I-Brexanolone (516-54-1) powder - Umhlinzeki Wefektri Yomkhiqizi
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I-Brexanolone

Isilinganiselwa: Isigaba:

Product Incazelo

Izici Eziyisisekelo

Igama Product I-Brexanolone
CAS Inombolo 516-54-1
Formula Yamamolekhula C21H34O2
Isisindo sesisindo 318.501
omqondofana I-Allopregnanolone

I-Brexanolone

516-54-1

I-Allotetrahydroprogesterone

I-Allopregnan-3alpha-ol-20-eyodwa

ukubukeka powder emhlophe
Isitoreji nokuphatha Okomile, okumnyama naku-0 - 4 C okwesikhashana (izinsuku kuya emasontweni) noma -20 C isikhathi eside (izinyanga kuya eminyakeni) ..

 

Incazelo yeBrexanolone

I-Brexanolone iyi-anti-depressant eyingqayizivele, ehlinzekwa ngemithambo yegazi, esetshenziswa ekwelashweni kokucindezeleka okulingene kuya kokubi kakhulu kwangemva kokubeletha. Ezivivinyweni zokwelashwa kwangaphambili, ukwelashwa kwe-brexanolone bekungahlotshaniswa nezinga elinyukile lokuphakama kwe-serum aminotransferase, futhi alixhunywanga ezimweni zokulimala okuqinile kwesibindi emtholampilo.

IBrexanolone futhi iyi-3-hydroxy-5alpha-pregnancy-20-eyodwa lapho iqembu le-hydroxy elisesikhundleni 3 line-alpha-configuration. I-metabolite ye-progesterone ye-sex sex futhi isetshenziselwa ukwelashwa kokucindezeleka kwangemva kokubeletha kwabesifazane. Inendima njenge-metabolite yomuntu, i-antidepressant, i-modulator ye-GABA, i-anesthetic ye-intravenous kanye ne-sedative.

 

Indlela yokusebenza yeBrexanolone

Indlela yokusebenza ye-brexanolone ayaziwa ngokugcwele. IBrexanolone ukwakheka okunamanzi kwe-allopregnanolone. I-Allopregnanolone iyi-metabolite enkulu ye-progesterone. Izinga le-allopregnanolone liyaqhubeka nokukhuphuka nge-progesterone ngesikhathi sokukhulelwa neliphezulu kakhulu ku-trimester yesithathu. I-Allopregnanolone iyi-steroid enamandla ne-endogenous neuroactive eguqula ukuthokozeka kwe-neuronal ngokusebenzisa ukuguquguquka okuhle kwe-allosteric ku-synaptic kanye ne-extrasynaptic gamma-aminobutyric acid (GABA) yohlobo lwe-A receptors. I-extrasynaptic GABA type A receptors mediate inhibition ye-tonic eyenza indlela ye-allopregnanolone ihluke uma iqhathaniswa ne-benzodiazepines elawula ukuvinjelwa kwe-phasic ku-GABA type A receptors.

 

Isicelo seBrexanolone

IBrexanolone yisidakamizwa sokuqala esake savunywa yi-US FDA ngokukhethekile ekwelapheni ukucindezeleka kwangemva kokubeletha (PPD) kwabesifazane abadala. Njengoba i-PPD, njengezinye izinhlobo ezahlukahlukene zokudangala, ibonakala ngemizwa yokudabuka, ukungabi nalutho noma ukuzizwa unecala, ukukhubazeka kwengqondo, kanye / noma umbono wokuzibulala, kubhekwa njengesimo esisongela impilo. Ucwaningo luthole ukuthi i-PPD ingaba nemiphumela emibi kakhulu ekuzibopheni komama nezinsana nasekuthuthukisweni kwezingane kamuva. Ukuthuthukiswa nokutholakala kwe-brexanolone ekwelapheni i-PPD kwabesifazane abadala ngemuva kwalokho kunikeza ukwelashwa okusha nokuthembisayo lapho bekukhona okumbalwa ngaphambili. Ngokuyinhloko, ukusetshenziswa kwe-brexanolone ekwelapheni i-PPD kuzungezwe ngesithembiso ngoba kusebenza njengengxenye yokwengeza yokwenziwa kwamaphutha e-endo native brexanolone (allopregnanolone) kwabesifazane abangemva kokubeletha abangaba sengozini ye-PPD kanti imishanguzo evame ukusetshenziswa yokulwa nokudangala icela izenzo lungisa ubukhona nomsebenzi wezinto ezifana ne-serotonin, norepinephrine, kanye / noma i-monoamine oxidase kepha ungalamuli imisebenzi ehambelana ngqo ne-PPD njengokushintshashintsha kwemvelo emazingeni ama-endo native steroids neuroactive njenge-allopregnanolone. Futhi ekugcineni, noma ngabe i-brexanolone kungenzeka ukuthi ibhekene nokuhlolwa komtholampilo ukuphenya amakhono ayo okwelapha isimo se-super-refractory epilepticus, kubonakala sengathi ezinye zalezo zifundo zehlulekile ukuhlangabezana neziphetho eziyinhloko eziqhathanisa impumelelo ekulunyweni kwama-ejenti olayini wesithathu kanye nokuxazululwa kwamandla isimo esisongela ukuphila isithuthwane nge-brexanolone vs. placebo lapho singezwa ekunakekelweni okujwayelekile.

 

Imiphumela emibi ye-Brexanolone & Isexwayiso

I-Brexanolone ihlanganiswa kakhulu nemigwaqo eminingi ngakho-ke akunakwenzeka ukuthi ibe nokuxhumana okuphawulekayo kwezidakamizwa. I-CYP2C9 ukuphela kwe-cytochrome P450 enzyme ekhombise ukuthi ivinjelwe yi-brexanolone ezifundweni ze-in vitro. Ucwaningo lokuxhumana ngemitholampilo lwehlulekile ukukhombisa noma yiziphi izinguquko ku-pharmacokinetics lapho i-brexanolone yayiphathwa nge-phenytoin, i-substrate ye-CYP2C9. Amandla okuhlukumeza nawo akhonjisiwe ukuthi aphansi, njengoba kufakazelwa ukungafani kwemibiko ezenzakalelayo uma kuqhathaniswa ne-placebo. Ngokuya ngomthelela wokukhubazeka kwe-hepatic ne-renal ku-pharmacokinetics, bekungekho zinguquko ekubekezelelekeni kweziguli ezinesifo sesibindi esilinganayo kuya kwesibucayi, futhi akukho zilungiso zomthamo ebezidingeka kwizifo zezinso ezinzima. Kodwa-ke, i-ejenti encibilikisa i-SBECD ingaqongelela ezigulini ezinokukhubazeka okukhulu kwezinso, ngakho-ke i-brexanolone akufanele inikezwe iziguli ezinesifo sezinso sokugcina.

 

Izikhombo

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[7] UJohannsen BM, uLarsen JT, uLaursen TM, uBergink V, uMeltzer-Brody S, uMunk-Olsen T. Konke-Isizathu Sokufa Kwabesifazane Abanezifo Ezinzima Zokubeletha Kwangemva Kokubeletha. NginguJ J Psychiatry. 2016 Juni 01; 173 (6): 635-42. [I-PMC i-athikili yamahhala] [I-PubMed].

[8] Noorlander Y, Bergink V, van den Berg MP. Ukubonwa nokubonwa kokuxhumana komama nengane ngesikhathi sokulaliswa esibhedlela nokukhululwa ekucindezelekeni kwangemva kokubeletha kanye nasengqondweni. I-Arch Womens Ment Health. 2008; 11 (1): 49-56. [I-PubMed].