Allopregnanolone (516-55-2) ntụ ntụ - Onye na-emepụta ihe nrụpụta
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Allopregnanolone

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Allopregnanolone, nke a makwaara dị ka Sepranolone na Isopregnanolone, bụ onye na-anabata ihe GABA na-agbanwe steroid antagonist na ụdị 11-betahydroxysteroid dehydrogenase ụdị 1 (11'-HSD1) XNUMX

Product Description

Njirimara Nhazi

Product Name Allopregnanolone
CAS Number 516-55-2
molekụla Formula C21H34O2
Ụdị Ụdị 318.5
Synonyms NSC-97078; U-0949; UC-1010; NSC97078; U0949; UC1010; NSC 97078; U 0949; UC 1010; Isopregnanolone; Allopregnanolon; Akara; 516-55-2; 5alpha-afọ ime-3beta-ol-20-one
ọdịdị White ntụ ntụ
Nchekwa na Ijikwa Akọrọ, ọchịchịrị na 0 - 4 C maka obere oge (ụbọchị ruo izu) ma ọ bụ -20 C maka ogologo oge (ọnwa ruo afọ).

 

Nkọwa Allopregnanolone

Allopregnanolone, nke a makwaara dị ka Sepranolone na Isopregnanolone, bụ onye na-anabata ihe GABA na-agbanwe steroid antagonist na 11-betahydroxysteroid dehydrogenase type 1 (11β-HSD1). Sepranolone bụ ihe na-agwọ ọrịa dị ike, nke a na-emepụta na ahụ, nke na-agbanwe mmetụta nke Allopregnanolone (ALLO). ALLO bụ neurosteroid siri ike nke metụtara nrụgide- na ọnọdụ mmanye sitere na Tourette ruo OCD, PTSD, ịgba chaa chaa ike, ị addictionụ ọgwụ ọjọọ, PMDD, Migraine nke oge.

 

Usoro Allopregnanolone nke Action

Mmekọrịta Molekụl

Allopregnanolone bụ ọrịa na-egbochi ime ime neurosteroid. Emere ya site na progesterone, ọ bụkwa ezigbo moderic modulator nke ọrụ γ-aminobutyric acid (GABA) na GABAA ihe nnabata. Allopregnanolone nwere mmetụta yiri nke ndị ọzọ na-arụ ọrụ alloba dị mma nke GABA na onye na-anabata GABAA dị ka benzodiazepines, gụnyere nchegbu, ọgwụ mgbochi, na ọrụ mgbochi. Endogenously mepụtara allopregnanolone na-arụ ọrụ neurophysiological site na nhazi nke onye na-anabata GABAA ma na-agbanwe usoro nke ọtụtụ modulators dị mma na agonists na GABAA receptor.

Allopregnanolone na-arụ ọrụ dị ka onye nwere ezigbo ike nke allosteric modulator nke nnabata GABAA. Ọ bụ ezie na allopregnanolone, dị ka ndị ọzọ na-egbochi neurosteroids dị ka THDOC, na-agbanwe mgbanwe niile nke GABAA isoforms, ọdịdị ndị ahụ nwere δ subunits na-egosipụta ike kachasị. A chọpụtakwara Allopregnanolone ka ọ rụọ ọrụ dị ka modulator dị mma nke onye na-anabata GABAA-,, ọ bụ ezie na ihe omume a edoghị. Na mgbakwunye na omume ya na ndị nabatara GABA, allopregnanolone, dị ka progesterone, maara na ọ bụ modulator allosteric na-adịghị mma nke ndị natara nACh, ọ na - egosikwa na ọ na - arụ ọrụ dịka modulator na - adịghị mma nke ihe nnabata 5-HT3. Tinyere neurosteroid ndị ọzọ na-emechi emechi, allopregnanolone na-egosi na ọ nwere ntakịrị ma ọ bụ enweghị ihe ọ bụla na ọwa ndị ọzọ nwere njikọ, gụnyere NMDA, AMPA, kainate, na glycine receptors.

 

Mmetụta antidepressant

A naghị amata usoro PAM dị ka brexanolone nke neurosteroid na-emetụta antidepressant mmetụta. A naghị eche PAM ndị ọzọ na-anata GABAA, dị ka benzodiazepines, dị ka antidepressants ma enweghị nrụpụta egosiri, n'agbanyeghị ndị dọkịta na-akọwa Alprazolam maka ịda mbà n'obi n'oge gara aga. Neurosteroid GABAA onye na-anabata PAMs maara ka ya na ndị GABAA nabatara na ndị bi na ya iche karịa benzodiazepines. Dịka ọmụmaatụ, onye na-anabata GABAA-na-eme ka neurosteroids nwere ike nwee ike ịchọrọ δ subunit nwere ndị nabatara GABAA, ma wulite ma mgbochi tonic na phasic nke ndị na-anabata GABAA. O nwekwara ike ịbụ na neurosteroids dị ka allopregnanolone nwere ike ime ihe ndị ọzọ, gụnyere membrane progesterone receptors, T-type voltage-gated calcium channels, na ndị ọzọ, iji gbasaa nsogbu antidepressant.

 

Ngwa Allopregnanolone

Allopregnanolone bụ ihe na-emepụta steroid nke na-arụ ọrụ na ụbụrụ. Dị ka ọgwụ, a na-ere ya n'okpuru aha Zulresso ma jiri ya na-emeso ịda mbà n'obi. A na-eji ya ogwu ogwu n’ime akwara karịa oge awa 60 n’okpuru nlekọta ahụike.

Mmetụta ndị ọzọ nke Allopregnanolone nwere ike ịgụnye nkwụsị, ụra, ọnụ akọrọ, ọkụ ọkụ, na enweghị uche. Ọ bụ neurosteroid ma na-eme dị ka ezigbo allosteric modulator nke onye na-anabata GABAA, bụ isi ihe dị ndụ nke na-egbochi neurotransmitter γ-aminobutyric acid (GABA).

A kwadoro Allopregnanolone maka ọgwụgwọ na United States na 2019. Nchịkwa nri na ọgwụ ọjọọ US (FDA) na-ele ya anya dị ka ọgwụ mbụ na klas. Ogologo oge nlekọta, yana ụgwọ maka ọgwụgwọ otu oge, ebutela nchegbu banyere nnweta ọtụtụ ụmụ nwanyị.

 

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 nyocha nke allopregnanolone, epiallopregnanolone, pregnanolone, dehydroepiandrosterone na dehydroepiandrosterone 3-sulfate na plasma mmadụ. Nyocha bioanalysis. 2017 Mar; 9 (6): 527-539. ma ọ bụ: 10.4155 / bio-2016-0262. PubMed PMID: 28207286.

[2] Horishita T, Yanagihara N, Ueno S, Sudo Y, Uezono Y, Okura D, Minami T, Kawasaki T, Sata T. Neurosteroids allopregnanolone sulfate na pregnanolone sulfate nwere mmetụta dị iche iche na mpaghara of nke neuronal voltage-gated sodium ọwa Nav1.2, Nav1.6, Nav1.7, na Nav1.8 kwupụtara na xenopus oocytes. Anesthesiology. 2014 Sep; 121 (3): 620-31. ma ọ bụ: 10.1097 / ALN.0000000000000296. PubMed PMID: 24809977.

[3] Zorumski CF, Paul SM, Covey DF, Mennerick S (Nọvemba 2019). "Neurosteroids dị ka akwụkwọ akụkọ antidepressants na anxiolytics: GABA-A ndị nabatara na gafere". Neurobiology nke Nchegbu. 11: 100196. doi: 10.1016 / j.ynstr.2019.100196. PMC 6804800. PMID 31649968.

[4] Onyekacha, MD; Peabody, CA; Whiteford, HA; Hollister, LE (Eprel 1988). "Alprazolam dị ka antidepressant". Akwụkwọ akụkọ Clinical Psychiatry. 49 (4): 148–150. ISSN 0160-6689. PMID 3281931.

[5] Srisurapanont, M .; Boonyanaruthee, V. (1997). Alprazolam na ọkọlọtọ antidepressants na ọgwụgwọ nke ịda mbà n'obi: meta-analysis nke mmetụta antidepressant. Forlọ Ọrụ Maka Nyocha na Mkesa (UK). PMID 9175386.

[6] Reddy DS (2010). Neurosteroids: ọrụ dị egwu na ụbụrụ mmadụ na ikike ịgwọ ọrịa. Prog. Inbụrụ Brain. Ọganihu na Brain Research. 186. peeji nke 113–37. ma ọ bụ: 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. (June 1997). "Neurosteroids na-agbanwe ọrụ nnabata nicotinic na mouse striatal na thalamic synaptosomes". Akwụkwọ nke Neurochemistry. 68 (6): 2412–23. ma ọ bụ: 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 na pregnanolone analogues gbanwere na C ring: njikọ na ọrụ. J Med Chem. 2013 Marụ 28; 56 (6): 2323-36. ma ọ bụ: 10.1021 / jm3016365. PubMed PMID: 23421641.