Brexanolone (516-54-1) poda - Mugadziri Fekitori Mutengesi
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Brexanolone

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Product Description

Basic Hunhu

Product Name Brexanolone
CAS Number 516-54-1
Molecular Formula C21H34O2
Formula Weight 318.501
Synonyms Allopregnanolone

Brexanolone

516-54-1

Allotetrahydroprogesterone

Allopregnan-3alpha-ol-20-imwe

Kuonekwa White powder
Kuchengeta uye Kubata Dry, rima uye nenguva 0 - 4 C kuti pfupi izwi (mazuva mavhiki) kana -20 C kwenguva yakareba (mwedzi makore) ..

 

Tsananguro yeBrexanolone

Brexanolone yakasarudzika, yakafambiswa inofambiswa, neuroactive steroidal antidepressant inoshandiswa pakurapa kwekuyera-kusvika-kwakasimba kusununguka kwekusununguka. Mune prelicensure kiriniki miedzo, brexanolone Therapy haina kubatana neyakawedzera mwero weserum aminotransferase kukwidziridzwa, uye haina kubatanidzwa kune zviitiko zvekiriniki zvinooneka zvakanyanya kukuvara kwechiropa.

Brexanolone zvakare iri 3-hydroxy-5alpha-nhumbu-20-imwe umo iro hydroxy boka panzvimbo 3 rine alpha-gadziriso. Iyo metabolite yeiyo pabonde kemikari progesterone uye inoshandiswa pakurapa kwekusununguka mushure mekusununguka mune vakadzi. Iyo ine basa seyemetabolite yemunhu, antidepressant, GABA modulator, intravenous anesthetic uye sedative.

 

Brexanolone Mashandiro Ekuita

Mechanism yekuita kwe brexanolone haina kuzivikanwa zvizere. Brexanolone inogadzirwa nemvura ine allopregnanolone. Allopregnanolone ndiyo yakakura metabolite yeprogesterone. Matanho eallopregnanolone anoenderera mberi achikwira neprogesterone panguva yekuzvitakura neyepamusoro-soro mune yechitatu trimester. Allopregnanolone ine simba, inogumira neuroactive steroid iyo inogadzirisa neuronal kusununguka kuburikidza neakanaka allosteric modulation pane iyo synaptic uye extrasynaptic gamma-aminobutyric acid (GABA) mhando A inogamuchira. Iyo extrasynaptic GABA mhando A receptors inopindirana tonic inhibition iyo inoita allopregnanolone's mashandiro akasarudzika kana ichienzaniswa ne benzodiazepines iyo inopindirana neiyo phasic inhibition paGABA mhando A receptors.

 

Brexanolone Chikumbiro

Brexanolone ndiwo mushonga wekutanga kumbobvumirwa neUS FDA yakanyanya kurapwa kwekusununguka mushure mekusununguka (PPD) mune vakuru vakadzi. Sezvo PPD, sedzimwe dzakasiyana mhando dzekushungurudzika, inoratidzirwa nemanzwiro ekusuwa, kusakosha kana mhosva, kukanganisika kwekuziva, uye / kana pfungwa dzekuzviuraya, inoonekwa seyakaisa hupenyu panjodzi. Zvidzidzo zvakazoona kuti PPD inogona kuve nemhedzisiro yakaipa pahukama hwevacheche nemucheche uye mushure mekukura kwevana. Iko kuvandudza uye kuwanikwa kwe brexanolone yekurapa kwePPD mune vanhukadzi vakuru kunozopa imwe nyowani uye inovimbisa kurapa uko vashoma vaivapo kare. Kunyanya, kushandiswa kweBrexanolone pakurapa PPD kwakakomberedzwa nevimbiso nekuti inoshanda muchikamu seyakakwenenzverwa yekuwedzera kushomeka mune endo native brexanolone (allopregnanolone) mumashure mekusununguka vakadzi vanokanganisa PPD nepo mishonga inowanzo shandiswa yekurwisa-kushushikana inokonzeresa zviito zvinogona chengetedza huvepo uye chiitiko chezvinhu zvakaita serotonin, norepinephrine, uye / kana monoamine oxidase asi usayananise zviitiko zvakanangana nePPD sekushanduka kwechisikigo mumatanho endogenous neuroactive steroids senge allopregnanolone. Uye pakupedzisira, kunyangwe brexanolone inogona zvakare kunge iri kuitiswa kiriniki miedzo kuti iongorore kugona kwayo kurapa yakanyanya-inoratidzira chimiro epilepticus, zvinoita sekunge zvimwe zvidzidzo zvakadaro zvakakundikana kusangana nemagumo ekutanga ayo anofananidza kubudirira mukurumwa kwevatatu-mutsara vamiririri uye kugadzirisa kweanogona hupenyu hunotyisidzira chimiro epilepticus ine brexanolone vs. placebo painowedzerwa kune yakajairwa-yekutarisira.

 

Brexanolone Side Mhedzisiro & Yambiro

Brexanolone yakanyanyisa kugadziriswa nenzira dzakawanda uye nekudaro hazvigone kuve nekudyidzana kwezvinodhaka-zvinodhaka. CYP2C9 ndiyo chete cytochrome P450 enzyme iyo yakaratidza kudziviswa ne brexanolone mune in vitro zvidzidzo. Kiriniki yekudyidzana kudzidza kwakatadza kuratidza chero shanduko mu pharmacokinetics apo brexanolone yaishandiswa pamwe ne phenytoin, iyo CYP2C9 substrate. Kushungurudza kugona kwakaratidzirwawo kuve kwakaderera, sezvinoonekwa nekusava nemusiyano mumishumo yekuzviisa pasi ichienzaniswa ne placebo. Panyaya yekukanganisa kwehepatic uye renal kukanganisika pane pharmacokinetics, pakanga pasina shanduko mukutsungirira mune varwere vane mwero kusvika kune yakakomba chirwere chechiropa, uye hapana gadziridzo yedosi yaidikanwa kune yakakomba itsvo chirwere. Zvisinei, iyo inogadzirisa mumiriri SBECD inogona kuunganidzwa mune varwere vane kukomba kwakakomba kweitsvo, uye nekudaro brexanolone haifanire kupihwa kune varwere vane yekupedzisira-danho renal chirwere.

 

Reference

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