词条 | Ciclotizolam |
释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 451307222 | IUPAC_name = 8-bromo-6-(o-chlorophenyl)-1-cyclohexyl-4H-5-triazolo(3,4-c)thieno(2,4-e)-1,4-diazepine | image = Ciclotizolam structure.svg | width = 145 | image2 = Ciclotizolam 3D ball.png | width2 = 200 | alt2 = Ball-and-stick model of the ciclotizolam molecule | tradename = | legal_CA = Schedule IV | legal_status = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 58765-21-2 | ATC_prefix = none | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 2105986 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C20H18BrClN4S/c21-16-10-14-18(13-8-4-5-9-15(13)22)23-11-17-24-25-19(26(17)20(14)27-16)12-6-2-1-3-7-12/h4-5,8-10,12H,1-3,6-7,11H2 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = ZOSHXIXUCKESEG-UHFFFAOYSA-N | PubChem = 71949 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 64956 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = JK517QTN4Q | C=20 | H=18 | Br=1 | Cl=1 | N=4 | S=1 | molecular_weight = 461.806 g/mol | smiles = Clc5ccccc5C/2=N/Cc1nnc(n1c3sc(Br)cc\\23)C4CCCCC4 }}Ciclotizolam[1] (WE-973) is a drug which is a thienotriazolodiazepine derivative. It is a partial agonist for the benzodiazepine site of the GABAA receptor, with similar binding affinity to related compounds like brotizolam, but a low efficacy.[2][3] See also
References1. ^DE Patent 2445430 {{Benzodiazepines}}{{GABAAR PAMs}}{{sedative-stub}}2. ^{{cite journal |vauthors=Weber KH, Kuhn FJ, Böke-Kuhn K, Lehr E, Danneberg PB, Hommer D, Paul SM, Skolnick P |title=Pharmacological and neurochemical properties of 1,4-diazepines with two annelated heterocycles ('hetrazepines') |journal=European Journal of Pharmacology |volume=109 |issue=1 |pages=19–31 |date=February 1985 |pmid=2986988 |doi= 10.1016/0014-2999(85)90535-7|url=}} 3. ^{{cite journal |vauthors=Ikeda M, Weber KH, Bechtel WD, Malatynska E, Yamamura HI |title=Relative efficacies of 1,4-diazepines on GABA-stimulated chloride influx in rat brain vesicles |journal=Life Sciences |volume=45 |issue=4 |pages=349–58 |year=1989 |pmid=2569655 |doi= 10.1016/0024-3205(89)90145-8|url=}} 5 : Benzodiazepines|Chloroarenes|GABAA receptor positive allosteric modulators|Bromoarenes|Thienotriazolodiazepines |
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