| 词条 | EVT-201 |
| 释义 |
| IUPAC_name = 7-Chloro-35-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl5-methyl-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one | image = EVT-201.svg | width = 223 | CAS_number = 308239-86-3 | ATC_prefix = None | ATC_suffix = | PubChem = 9885841 | DrugBank = | ChemSpiderID = 8061514 | chemical_formula = | C=17 | H=17 | Cl=1 | N=6 | O=2 | molecular_weight = 372.809 g/mol | smiles = Clc4cccc3n2cnc(c1nc(on1)CN(C)C)c2CN(C(=O)c34)C | StdInChI = 1S/C17H17ClN6O2/c1-22(2)8-13-20-16(21-26-13)15-12-7-23(3)17(25)14-10(18)5-4-6-11(14)24(12)9-19-15/h4-6,9H,7-8H2,1-3H3 | StdInChIKey = JCYLWUVDHLVGER-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 = }}EVT-201 is a benzodiazepine derivative drug and partial positive allosteric modulator of the benzodiazepine site of the GABAA receptor.[1] It has 2–4-fold higher functional affinity for the α1 subunit relative to the α2, α3, and α5 subunits and significantly less intrinsic activity in comparison to currently-marketed benzodiazepines and the Z-drugs.[2] Despite the lower efficacy, EVT-201 still shows effectiveness in the treatment of insomnia, and it is thought that the lower efficacy may result in fewer side effects, such as motor incoordination.[2] The drug was originally developed by Roche, based on preclinical data, as a non-sedating anxiolytic, but was found to produce sedation in humans in phase I clinical trials. For this reason, it was subsequently licensed to Evotec, which is now developing it for the treatment of insomnia.[2] {{as of|2007}}, EVT-201 has completed phase II clinical trials for this indication, with positive findings reported.[3] {{as of|2015|August}}, Phase II development is ongoing in China.[4] See also
References1. ^{{cite book|author=Christian Guilleminault|title=Sleep Medicine|url=https://books.google.com/books?id=np1NaFTF_CQC&pg=PA574|year=2010|publisher=Elsevier Health Sciences|isbn=1-4377-1836-1|pages=574–}} 2. ^1 2 {{cite book|author1=Jaime M. Monti|author2=Seithikurippu Ratnas Pandi-Perumal|author3=Hanns Möhler|title=GABA and Sleep: Molecular, Functional and Clinical Aspects|url=https://books.google.com/books?id=u54tqIOP8RUC&pg=PA50|date=28 September 2010|publisher=Springer Science & Business Media|isbn=978-3-0346-0226-6|pages=50–51}} 3. ^{{cite book|author=Jack W. Plunkett|title=Plunkett's Biotech & Genetics Industry Almanac 2008: Biotech & Genetics Industry Market Research, Statistics, Trends & Leading Companies|url=https://books.google.com/books?id=3BGBibHJ1FYC&pg=PT311|date=September 2007|publisher=Plunkett Research, Ltd.|isbn=978-1-59392-087-6|pages=311–}} 4. ^{{cite web|title=Drug Profile: EVT 201|url=http://adisinsight.springer.com/drugs/800023883|website=AdisInsight|publisher=Adis International Ltd, part of Springer Science+Business Media|accessdate=30 November 2015}} External links
9 : Amines|Chloroarenes|Experimental drugs|GABAA receptor positive allosteric modulators|Hypnotics|Imidazobenzodiazepines|Ketones|Oxadiazoles|Sedatives |
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