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Brexanolone

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Product Description

Astaamaha Aasaasiga ah

Product Name Brexanolone
CAS Number 516-54-1
Formula kelli C21H34O2
Miisaanka Nooca 318.501
Isku mid ahaanshaha Allopregnanolone

Brexanolone

516-54-1

Allotetrahydroprogesterone

Allopregnan-3alpha-ol-20-mid

Imaanshaha budo White
Kaydinta iyo Isticmaalka Qalalan, madow iyo 0 - 4 C muddo gaaban (maalmo illaa toddobaadyo) ama -20 C muddo dheer (bilo illaa sannado) ..

 

Sharaxaadda 'Brexanolone'

Brexanolone waa mid khaas ah, oo xididka lagu shubo, neuroactive steroid antidepressant oo loo isticmaalo daaweynta niyad-jabka dhalmada ee dhexdhexaad-ilaa-daran. Marka la eego tijaabooyinka bukaan socodka, daaweynta brexanolone lama xiriirin heerka sii kordhaya ee serum aminotransferase, mana ku xirneyn xaalado caafimaad ahaan u muuqda dhaawac beerka ah.

Brexanolone sidoo kale waa 3-hydroxy-5alpha-pregnan-20-mid taas oo kooxda hydroxy ee booska 3 ay leedahay qaabeynta alfa. Waa dheef-shiid kiimikaad hormoonka galmada ah progesterone waxaana loo isticmaalaa daaweynta murugada umusha ka dib dumarka. Waxay leedahay door sida dheef-shiid kiimikaad bani'aadam ah, antidepressant, a GABA modulator, suuxdiyaha xididka iyo daweynta.

 

Mashruuca Brexanolone ee Waxqabadka

Farsamaynta ficilka brexanolone si buuxda looma yaqaan. Brexanolone waa qaabeynta aqueous ee allopregnanolone. Allopregnanolone waa dheef-shiid kiimikaad weyn ee progesterone. Heerarka allopregnanolone ayaa sii wadaya inay la soo baxaan qanjirka 'progesterone' inta lagu guda jiro uurka iyadoo ugu sarreysa saddexda bilood ee saddexaad. Allopregnanolone waa awood firfircoon, endogenous neuroactive steroid oo wax ka beddeleysa dareemayaasha neerfaha iyada oo loo marayo isku-dhafka allosteric-ka ee 'synaptic' iyo 'extrasynaptic gamma-aminobutyric acid (GABA) type A receptors. Noocyada 'Extrasynaptic GABA type A receptors' waxay dhexdhexaadinayaan ka hortagga tonic taas oo ka dhigaysa farsamooyinka allopregnanolone mid gaar ah marka la barbar dhigo benzodiazepines oo dhexdhexaadiya joojinta ficilka ee nooca GABA nooca A.

 

Codsiga Brexanolone

Brexanolone waa daroogada ugu horeysa ee waligeed ay ansixisay US FDA gaar ahaan daaweynta murugada umusha (PPD) ee dumarka qaangaarka ah. Maaddaama PPD, sida noocyada kale ee kale ee niyad-jabka, lagu gartaa dareemo murugo, qiimo-darro ama dambi, cillad garasho, iyo / ama suuragalnimada is-dilid, waxaa loo tixgeliyaa xaalad naf-gooyo ah. Daraasaduhu waxay sidaas ku ogaadeen in PPD ay si dhab ah ugu yeelan karto saameyn taban oo qoto dheer hooyada iyo dhallaanka iyo horumarka ilmaha dambe. Horumarinta iyo helitaanka brexanolone ee daaweynta PPD ee haweenka qaangaarka ah ayaa markaa kadib bixisa daaweyn cusub oo rajo leh halkaas oo in yar ay jireen ka hor. Gaar ahaan, isticmaalka brexanolone ee daaweynta PPD waxay ku wareegsan tahay balanqaad maxaa yeelay waxay u dhaqantaa qayb ahaan sidii dheellitir dheeri ah oo loogu talagalay cilladaha suurtagalka ah ee brexanolone endogenous (allopregnanolone) ee haweenka dhalmada kadib ee u nugul PPD halka daawooyin badan oo looga hortago niyad-jabka ay muujiyaan ficilo laga yaabo inay wax ka beddel joogitaanka iyo waxqabadka walxaha sida serotonin, norepinephrine, iyo / ama monoamine oxidase laakiin ha dhexdhexaadin howlaha tooska ula xiriira PPD sida isbeddelka dabiiciga ah ee heerarka istiraatiijiyadaha neerfaha ee firfircoon sida allopregnanolone. Ugu dambeyntiina, inkasta oo brexanolone laga yaabo inay sidoo kale ku socoto tijaabooyin caafimaad si loo baaro awooddeeda si loo daaweeyo xaalad qalafsan oo heer sare ah, waxay u muuqataa in qaar ka mid ah daraasadaha noocan oo kale ah ay ku guuldareysteen inay la kulmaan natiijooyinka aasaasiga ah ee isbarbar dhiga guusha naas-nuujinta wakiilada sadarka saddexaad iyo xallinta suurtogalka Xaaladda suuxdinta leh ee nafta halis gelisa oo leh brexanolone iyo placebo markii lagu daro heerka daryeelka.

 

Waxyeelada & Digniinta Brexanolone

Brexanolone waxaa si ballaaran loogu dheeftaa wadooyin badan sidaa darteedna uma badna inay yeeshaan isdhexgal daroogo daroogo oo muhiim ah. CYP2C9 waa cytochrome P450 enzyme oo kaliya oo muujisay in laga hortago brexanolone ee daraasadaha kujira fitamiinada. Daraasad isdhexgal caafimaad ayaa ku guuldareysatay inay muujiso wax isbeddel ah oo ku saabsan farmasokokinetics markii brexanolone la maamuley phenytoin, CYP2C9 substrate. Awoodda xad-gudubka ayaa sidoo kale la muujiyey inay hooseyso, sida lagu caddeeyey inaysan ku kala duwaneyn warbixinnada u gaarka ah marka la barbardhigo placebo. Marka la eego saameynta cagaarshowga iyo kelyaha ee cilladda farmasokokinetikada, ma jirin wax isbeddel ah oo ku saabsan dulqaadka bukaanka qaba cudur beerka oo dhexdhexaad ah ama daran, mana jirin wax isbeddel ah oo qalliin ah oo lagama maarmaan u ah cudurka kelyaha ee daran. Si kastaba ha noqotee, wakiilka xallinta SBECD wuxuu ku urursan karaa bukaanada qaba cillad daran oo kelyaha ah, sidaas awgeed brexanolone ma ahan in la siiyo bukaanada qaba cudurka kelyaha ee marxaladda ugu dambeysa.

 

Tixraaca

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[7] Johannsen BM, Larsen JT, Laursen TM, Bergink V, Meltzer-Brody S, Munk-Olsen T. Dhammaan Sababaha Dhimashada ee Haweenka Dhibaatooyinka Maskaxda ee Dhalashada Kadib. Am J Maskaxda. 2016 Juun 01; 173 (6): 635-42. [Maqaalka bilaashka ah ee PMC] [PubMed].

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