Английская Википедия:Esmodafinil

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Версия от 15:24, 4 марта 2024; EducationBot (обсуждение | вклад) (Новая страница: «{{Английская Википедия/Панель перехода}} {{Short description|Unmarketed enantiomer of modafinil}} {{cs1 config|name-list-style=vanc}} {{Chembox | ImageFile = (S)-(+)-modafinil.svg | ImageCaption = (''S'')-(+)-modafinil | IUPACName = 2-[(''S'')-benzhydrylsulfinyl]acetamide |Section1={{Chembox Identifiers | CASNo = 112111-47-4 | ChEBI = 77591 | ChEMBL = 1672355 | ChemSpiderID = 9348458 | EC_number = 807-091-3 | PubChem = 11173...»)
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Шаблон:Short description Шаблон:Cs1 config Шаблон:Chembox Esmodafinil (also known as (S)-modafinil or (+)-Modafinil) is the enantiopure isolation of the (S) enantiomer of modafinil. Unlike armodafinil, esmodafinil has never been marketed on its own.[1]

Esmodafinil is suspected to be less clinically useful for treating conditions that modafinil and armodafinil are marketed for, such as narcolepsy, sleep-shift work disorder, and obstructive sleep apnea.[2]

Pharmacology

Pharmacokinetics

Esmodafinil possesses a substantially shorter half life (3–5 hours) compared to armodafinil (10–13 hours).[3]

Pharmacodynamics

Esmodafinil has a 3 times lower affinity for the dopamine transporter compared to armodafinil.[3] Both enantiomers of modafinil preferentially bind to the dopamine transporter in an inward facing conformation.[3][4]

Preclinical research

Esmodafinil has been researched for the treatment of cocaine addiction.[3][4] Like armodafinil, esmodafinil attenuates the effects of cocaine by occupying the dopamine transporter.[4] While doing so, esmodafinil increases dopamine in the nucleus accumbens to a lesser extent than cocaine.[3] However, the short half-life of esmodafinil has been cited as reason to investigate armodafinil as a cocaine addiction treatment instead.[3]

Analysis in biological samples

Modafinil is considered a stimulant doping agent and as such is prohibited by World Anti-Doping Agency in sports competitions.[5] The validated methods are researched to separately quantify modafinil enantiomers in the real samples.[6]

References

Шаблон:Reflist Шаблон:Stimulants