I-Allopregnanolone (516-55-2) powder - Umhlinzeki Wefektri Yomkhiqizi
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I-Allopregnanolone

Isilinganiselwa: Isigaba:

I-Allopregnanolone, eyaziwa nangokuthi i-Sepranolone ne-Isopregnanolone, i-GABA receptor modulating steroid antagonist kanye no-11-betahydroxysteroid dehydrogenase type 1 (11β-HSD1)…

Product Incazelo

Izici Eziyisisekelo

Igama Product I-Allopregnanolone
CAS Inombolo 516-55-2
Formula Yamamolekhula C21H34O2
Isisindo sesisindo 318.5
omqondofana I-NSC-97078; U-0949; UC-1010; I-NSC97078; U0949; UC1010; I-NSC 97078; U-0949; UC 1010; Isopregnanolone; I-Allopregnanolon; I-Sepranolone; 516-55-2; I-5alpha-Pregnan-3beta-ol-20-eyodwa
ukubukeka powder emhlophe
Isitoreji nokuphatha Okomile, okumnyama naku-0 - 4 C isikhathi esifushane (izinsuku kuya emavikini) noma -20 C isikhathi eside (izinyanga kuya eminyakeni).

 

Incazelo ye-Allopregnanolone

I-Allopregnanolone, eyaziwa nangokuthi i-Sepranolone ne-Isopregnanolone, iyi-GABA receptor modulating steroid antagonist kanye no-11-betahydroxysteroid dehydrogenase type 1 (11β-HSD1). ISepranolone iyinhlanganisela enamandla yezinzwa, ekhiqizwa ngokwemvelo emzimbeni, eguqula imiphumela ye-Allopregnanolone (ALLO). I-ALLO iyi-neurosteroid enamandla ethintekayo ezimweni ezihlobene nengcindezi neziphoqelela kusuka kuTourette kuya ku-OCD, i-PTSD, ukugembula okuphoqelela, ukuluthwa, i-PMDD, i-Menstrual Migraine.

 

I-Allopregnanolone Mechanism of Action

Ukusebenzisana kwamangqamuzana

I-Allopregnanolone iyi-endo native inhibitory pregnancy i-neurosteroid. Yenziwe nge-progesterone, futhi iyimoduli enhle ye-allosteric yesenzo se-γ-aminobutyric acid (GABA) e-GABAA receptor. I-Allopregnanolone inemiphumela efana naleyo yeminye imodulators emihle yesenzo se-GABA e-GABAA receptor efana ne-benzodiazepines, kufaka phakathi i-anxiolytic, sedative, ne-anticonvulsant activity. I-allopregnanolone ekhiqizwe ngokungaguquki inendima ye-neurophysiological ngokulungisa kahle i-GABAA receptor kanye nokuguqula isenzo sabaningi bama-modulators nama-agonists amahle e-GABAA receptor.

I-Allopregnanolone isebenza njengemoduli ye-allosteric enamandla kakhulu ye-GABAA receptor. Ngenkathi i-allopregnanolone, njengamanye ama-neurosteroids avimbelayo afana ne-THDOC, enza kahle wonke ama-GABAA receptor isoforms, lawo ma-isoforms aqukethe ama-subunits akhombisa amandla amakhulu kakhulu. I-Allopregnanolone nayo itholakale isebenza njengemoduli enhle ye-allosteric ye-GABAA-ρ receptor, yize imiphumela yalesi senzo ingacacile. Ngaphezu kwezenzo zayo kuma-GABA receptors, i-allopregnanolone, njenge-progesterone, yaziwa njenge-moduli engeyiyo ye-allosteric yama-receptors we-nACh, futhi futhi ibonakala isebenza njenge-modulator engeyiyo ye-allosteric ye-5-HT3 receptor. Kanye namanye ama-neurosteroids avimbelayo, i-allopregnanolone ibonakala ingenasenzo esincane noma ingenaso isenzo kwezinye iziteshi ze-ion ezinamagagand, okubandakanya i-NMDA, AMPA, kainate, ne-glycine receptors.

 

Imiphumela ye-antidepressant

Indlela i-neurosteroid GABAA receptor PAMs efana ne-brexanolone enemiphumela yokulwa nokudangala ayaziwa. Amanye ama-PAMs receptor GAMA, afana ne-benzodiazepines, awacatshangwa njenge-anti-depressants futhi awanakho ukusebenza okuqinisekisiwe, yize odokotela bebeka i-Alprazolam ngokudangala esikhathini esedlule. Ama-PAMs we-Neurosteroid GABAA receptor PAMs ayaziwa ngokuxhumana nama-receptors we-GABAA kanye nabantu abangaphansi ngokuhlukile kune-benzodiazepines. Njengezibonelo, ama-neurosteroid we-GABAA receptor-potentiating neurosteroids angahle akhethe ama-receptors aqukethe ama-GABAA, futhi athuthukise ukuvinjelwa kwe-tonic ne-phasic okulamulelwe yi-GABAA receptors. Kungenzeka futhi ukuthi ama-neurosteroid afana ne-allopregnanolone angasebenza kwezinye izinhloso, kufaka phakathi i-membrane progesterone receptors, T-type voltage-gated calcium channels, nezinye, ukulamula imiphumela ye-antidepressant.

 

Isicelo se-Allopregnanolone

I-Allopregnanolone iyi-steroid ekhiqizwa ngokwemvelo esebenza ebuchosheni. Njengomuthi, ithengiswa ngaphansi kwegama lomkhiqizo iZulresso futhi isetshenziselwa ukwelapha ukucindezeleka kwangemva kokubeletha. Isetshenziswa ngomjovo emthanjeni isikhathi esingamahora angama-60 ngaphansi kokuqondisa kwezokwelapha.

Imiphumela emibi ye-Allopregnanolone ingabandakanya ukudambisa, ukulala, umlomo owomile, ukukhanya okushisayo nokulahlekelwa ukwazi. I-neurosteroid futhi isebenza njenge-modulator enhle ye-allosteric ye-GABAA receptor, okuyiyona nto ebhekiswe kakhulu ku-inhibitory neurotransmitter γ-aminobutyric acid (GABA).

I-Allopregnanolone yamukelwa ukuthi isetshenziselwe ukwelashwa e-United States ngo-2019. I-US Food and Drug Administration (i-FDA) ikuthatha njengomuthi wokuqala osezingeni. Isikhathi eside sokuphatha, kanye nezindleko zokwelashwa okukodwa, kuphakamise ukukhathazeka ngokutholakala kwabesifazane abaningi.

 

Izikhombo

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[2] Horishita T, Yanagihara N, Ueno S, Sudo Y, Uezono Y, Okura D, Minami T, Kawasaki T, Sata T. Neurosteroids allopregnanolone sulphate kanye ne-pregnanolone sulphate zinomthelela ohlukahlukene ku-α subunit ye-sodium neuronal voltage-gated iziteshi i-Nav1.2, i-Nav1.6, i-Nav1.7, ne-Nav1.8 evezwe ngama-xenopus oocytes. I-Anesthesiology. 2014 Septhemba; 121 (3): 620-31. i-doi: 10.1097 / ALN.0000000000000296. I-PMID ekhishwe: 24809977.

[3] UZorumski CF, Paul SM, Covey DF, Mennerick S (Novemba 2019). "Ama-Neurosteroids njenge-anti-depressants yenoveli kanye ne-anxiolytics: Ama-GABA-A receptors nangaphezulu". I-Neurobiology Yokucindezeleka. 11: 100196. doi: 10.1016 / j.ynstr.2019.100196. I-PMC 6804800. PMID 31649968.

[4] I-Warner, MD; Peabody, CA; I-Whiteford, HA; Hollister, LE (Ephreli 1988). "I-Alprazolam njenge-anti-depressant". Ijenali yeClinical Psychiatry. 49 (4): 148-150. ISSN 0160-6689. I-PMID 3281931.

[5] ISrisurapanont, M.; I-Boonyanaruthee, V. (1997). I-Alprazolam kanye ne-antidepressants ejwayelekile ekwelapheni ukucindezeleka: ukuhlaziywa kwe-meta komphumela wokulwa nokucindezelwa. Isikhungo Sokubuyekeza Nokusabalalisa (UK). I-PMID 9175386.

[6] I-Reddy DS (2010). Ama-Neurosteroids: indima engapheli ebuchosheni bomuntu nasemandleni okwelapha. Inqubekela phambili. I-Brain Res. Intuthuko ekucwaningweni kobuchopho. 186. amakhasi 113-37. i-doi: 10.1016 / B978-0-444-53630-3.00008-7. I-ISBN 9780444536303. PMC 3139029. PMID 21094889.

[7] IBullock AE, uClark AL, uGrady SR, uRobinson SF, uSlobe BS, uMarks MJ, et al. (Juni 1997). "I-Neurosteroids ilinganisa umsebenzi we-nicotinic receptor kuma-synaptosomes we-mouse striatal and thalamic". Ijenali yeNeurochemistry. 68 (6): 2412-23. i-doi: 10.1046 / j.1471-4159.1997.68062412.x. I-PMID 9166735.

[8] Slavíková B, Bujons J, Matyáš L, Vidal M, Babot Z, Krištofíková Z, Suñol C, Kasal A. Allopregnanolone kanye ne-pregnanolone analogue eziguqulwe kwindandatho ye-C: synthesis kanye nomsebenzi. UJ Med Chem. 2013 uMar 28; 56 (6): 2323-36. i-doi: 10.1021 / jm3016365. I-PMID ekhishwe: 23421641.