I-Brexanolone (516-54-1) ipowder-Umthengisi weFektri yoMvelisi
I-AASraw ivelisa i-Cannabidiol (CBD) ipowder kunye ne-Hemp ebalulekileyo yeoyile ngobuninzi!

IBrexanolone

Akukho kalo Udidi:

Ingcaciso yeMveliso

Iimpawu ezisisiseko

Igama lemveliso IBrexanolone
Inani leCAS 516-54-1
I-Molecular Formula C21H34O2
Ubukhulu beFormula 318.501
Iintetho ezifanayo Zonke iinkonzo ze-intanethi

IBrexanolone

516-54-1

I-allotetrahydroprogesterone

Allopregnan-3alpha-ol-20-nye

Kubonakala Powder
Ukugcina nokuPhatha Okomileyo, omnyama kunye no-0 - 4 C okwexeshana (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (iinyanga ukuya kwiminyaka).

 

Inkcazo yeBrexanolone

I-Brexanolone iyodwa, ilawulwa nge-intravenously, neuroactive steroidal antidepressant esetyenziselwa unyango lokudakumba okuphakathi ukuya koxinzelelo lwasemva kokubeleka. Kwizilingo zokuqala zeklinikhi, unyango lwe-brexanolone aluzange luhambelane nenqanaba elonyukayo lokuphakama kwe-serum aminotransferase, kwaye khange linxulunyaniswe neemeko zokonzakala kwesibindi.

I-Brexanolone ikwayi-3-hydroxy-5alpha-pregnan-20-enye apho iqela le-hydroxy kwindawo ye-3 ine-alpha-configuration. Yimetabolite yehomoni yesini yeprogesterone kwaye isetyenziselwa unyango loxinzelelo lwasemva kokubeleka kwabasetyhini. Inendima njengemetabolite yomntu, i-antidepressant, imodyuli ye-GABA, i-anesthetic efakwa ngaphakathi kunye nokuthomalalisa.

 

Indlela yeBrexanolone yokuSebenza

Indlela yokwenza i-brexanolone ayaziwa ngokupheleleyo. I-Brexanolone yindlela yokwenza amanzi ene-allopregnanolone. I-Allopregnanolone yimetabolite enkulu yeprogesterone. Amanqanaba e-allopregnanolone ayaqhubeka nokunyuka neprogesterone ngexesha lokukhulelwa kwelona liphezulu kwikota yesithathu. I-Allopregnanolone inamandla, i-endo native neuroactive steroid ehlengahlengisa ukonwaba kwe-neuronal ngokusebenzisa imodyuli elungileyo ye-allosteric kwi-synaptic kunye ne-extrasynaptic gamma-aminobutyric acid (GABA) yohlobo lwe-A receptors. Uhlobo lwe-GABA ye-extrasynaptic uhlobo lwee-receptors zilamla i-tonic inhibition eyenza ukuba i-allopregnanolone's mechanism ikhetheke xa ithelekiswa ne-benzodiazepines elawula ukuthintela i-phasic in GABA type A receptors.

 

Isicelo seBrexanolone

IBrexanolone sisiyobisi sokuqala esakha samkelwa yi-US FDA ngokukodwa kunyango loxinzelelo lwasemva kokubeleka (PPD) kubantu ababhinqileyo abadala. Kuba i-PPD, njengezinye iintlobo ezahlukeneyo zoxinzelelo, ibonakaliswa kukuziva ungonwabanga, ukuziva ungenamsebenzi okanye unetyala, ukukhubazeka kwengqondo, kunye / okanye umbono wokuzibulala, uthathwa njengemeko esongela ubomi. Izifundo ziye zafumanisa ukuba i-PPD inokuba neziphumo ezibi kakhulu kwisibophelelo soomama kunye neentsana kunye nakuphuhliso lweentsana kamva. Ukuphuhliswa kunye nokufumaneka kwe-brexanolone kunyango lwe-PPD kubantu ababhinqileyo abadala emva koko kubonelela ngonyango olutsha noluthembisayo apho bambalwa ababekho ngaphambili. Ngokukodwa, ukusetyenziswa kwe-brexanolone ekunyangeni i-PPD ijikelezwe ngesithembiso kuba isebenza njengenxalenye yesongezelelo sokwenzela ukusilela kwi-endo native brexanolone (allopregnanolone) kumanina asemva kokubeleka anokuchaphazeleka kwi-PPD ngelixa amayeza amaninzi asetyenziswa kuxinzelelo. modulate ubukho kunye nomsebenzi wezinto ezifana ne-serotonin, norepinephrine, kunye / okanye i-monoamine oxidase kodwa musa ukulamla imisebenzi enxibelelene ngqo ne-PPD njengokuguquguquka kwendalo kumanqanaba e-endo native neuroactive steroids like allopregnanolone. Kwaye okokugqibela, nangona i-brexanolone isenokuba iphantsi kovavanyo lweklinikhi lokuphanda ubuchule bayo bokunyanga imeko ye-epilepticus ephezulu kakhulu, kuyabonakala ukuba olo phononongo luye lwasilela ukufikelela kwiziphelo eziphambili ezithelekisa impumelelo ekulunyulweni kwearhente yomgca wesithathu kunye nesisombululo imeko ebeka ubomi esichengeni sokuxhuzula nge-brexanolone vs. placebo xa ifakwe kumgangatho wokhathalelo.

 

Iziphumo ebezingalindelekanga zeBrexanolone kunye nesilumkiso

I-Brexanolone idityaniswa kakhulu ziindlela ezininzi kwaye ke akunakulindeleka ukuba ibe nokudibana kweziyobisi. I-CYP2C9 kuphela kwe-cytochrome P450 enzyme ebonakalise ukuba iyathintelwa yi-brexanolone kwizifundo ze-vitro. Isifundo sonxibelelwano ngeklinikhi asiphumelelanga ukubonisa naluphi na utshintsho kwi-pharmacokinetics xa i-brexanolone yayiqhutywa nge-phenytoin, i-CYP2C9 substrate. Amandla okuphatha gadalala kuye kwabonakaliswa ukuba aphantsi, njengoko oku kungqinwa kukungafani kweengxelo ezizezinye xa kuthelekiswa ne-placebo. Ngokwempembelelo yokuphazamiseka kwesibindi kunye nokuphazamiseka kwethambo kwi-pharmacokinetics, kwakungekho lutshintsho kunyamezelo kwizigulana ezinesifo esimndilili ukuya kwisibindi, kwaye akukho luhlengahlengiso lwethamo lwaluyimfuneko kwisifo sezintso. Nangona kunjalo, iarhente yokunyibilikisa i-SBECD inokuqokelelana kwizigulana ezinokukhubazeka okukhulu kwezintso, kwaye ngenxa yoko i-brexanolone akufuneki inikwe abaguli abanesifo sezintso.

 

isingqiniso

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