Английская Википедия:EVT-201

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Версия от 09:25, 1 марта 2024; EducationBot (обсуждение | вклад) (Новая страница: «{{Английская Википедия/Панель перехода}} {{Short description|Chemical compound}} {{Drugbox | 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 | image = EVT-201.svg | width = 223 | CAS_number = 308239-86-3 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 6J8AF7CLE4 | ATC_prefix = None | ATC_suffix = | PubChem = 9885841 | DrugBank = |...»)
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Шаблон:Short description Шаблон:Drugbox

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] Шаблон:As of, EVT-201 has completed phase II clinical trials for this indication, with positive findings reported.[3] Шаблон:As of, Phase II development is ongoing in China.[4]

See also

References

Шаблон:Reflist

External links

Шаблон:Insomnia pharmacotherapies Шаблон:GABAAR PAMs Шаблон:Benzodiazepines


Шаблон:Sedative-stub

Партнерские ресурсы
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Разное

  1. ↑ Шаблон:Cite book
  2. ↑ 2,0 2,1 2,2 Шаблон:Cite book
  3. ↑ Шаблон:Cite book
  4. ↑ Шаблон:Cite web
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