EVT-201: Difference between revisions
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Importing Wikidata short description: "Chemical compound" (Shortdesc helper) |
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{{Short description|Chemical compound}} |
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{{R from alternative name}} |
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{{Drugbox |
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| IUPAC_name = 7-Chloro-3-{5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl}-5-methyl-4,5-dihydro-6''H''-imidazo[1,5-''a''][1,4]benzodiazepin-6-one |
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| image = EVT-201.svg |
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| width = 223 |
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| CAS_number = 308239-86-3 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 6J8AF7CLE4 |
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| ATC_prefix = None |
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| ATC_suffix = |
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| PubChem = 9885841 |
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| DrugBank = |
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| ChemSpiderID = 8061514 |
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| chemical_formula = |
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| C=17 | H=17 | Cl=1 | N=6 | O=2 |
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| smiles = Clc4cccc3n2cnc(c1nc(on1)CN(C)C)c2CN(C(=O)c34)C |
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| 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 |
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| StdInChIKey = JCYLWUVDHLVGER-UHFFFAOYSA-N |
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| bioavailability = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category = |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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}} |
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'''EVT-201''' is a [[benzodiazepine]] [[chemical derivative|derivative]] [[drug]] and [[partial agonist|partial]] [[positive allosteric modulator]] of the [[benzodiazepine site]] of the [[GABAA receptor|GABA<sub>A</sub> receptor]].<ref name="Guilleminault2010">{{cite book| vauthors = Guilleminault C |title=Sleep Medicine|url=https://books.google.com/books?id=np1NaFTF_CQC&pg=PA574|year=2010|publisher=Elsevier Health Sciences|isbn=978-1-4377-1836-2|pages=574–}}</ref> It has 2–4-fold higher functional [[affinity (pharmacology)|affinity]] for the [[GABRA1|α<sub>1</sub> subunit]] relative to the [[GABRA2|α<sub>2</sub>]], [[GABRA3|α<sub>3</sub>]], and [[GABRA5|α<sub>5</sub> subunit]]s and significantly less [[intrinsic activity]] in comparison to currently-marketed benzodiazepines and the [[Z-drug]]s.<ref name="MontiPandi-Perumal2010">{{cite book| vauthors = Monti JM, Pandi-Perumal SR, Möhler H |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}}</ref> 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 effect]]s, such as [[motor incoordination]].<ref name="MontiPandi-Perumal2010" /> The drug was originally developed by [[Hoffmann-La Roche|Roche]], based on [[preclinical]] data, as a non-[[sedation|sedating]] [[anxiolytic]], but was found to produce [[sedation]] in humans in [[Phases of clinical research#Phase I|phase I]] [[clinical trial]]s. For this reason, it was subsequently licensed to Evotec, which is now developing it for the treatment of insomnia.<ref name="MontiPandi-Perumal2010" /> {{as of|2007}}, EVT-201 has completed [[Phases of clinical research#Phase II|phase II]] clinical trials for this indication, with positive findings reported.<ref name="Plunkett2007">{{cite book| vauthors = Plunkett JW |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–}}</ref> {{as of|2015|August}}, [[Phases of clinical research|Phase II]] development is ongoing in [[China]].<ref>{{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|access-date=30 November 2015}}</ref> |
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==See also== |
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* [[List of investigational sleep drugs]] |
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==References== |
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{{Reflist|2}} |
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==External links== |
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* [http://adisinsight.springer.com/drugs/800023883 EVT-201 - AdisInsight] |
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{{Insomnia pharmacotherapies}} |
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{{GABAAR PAMs}} |
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{{Benzodiazepines}} |
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[[Category:Dimethylamino compounds]] |
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[[Category:Chloroarenes]] |
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[[Category:Experimental drugs]] |
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[[Category:GABAA receptor positive allosteric modulators]] |
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[[Category:Hypnotics]] |
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[[Category:Imidazobenzodiazepines]] |
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[[Category:Oxadiazoles]] |
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[[Category:Sedatives]] |
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{{sedative-stub}} |
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Latest revision as of 18:49, 18 April 2024
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