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Allopregnanolone

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Allopregnanolone, e taʻua foi Sepranolone ma Isopregnanolone, o le GABA talimalo fesuiaʻi le vailaʻau feteʻenaʻi ma le 11-betahydroxysteroid dehydrogenase ituaiga 1 (11β-HSD1)…

Faamatalaga oloa

Tulaga Autu

Igoa oloa Allopregnanolone
Numera CAS 516-55-2
Faiga Faʻavae Molecular C21H34O2
Fua Faatatau o le Umi 318.5
Synonyms NSC-97078; U-0949; UC-1010; NSC97078; U0949; UC1010; NSC 97078; U 0949; UC 1010; Isopregnanolone; Allopregnanolon; Sepranolone; 516-55-2; 5alpha-Pregnan-3beta-ol-20-tasi
Faʻaaliga Paʻu paʻu
Teuina ma Taulimaina Faʻamago, pogisa ma i le 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso) poʻo le -20 C mo se taimi umi (masina i tausaga).

 

Allopregnanolone Faʻamatalaga

Allopregnanolone, e taʻua foi Sepranolone ma Isopregnanolone, o le GABA receptor o loʻo faʻataʻitaʻia le antagonist steroid ma le 11-betahydroxysteroid dehydrogenase ituaiga 1 (11β-HSD1). O le Sepranolone ose vaega malosi o le neura, e gaosia lava i le tino, e suia ai aafiaga o le Allopregnanolone (ALLO). O le ALO o se neurosteroid malosi o loʻo aʻafia i faʻatiga-ma faʻamalosi-e fesoʻotaʻi tulaga e amata mai Tourette i OCD, PTSD, faʻamalosia taʻalo faitupe, vaisu, PMDD, Menstrual Migraine.

 

Allopregnanolone Faʻagaioiga o gaioiga

Fetuʻunaʻiga faʻamalosi

Allopregnanolone o se endogenous taofiofia maitaga neurosteroid. Na faia mai le progesterone, ma o se lelei allosteric modulator o gaioiga a le amin-aminobutyric acid (GABA) i le GABAA talipapa. Allopregnanolone ei ai aafiaga e tutusa ma isi lelei allosteric modulator o le GABA gaioiga i le GABAA talimalo e pei o le benzodiazepines, e aofia ai le popolevale, faʻafilemuina, ma le anticonvulsant gaoioiga. Endogenously gaosia allopregnanolone faʻaaogaina se neurophysiological matafaioi e ala i le faʻalelei lelei o le GABAA receptor ma faʻataʻitaʻia le gaioiga a le tele lelei allosteric modulator ma agonists i GABAA talimalo.

Allopregnanolone galue o se sili ona malosi lelei allosteric modulator o le mauaina GABAA. E ui o le allopregnanolone, e pei o isi mea faʻaleagaina e pei o le THDOC, e fesuiaʻi lelei suiga uma o le GABAA isoforms, o na isoforms o loʻo iai δ subunits o loʻo faʻaalia ai le malosiaga sili. Allopregnanolone ua maua foi e galue o se lelei allosteric modulator o le GABAA-ρ mauaina, e ui o le aʻafiaga o lenei gaioiga e le manino. I le faʻaopopoga i ana gaioiga i le GABA talimalo, allopregnanolone, pei o le progesterone, ua lauiloa o se le lelei allosteric modulator o nACh talimalo, ma e foliga mai foi e avea o se le lelei allosteric modulator o le 5-HT3 talimalo. Faʻatasi ai ma isi faʻafitauli o le neurosteroids, allopregnanolone foliga mai e leai pe leai foi se gaioiga i isi ligand-gated ion auala, e aofia ai le NMDA, AMPA, kainate, ma glycine taliaina.

 

Aafiaga Antidepressant

O le auala e le iloa ai le neurosteroid GABAA talimalo PAM e pei o le brexanolone aafiaga antidepressant. O isi GABAA talimalo PAMs, pei o benzodiazepines, e le o ni antidepressants ma e leai se aoga faʻamaonia, e ui lava i fomaʻi faʻatonuina Alprazolam mo faʻanoanoaga i taimi ua tuanaʻi. Neurosteroid GABAA talimalo PAM e iloa e fegalegaleai ma GABAA talimalo ma sub-faitau aofaʻi tagata ese nai lo benzodiazepines. Mo se faʻataʻitaʻiga, atonu e sili atu le faʻatatau o le GABAA receptor-potentiating neurosteroids i le unit subunit-o loʻo i ai ni talileleia o le GABAA, ma faʻaleleia atili ai le tonic ma le phasic taofi e faʻatonutonuina e le au faʻaalia o le GABAA. E mafai foi ona avea neurosteroids pei allopregnanolone ono galue i luga o isi sini, e aofia ai membrane progesterone taliaina, T-ituaiga voltage-gated calcium auala, ma isi, e fefautuaai antidepressant aafiaga.

 

Talosaga Allopregnanolone

Allopregnanolone o se mea masani e gaosia vailaʻau e galue i luga o le faiʻai. I le avea ai ma vailaʻau, e faʻatau atu i lalo ole igoa Zulresso ma faʻaaoga e togafitia ai le faʻanoanoaga ole tina failele. E faʻaaogaina i le tuiina i totonu o se uaua i luga o le 60-itula vaitaimi i lalo o le vaʻavaʻai fomaʻi.

Aʻafiaga o Allopregnanolone ono aofia ai le faʻamalieina, moe, moe mago, vevela susulu, ma leiloa o le malamalama. O le neurosteroid ma galue o se lelei allosteric modulator o le GABAA talimalo, o le autu autu faʻamoemoe o le taofiofia neurotransmitter γ-aminobutyric acid (GABA).

Allopregnanolone na faʻamaonia mo le faʻaogaina o vailaʻau i le Iunaite Setete i le 2019. O le US Food and Drug Administration (FDA) manatu o se muamua-i-vasega vailaʻau. Ole taimi umi ole pulega, faʻapea foi ma le tau mo togafitiga e tasi le taimi, na faʻatupuina atugaluga e uiga i le faʻaaogaina o le tele o fafine.

 

Tusitaiala

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