Allopregnanolone (516-55-2) phofo - Mofani oa thepa ea moetsi
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Allopregnanolone, e tsejoang hape e le Sepranolone le Isopregnanolone, ke mohanyetsi oa GABA receptor modulating steroid antagonist le 11-betahydroxysteroid dehydrogenase mofuta 1 (11β-HSD1)…

Tlhaloso ea Sehlahisoa

Litšobotsi tsa Motheo

Name Product Letsoalo
Nomoro ea CAS 516-55-2
Molecular Formula C21H34O2
Boima ba 'mele 318.5
Li-synonyms EA-97078-KS U-0949; UC-1010; EA-97078-KS U0949; UC1010; EA-97078-KS U 0949; UC 1010; Isopregnanolone; Allopregnanolon; Sepranolone; EA-516-55-2 5alpha-Pregnan-3beta-ol-20-e le 'ngoe
Ponahalo Pula e tšoeu
Ho Boloka le ho Sebetsana E omme, e lefifi ebile e le 0 - 4 C ka nako e khuts'oane (matsatsi ho isa ho libeke) kapa -20 C nako e telele (likhoeli ho isa ho lilemo).

 

Tlhaloso ea Allopregnanolone

Allopregnanolone, eo hape e tsejoang e le Sepranolone le Isopregnanolone, ke mohanyetsi oa GABA receptor modulating steroid antagonist le 11-betahydroxysteroid dehydrogenase mofuta 1 (11β-HSD1). Sepranolone ke motsoako o matla oa methapo, o hlahisoang ka tlhaho 'meleng, o hlophisang litlamorao tsa Allopregnanolone (ALLO). ALLO ke methapo e matla ea methapo ea kutlo e amehang maemong a amanang le khatello ea maikutlo le ho qobelloa ho tloha Tourette ho ea OCD, PTSD, papali ea chelete e qobelloang, bokhoba ba lithethefatsi, PMDD, Menstrual Migraine.

 

Mokhoa oa Ketso oa Allopregnanolone

Likamano tsa limolek'hule

Allopregnanolone ke tšitiso ea nako e telele e thibelang bokhachane e nang le bokhachane. E entsoe ka progesterone, 'me ke modulator e ntle ea allosteric ea ketso ea γ-aminobutyric acid (GABA) ho GABAA receptor. Allopregnanolone e na le litlamorao tse ts'oanang le tsa li-modulator tse ling tse ntle tsa ketso ea GABA ho GABAA receptor joalo ka benzodiazepines, ho kenyeletsoa khatello ea kelello, sedative le ts'ebetso ea anticonvulsant. E hlahisitsoeng ka ho sa feleng allopregnanolone e na le karolo ea methapo ea kutlo ka ho hlophisa hantle mokamo oa GABAA le ho hlophisa ketso ea li-modulator le li-agonists tse 'maloa tse ntle ho GABAA receptor.

Allopregnanolone e sebetsa e le sesebelisoa se matla sa allosteric modulator ea GABAA receptor. Le ha allopregnanolone, joalo ka li-neurosteroid tse ling tse thibelang ts'oaetso joalo ka THDOC, ka nepo e hlophisa li-isoforms tsohle tsa GABAA, li-isoforms tse nang le li-subunits li bonts'a monyetla o moholo ka ho fetisisa. Allopregnanolone le eona e fumanoe e sebetsa joalo ka modulator e ntle ea allosteric ea mokamo oa GABAA-ρ, leha litlamorao tsa ketso ena li sa hlaka. Ntle le liketso tsa eona ho li-receptors tsa GABA, allopregnanolone, joalo ka progesterone, e tsejoa e le modulator e mpe ea allosteric ea li-receptor tsa nACh, hape e bonahala e sebetsa e le modulator e mpe ea allosteric ea 5-HT3 receptor. Hammoho le li-neurosteroid tse ling tse thibelang, allopregnanolone e bonahala e sena khato e nyane kapa e se na khato ho liteishene tse ling tsa ion tse nang le li-ligand, ho kenyeletsoa li-receptor tsa NMDA, AMPA, kainate le glycine.

 

Litlamorao tsa khatello ea maikutlo

Ha ho tsejoe mokhoa oo li-PAMs tsa receptor tsa GABAA tsa neurosteroid tse kang brexanolone li nang le litlamorao tsa khatello ea maikutlo. Li-PAM tse ling tsa GABAA receptor, tse kang benzodiazepines, ha li nkoe e le li-anti-depressing ebile ha li na tšebetso e netefalitsoeng, leha lingaka li ne li laela Alprazolam bakeng sa khatello ea maikutlo nakong e fetileng. Li-PAM tsa Neurosteroid GABAA receptor PAMs li tsejoa hore li sebelisana le li-receptor tsa GABAA le batho ba tlase ka tsela e fapaneng le ea benzodiazepines. Joaloka mehlala, GABAA receptor-potentiating neurosteroids e kanna ea lebisa tlhokomelo ho li-receptor tsa GABAA tse nang le likaroloana, hape e matlafatse thibelo ea tonic le phasic e buelletsoeng ke li-receptor tsa GABAA. Hape, ho ka etsahala hore li-neurosteroids tse kang allopregnanolone li ka sebetsa ho tse ling, ho kenyeletsoa le membrane progesterone receptors, T-type voltage-gated calcium channels, le tse ling, ho loants'a litlamorao tsa khatello ea maikutlo.

 

Kopo ea Allopregnanolone

Allopregnanolone ke steroid e hlahisoang ka tlhaho e sebetsang bokong. Joaloka moriana, e rekisoa tlasa lebitso la lebitso la Zulresso mme e sebelisetsoa ho phekola khatello ea maikutlo kamora 'pelehi. E sebelisoa ka ente ka mothapong ka nako ea lihora tse 60 tlasa tlhokomelo ea bongaka.

Litla-morao tsa Allopregnanolone li ka kenyelletsa sedation, boroko, molomo o omileng, mahlaseli a chesang le ho lahleheloa ke kelello. Ke neurosteroid mme e sebetsa e le modulator e ntle ea allosteric ea GABAA receptor, sepheo se seholo sa bioloji sa methapo ea methapo ea γ-aminobutyric acid (GABA).

Allopregnanolone e ile ea amoheloa bakeng sa ts'ebeliso ea bongaka United States ka 2019. Tsamaiso ea Lijo le Lithethefatsi ea Amerika (FDA) e e nka e le moriana oa maemo a pele. Nako e telele ea tsamaiso, hammoho le litšenyehelo tsa kalafo ea hanngoe, li hlahisitse matšoenyeho mabapi le phihlello ho basali ba bangata.

 

Reference

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