I-Allopregnanolone (516-55-2) ipowder-Umthengisi weFektri yoMvelisi
I-AASraw ivelisa i-Cannabidiol (CBD) ipowder kunye ne-Hemp ebalulekileyo yeoyile ngobuninzi!

Zonke iinkonzo ze-intanethi

Akukho kalo Udidi:

I-Allopregnanolone, ekwabizwa ngokuba yi-Sepranolone kunye ne-Isopregnanolone, yi-GABA receptor modulating steroid antagonist kunye ne-11-betahydroxysteroid dehydrogenase yohlobo 1 (11β-HSD1)…

Ingcaciso yeMveliso

Iimpawu ezisisiseko

Igama lemveliso Zonke iinkonzo ze-intanethi
Inani leCAS 516-55-2
I-Molecular Formula C21H34O2
Ubukhulu beFormula 318.5
Iintetho ezifanayo I-NSC-97078; U-0949; UC-1010; I-NSC97078; U0949; UC1010; I-NSC 97078; U-0949; UC 1010; Isopregnanolone; Zonke iinkonzo ze-intanethi. Isepranolone; 516-55-2; 5alpha-Pregnan-3beta-ol-20-nye
Kubonakala Powder
Ukugcina nokuPhatha Okomileyo, omnyama kunye no-0 ukuya ku-4 C okwexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (iinyanga ukuya kwiminyaka).

 

Inkcazo yeAllopregnanolone

I-Allopregnanolone, ekwabizwa ngokuba yi-Sepranolone kunye ne-Isopregnanolone, yi-GABA receptor modulating steroid antagonist kunye ne-11-betahydroxysteroid dehydrogenase yohlobo 1 (11β-HSD1). ISepranolone sisixhobo esinamandla se-neurological, esiveliswa ngokwendalo emzimbeni, esimodareyitha iziphumo ze-Allopregnanolone (ALLO). I-ALLO yinyani ye-neurosteroid enefuthe kuxinzelelo- kunye neemeko ezinxulumene nokunyanzelwa ukusukela eTourette ukuya kwi-OCD, i-PTSD, ukungcakaza okunyanzelekileyo, umlutha, i-PMDD, iMigraine yokuya exesheni.

 

Indlela yokusebenza yeAllopregnanolone

Ukudibana kweMolekyuli

I-Allopregnanolone yinto engapheliyo yokukhulelwa kwe-neuraneoidid. Yenziwe ngeprogesterone, kwaye iyimodareyitha elungileyo ye-all-aminobutyric acid (GABA) kwi-GABAA receptor. I-Allopregnanolone ineziphumo ezifanayo nezinye zezinto ezintle ezenziwayo ze-modulators yesenzo se-GABA kwi-GABAA receptor efana ne-benzodiazepines, kubandakanya i-anxiolytic, sedative, kunye ne-anticonvulsant. Iveliswe ngokungagungqiyo i-allopregnanolone inendima ye-neurophysiological ngokulungiswa kakuhle kwe-GABAA receptor kunye nokumodareyitha isenzo seemodulators kunye ne-agonists ezilungileyo kwi-GABAA receptor.

I-Allopregnanolone isebenza njengemodyuli elungileyo ye-allosteric ye-GABAA receptor. Ngelixa i-allopregnanolone, njengezinye izithintelo ze-neurosteroids ezinje nge-THDOC, ngokuqinisekileyo imodareyitha zonke i-GABAA receptor isoforms, ezo isoforms ziqukethe ii-subunits zibonisa eyona nto inokubakho. I-Allopregnanolone ikwafumaneke isebenza njengemodyuli ye-allosteric efanelekileyo ye-GABAA-of receptor, nangona iziphumo zale nyathelo zingacacanga. Ukongeza kwizenzo zayo kwii-GABA receptors, i-allopregnanolone, njenge-progesterone, yaziwa ngokuba yi-allosteric modulator ye-nACh receptors, kwaye ikwasebenza njenge-allosteric modulator ye-5-HT3 receptor. Ngokubambisana nezinye i-neurosteroids ezingavimbeliyo, i-allopregnanolone ibonakala ingenamsebenzi okanye ingenantshukumo kwezinye iindlela ze-ion ze-ligand, kubandakanya i-NMDA, i-AMPA, i-kainate, kunye ne-glycine receptors.

 

Iziphumo zoxinzelelo

Indlela i-neurosteroid ye-GABAA receptor PAMs efana ne-brexanolone eneziphumo zokulwa noxinzelelo ayaziwa. Ezinye ii-PAMs receptor PAMs, ezinje nge-benzodiazepines, azicingelwa njenge-anti-depressants kwaye azinabungqina bokusebenza, ngaphandle kweeklinikhi ezimisela i-Alprazolam yoxinzelelo ngaphambili. I-Neurosteroid GABAA receptor PAMs ziyaziwa ukuba zinxibelelana nee-GABAA receptors kunye nabantu abaphantsi ngokwahlukileyo kune-benzodiazepines. Njengemizekelo, i-GABAA receptor-potentiating neurosteroids inokukhetha ngokukhethekileyo i-subunit equkethe i-GABAA receptors, kwaye yonyuse zombini i-tonic kunye ne-phasic inhibition edityaniswe zii-GABAA receptors. Kuyenzeka ukuba ii-neurosteroids ezinjenge-allopregnanolone zinokuthi zisebenze kwezinye iithagethi, kubandakanya i-membrane progesterone receptors, T-uhlobo lwevolthi-gated calcium channels, kunye nezinye, ukulamla iziphumo zoxinzelelo.

 

Isicelo seAllopregnanolone

I-Allopregnanolone yi-steroid eveliswa ngokwendalo esebenza kwingqondo. Njengeyeza, ithengiswa phantsi kwegama lophawu lweZulresso kwaye isetyenziselwa ukunyanga uxinzelelo lwasemva kokubeleka. Isetyenziswa ngenaliti emthanjeni kwisithuba seeyure ezingama-60 phantsi kolawulo lwezonyango.

Iziphumo ebezingalindelekanga ze-Allopregnanolone zinokubandakanya ukulala, ukulala, umlomo owomileyo, ukukhanya okutshisayo kunye nokulahleka kwengqondo. I-neurosteroid kwaye isebenza njengemodyuli elungileyo ye-allosteric ye-GABAA receptor, eyona nto iphambili ekujoliseni ibhayoloji ye-inhibitory neurotransmitter γ-aminobutyric acid (GABA).

I-Allopregnanolone yavunywa ukuba isetyenziswe kwezonyango e-United States ngo-2019. I-US Food and Drug Administration (i-FDA) iyithatha njengeyeza ekumgangatho wokuqala. Ixesha elide lolawulo, kunye neendleko zonyango lwexesha elinye, ziye zaphakamisa inkxalabo malunga nokufikeleleka kwabafazi abaninzi.

 

isingqiniso

[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 uhlalutyo ngaxeshanye lwe allopregnanolone, i-epiallopregnanolone, i-pregnanolone, i-dehydroepiandrosterone kunye ne-dehydroepiandrosterone 3-sulphate kwiplasma yabantu. Uhlalutyo lweBioanalysis. Ngo-2017 Mar; 9 (6): 527-539. ikhonkco: 10.4155 / bio-2016-0262. Ipapashwe kwi-PMID: 28207286.

[2] Horishita T, Yanagihara N, Ueno S, Sudo Y, Uezono Y, Okura D, Minami T, Kawasaki T, Sata T. amajelo Nav1.2, Nav1.6, Nav1.7, kunye Nav1.8 abonakaliswe kwi-xenopus oocytes. Ukubulala iintlungu. Ngo-2014 Sep; 121 (3): 620-31. ikhonkco: 10.1097 / ALN.0000000000000296. Ipapashwe kwi-PMID: 24809977.

[3] Zorumski CF, Paul SM, Covey DF, Mennerick S (Novemba 2019). "I-Neurosteroids njenge-antidepressants yenoveli kunye ne-anxiolytics: I-GABA-A receptors nangaphaya". I-Neurobiology yoxinzelelo. 11: 100196. ikhonkco: 10.1016 / j.ynstr.2019.100196. IINKCUKACHA: PMC 6804800.

[4] Isilumkiso, MD; I-Peabody, CA; IWhiteford, HA; Hollister, LE (Epreli 1988). "I-Alprazolam njenge-antidepressant". Ijenali yoNyango lwezeMpilo. 49 (4): 148-150. ISSN 0160-6689. IINKCUKACHA:

[5] ISrisurapanont, M.; I-Boonyanaruthee, V. (1997). I-Alprazolam kunye ne-anti-depressants esemgangathweni kunyango loxinzelelo: uhlalutyo lweemeta zempembelelo yoxinzelelo. Iziko loPhononongo kunye nokuSasazwa (UK). IINKCUKACHA:

[6] I-Reddy DS (2010). Neurosteroids: Indima engapheliyo kwingqondo yomntu kunye namandla okunyanga. Inkqubela. Indawo yeBrain. Inkqubela phambili kuPhando lweBongo. 186. Iphepha 113-37. ikhonkco: 10.1016 / B978-0-444-53630-3.00008-7. I-ISBN 9780444536303. PMC 3139029. PMID 21094889.

[7] I-Bullock AE, Clark AL, Grady SR, Robinson SF, Slobe BS, Amanqaku MJ, et al. (NgoJuni 1997). "I-Neurosteroids modulate nicotinic receptor function in mouse striatal and thalamic synaptosomes". Ijenali yeNeurochemistry. 68 (6): 2412-23. ikhonkco: 10.1046 / j.1471-4159.1997.68062412.x. IINKCUKACHA:

[8] Slavíková B, Bujons J, Matyáš L, Vidal M, Babot Z, Krištofíková Z, Suñol C, Kasal A. Allopregnanolone kunye neepreganolone analogue eziguqulwe kwindandatho ye-C: synthesis kunye nomsebenzi. UJ Med Chem. Ngo-2013 ngoMatshi 28; 56 (6): 2323-36. ikhonkco: 10.1021 / jm3016365. I-PMID epapashiweyo: 23421641.