4=L. N.|last5=Sava|first5=V. M.|last6=Andronati|first6=K. S.|title=Bioaccessibility of cinazepam introduced as inclusion complex with β-cyclodextrin|journal=Pharmaceutical Chemistry Journal|volume=32|issue=10|year=1998|pages=513–515|issn=0091-150X|doi=10.1007/BF02465736}} 8 : Abandoned drugs|Anxiolytics|Benzodiazepines|Chloroarenes|GABAA receptor positive allosteric modulators|Hypnotics|Bromoarenes|Prodrugs |
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