Allopregnanolone (516-55-2) lulú - Olupese Ile-iṣẹ Ẹlẹda
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Allopregnanolone

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Allopregnanolone, ti a tun mọ ni Sepranolone ati Isopregnanolone, jẹ olugba GABA ti n ṣatunṣe antagonist sitẹriọdu ati iru 11-betahydroxysteroid dehydrogenase type 1 (11β-HSD1)…

Ọja Apejuwe

Awọn Abuda Ipilẹ

ọja orukọ Allopregnanolone
CAS Number 516-55-2
molikula agbekalẹ C21H34O2
Ilana iwuwo 318.5
Awọn Synonyms NSC-97078; U-0949; UC-1010; NSC97078; U0949; UC1010; NSC 97078; U 0949; UC 1010; Isopregnanolone; Allopregnanolon; Sepranolone; 516-55-2; 5alpha-Oyun-3beta-ol-20-ọkan
irisi White lulú
Ifipamọ ati mimu Gbẹ, okunkun ati ni 0 - 4 C fun igba kukuru (awọn ọjọ si awọn ọsẹ) tabi -20 C fun igba pipẹ (awọn oṣu si ọdun).

 

Apejuwe Allopregnanolone

Allopregnanolone, ti a tun mọ ni Sepranolone ati Isopregnanolone, jẹ olugba GABA ti n ṣatunṣe antagonist sitẹriọdu ati iru 11 (1β-HSD11) dehydrogenase 1-betahydroxysteroid. Sepranolone jẹ ẹya iṣan ti iṣan ti o lagbara, ti a ṣe ni ti ara ninu ara, ti o ṣe atunṣe awọn ipa ti Allopregnanolone (ALLO). ALLO jẹ neurosteroid ti o ni agbara ti o wa ninu wahala- ati awọn ipo ti o ni agbara mu lati Tourette si OCD, PTSD, ayo ti o ni ipa, afẹsodi, PMDD, Migraine Iṣọnṣọn.

 

Ilana Allopregnanolone ti Iṣe

Awọn ibaraẹnisọrọ molikula

Allopregnanolone jẹ neurosteroid oyun onidena inhibitory. O ti ṣe lati progesterone, ati pe o jẹ modulator allosteric rere ti iṣe ti γ-aminobutyric acid (GABA) ni olugba GABAA. Allopregnanolone ni awọn ipa ti o jọra ti awọn ti awọn modulata allosteric rere miiran ti iṣẹ GABA ni olugba GABAA gẹgẹbi awọn benzodiazepines, pẹlu anxiolytic, sedative, ati iṣẹ adaṣe. Endogenously ṣe agbejade allopregnanolone n ṣe ipa ti neurophysiological nipasẹ titọ-iṣatunṣe ti olugba GABAA ati ṣe atunṣe iṣe ti ọpọlọpọ awọn modulators allosteric rere ati awọn agonists ni olugba GABAA.

Allopregnanolone n ṣiṣẹ bi modulator allosteric ti o ni agbara ti o lagbara pupọ ti olugba GABAA. Lakoko ti allopregnanolone, bii awọn neurosteroid inhibitory miiran bii THDOC, daadaa ṣe atunṣe gbogbo awọn isoforms olugba GABAA, awọn ipinya wọnyẹn ti o ni awọn ipin-kekere ṣe afihan agbara ti o tobi julọ. A tun rii Allopregnanolone lati ṣiṣẹ bi modulator allosteric ti o dara ti olugba GABAA-,, botilẹjẹpe awọn iṣe ti iṣe yii koyewa. Ni afikun si awọn iṣe rẹ lori awọn olugba GABA, allopregnanolone, bii progesterone, ni a mọ lati jẹ modulator allosteric odiwọn ti awọn olugba nACh, ati pe o tun han lati ṣe bi modulator allosteric odi ti olugba 5-HT3. Pẹlú pẹlu awọn neurosteroid inhibitory miiran, allopregnanolone han lati ni kekere tabi ko si igbese ni awọn ikanni dẹlẹ ligand-gated miiran, pẹlu awọn NMDA, AMPA, kainate, ati awọn olugba glycine.

 

Awọn ipa Antidepressant

Ilana ti eyiti awọn PAM olugba olugba GABAA bii brexanolone ni awọn ipa ipanilara jẹ aimọ. Awọn PAM olugba GABAA miiran, gẹgẹ bi awọn benzodiazepines, ko ni ronu bi awọn antidepressants ati pe ko ni ipa ti a fihan, botilẹjẹpe awọn oniwosan ti n ṣalaye Alprazolam fun ibanujẹ ni igba atijọ. Neurosteroid GABAA olugba olugba PAMs ni a mọ lati ṣepọ pẹlu awọn olugba GABAA ati awọn olugbe kekere yatọ si awọn benzodiazepines. Gẹgẹbi awọn apẹẹrẹ, olugba GABAA-ti o ni agbara awọn neurosteroids le ni iṣojulọyin δ awọn olugba GABAA ti o ni subunit, ki o mu ki iṣan tonic ati phasic dojukọ nipasẹ awọn olugba GABAA. O tun ṣee ṣe pe awọn neurosteroids bi allopregnanolone le ṣiṣẹ lori awọn ibi-afẹde miiran, pẹlu awọn olugba progesterone membrane, awọn ikanni kalisiomu ti a fi agbara mu iru T, ati awọn omiiran, lati ṣe ilaja awọn ipa antidepressant.

 

Ohun elo Allopregnanolone

Allopregnanolone jẹ sitẹriọdu ti iṣelọpọ ti iṣelọpọ ti o ṣiṣẹ lori ọpọlọ. Gẹgẹbi oogun, o ta labẹ orukọ iyasọtọ Zulresso ati pe o lo lati ṣe itọju ibanujẹ ọmọ lẹhin ọjọ. O ti lo nipasẹ abẹrẹ sinu iṣọn kan lori akoko 60-wakati labẹ abojuto iṣoogun.

Awọn ipa ẹgbẹ ti Allopregnanolone le pẹlu ifilọra, oorun, ẹnu gbigbẹ, awọn itanna to gbona, ati isonu ti aiji. O jẹ neurosteroid ati pe o ṣe bi modulator allosteric ti o dara ti olugba GABAA, ibi-afẹde pataki ti ẹda ti neurotransmitter inhibitory γ-aminobutyric acid (GABA).

A fọwọsi Allopregnanolone fun lilo iṣoogun ni Amẹrika ni ọdun 2019. US Food and Drug Administration (FDA) ka pe o jẹ oogun-kilasi akọkọ. Akoko iṣakoso gigun, bii idiyele fun itọju akoko kan, ti gbe awọn ifiyesi dide nipa iraye si fun ọpọlọpọ awọn obinrin.

 

Reference

[1] Lionetto L, De Andrés F, Capi M, Curto M, Sabato D, Simmaco M, Bossù P, Sacchinelli E, Orfei MD, Piras F, Banaj N, Spalletta G. LC-MS / MS igbekale nigbakan ti allopregnanolone, epiallopregnanolone, pregnanolone, dehydroepiandrosterone ati dehydroepiandrosterone 3-imi-ọjọ ninu pilasima eniyan. Itan-jinlẹ. Oṣu Kẹwa 2017; 9 (6): 527-539. ṣe: 10.4155 / bio-2016-0262. PMID ti PubMed: 28207286.

[2] Horishita T, Yanagihara N, Ueno S, Sudo Y, Uezono Y, Okura D, Minami T, Kawasaki T, Sata T. Neurosteroids allopregnanolone imi-ọjọ ati imi-ọjọ sulfate ni ipa ti o yatọ lori α ipin ti iṣuu soda ti o ni foliteji awọn ikanni Nav1.2, Nav1.6, Nav1.7, ati Nav1.8 ti a ṣalaye ninu oocytes xenopus. Anesthesiology. Oṣu Kẹsan 2014; 121 (3): 620-31. ṣe: 10.1097 / ALN.0000000000000296. PMID ti PubMed: 24809977.

[3] Zorumski CF, Paul SM, Covey DF, Mennerick S (Oṣu kọkanla 2019). “Neurosteroids bi aramada antidepressants ati anxiolytics: GABA-A awọn olugba ati ju”. Neurobiology ti Wahala. 11: 100196. doi: 10.1016 / j.ynstr.2019.100196. PMC 6804800. PMID 31649968.

[4] Warner, MD; Peabody, CA; Whiteford, HA; Hollister, LE (Oṣu Kẹrin ọdun 1988). “Alprazolam gege bi antidepressant”. Iwe akosile ti Aisan Iṣọn-iwosan. 49 (4): 148-150. ISSN 0160-6689. PMID 3281931.

[5] Srisurapanont, M.; Boonyanaruthee, V. (1997). Alprazolam ati awọn antidepressants bošewa ni itọju ti ibanujẹ: apẹẹrẹ-igbekale ti ipa antidepressant. Ile-iṣẹ fun Awọn atunyẹwo ati Itankale (UK). PMID 9175386.

[6] Reddy DS (2010). Neurosteroids: ipa ailopin ninu ọpọlọ eniyan ati awọn agbara itọju. Pirogi Ọpọlọ Res. Ilọsiwaju ni Iwadi Brain. 186. oju-iwe 113-37. ṣe: 10.1016 / B978-0-444-53630-3.00008-7. ISBN 9780444536303. PMC 3139029. PMID 21094889.

[7] Bullock AE, Clark AL, Grady SR, Robinson SF, Slobe BS, Marks MJ, et al. (Oṣu kẹfa ọdun 1997). “Neurosteroids ṣe modulate iṣẹ olugba ti nicotinic ni striatal eku ati synaptosomes thalamic”. Iwe akosile ti Neurochemistry. 68 (6): 2412–23. ṣe: 10.1046 / j.1471-4159.1997.68062412.x. PMID 9166735.

[8] Slavíková B, Bujons J, Matyáš L, Vidal M, Babot Z, Krištofíková Z, Suñol C, Kasal A. Allopregnanolone ati awọn analogues pregnanolone ti a tunṣe ninu oruka C: iṣelọpọ ati iṣẹ. J Med Chem. 2013 Oṣu Kẹta Ọjọ 28; 56 (6): 2323-36. ṣe: 10.1021 / jm3016365. PMID ti PubMed: 23421641.