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Allopregnanolone

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ʻO Allopregnanolone, i kapa ʻia ʻo Sepranolone a me Isopregnanolone, he mea loaʻa i ka GABA modulate steroid antagonist a me 11-betahydroxysteroid dehydrogenase ʻano 1 (11β-HSD1)…

Product Description

Nā ʻano kikoʻī

Product Name Allopregnanolone
Kāleka CAS 516-55-2
Ka Lā Molecular C21H34O2
Kaumaha Kaumaha 318.5
'O 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-one
Keʻano ʻO ka pauma
Ka mālama a me ka lima lima Maloʻo, ʻeleʻele a ma 0 - 4 C no ka wā pōkole (mau lā a i mau pule) a i ʻole -20 C no ka wā lōʻihi (mau mahina i mau makahiki).

 

Hōʻike Allopregnanolone

ʻO Allopregnanolone, ʻike ʻia ʻo Sepranolone a me Isopregnanolone, kahi mea loaʻa GABA modulate steroid antagonist a me 11-betahydroxysteroid dehydrogenase ʻano 1 (11β-HSD1). ʻO Sepranolone kahi hui neurological ikaika, hana maoli ʻia i loko o ke kino, e hoʻololi i nā hopena o Allopregnanolone (ALLO). ʻO ALLO kahi neurosteroid ikaika i hoʻopili ʻia i nā kūlana pili i ke koʻikoʻi a me nā koi e kū ana mai Tourette a i OCD, PTSD, piliwaiwai koi, hoʻopilikia, PMDD, Menstrual Migraine.

 

ʻO Allopregnanolone Hana Hana

Nā laʻana Molecular

ʻO Allopregnanolone kahi neurosteroid hāpai hānai endogenous. Hana ʻia ia mai ka progesterone, a he modulator allosteric maikaʻi o ka hana o ka acid-aminobutyric acid (GABA) ma ka GABAA receptor. Loaʻa nā hopena e like me ka Allopregnanolone like me nā modulate allosteric maikaʻi ʻē aʻe o ka hana GABA ma ka receptor GABAA e like me nā benzodiazepines, e komo pū ana me ka trigiolytic, sedative, a me ka anticonvulsant. Hana ʻia ʻo endogenous allopregnanolone i kahi kuleana neurophysiological e ka hoʻopiʻi maikaʻi ʻana o ka receptor GABAA a me ka hoʻololi ʻana i ka hana o nā mododer allosteric maikaʻi a me nā agonists ma GABAA receptor.

Hana ʻo Allopregnanolone ma ke ʻano he modulator allosteric maikaʻi maikaʻi loa o ka mea loaʻa ʻo GABAA. ʻOiai ʻo allopregnanolone, e like me nā neurosteroids kaohi like e like me THDOC, hoʻololi pono i nā isoforms receptor GABAA, ʻo kēlā mau isoform i loaʻa nā un subunits e hōʻike ana i ka potentiation ʻoi loa. Ua loaʻa pū ʻo Allopregnanolone e hana ma ke ʻano he allosteric modulator maikaʻi o ka GABAA-ρ receptor, ʻoiai ʻaʻole maopopo ka hopena o kēia hana. Ma waho aʻe o kāna mau hana ma nā GABA receptor, allopregnanolone, e like me progesterone, ʻike ʻia he modulator allosteric maikaʻi ʻole o nā nach receptor, a ʻike ʻia hoʻi e hana ma ke ʻano he modulator allosteric maikaʻi ʻole o ka mea loaʻa 5-HT3. Me nā neurosteroids inhibitory ʻē aʻe, ʻaʻohe a hana iki paha o allopregnanolone ma nā kahawai ion ligand-gated ʻē aʻe, e like me ka NMDA, AMPA, kainate, a me nā glycine receptor.

 

Nā hopena antidepressant

ʻO ke ʻano e ʻike ʻole ʻia ai nā hopena o ka neurosteroid GABAA PAM e like me brexanolone. ʻO nā PAM receptor GABAA ʻē aʻe, e like me benzodiazepines, ʻaʻole i manaʻo ʻia he antidepressants a ʻaʻohe hopena i hōʻike ʻia, ʻoiai nā kauka e kuhikuhi ana iā Alprazolam no ke kaumaha i ka wā i hala. ʻIke ʻia nā PAM receptor Neurosteroid GABAA e launa pū me nā GABAA receptor a me nā sub-populasyon ʻokoʻa ma mua o benzodiazepines. Ma ke ʻano he laʻana, GABAA receptor-potentiating neurosteroids hiki i ka pahuhopu nui δ subunit-i loaʻa nā GABAA receptor, a hoʻonui i ka tonic a me ka phasic inhibition i hoʻopili ʻia e nā mea loaʻa ʻo GABAA. Hiki nō paha i nā neurosteroids e like me allopregnanolone ke hana i nā pahuhopu ʻē aʻe, e like me nā mea loaʻa nā progesterone membrane, nā ʻano kalipuna G-type voltage, a me nā mea ʻē aʻe, e hoʻoponopono i nā hopena antidepressant.

 

Noi Allopregnanolone

ʻO Allopregnanolone kahi steroid i hana maoli ʻia e hana ma ka lolo. Ma ke ʻano he lāʻau lapaʻau, kūʻai ʻia aku ia ma lalo o ka inoa Zulresso a hoʻohana ʻia e mālama i ke kaumaha postpartum. Hoʻohana ʻia ia e ka pahu ʻana i loko o kahi aa i loko o kahi manawa he 60 mau hola ma lalo o ka nānā lāʻau.

Hiki i nā hopena o Allopregnanolone ke hoʻopili i ka sedation, ka hiamoe, ka waha maloʻo, nā uila wela, a me ka nalo o ka ʻike. He neurosteroid ia a hana ma ke ʻano he allosteric modulator maikaʻi o ka GABAA receptor, ke kumu pahuhopu nui o ka mea hoʻopiha neurotransmitter γ-aminobutyric acid (GABA).

Ua ʻae ʻia ʻo Allopregnanolone no ka hoʻohana lapaʻau ma United States i ka makahiki 2019. Ua manaʻo ka US Food and Drug Administration (FDA) he lāʻau lapaʻau mua ia ma ka papa. ʻO ka manawa hoʻomalu lōʻihi, a me ke kumukūʻai no ka hana hoʻokahi manawa, ua hāpai i nā hopohopo e pili ana i ke kiʻi no nā wahine he nui.

 

Reference

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[2] ʻO Horishita T, Yanagihara N, Ueno S, Sudo Y, Uezono Y, Okura D, Minami T, Kawasaki T, Sata T. Neurosteroids allopregnanolone sulfate a me ka pregnanolone sulfate i nā hopena like ʻole ma ka sub α o ka sodium nā kahawai Nav1.2, Nav1.6, Nav1.7, a me Nav1.8 i hōʻike ʻia i nā xenopus oocytes. Anesthesiology. 2014 Sep; 121 (3): 620-31. hana: 10.1097 / ALN.0000000000000296. ʻO PubMed PMID: 24809977.

[3] Zorumski CF, Paul SM, Covey DF, Mennerick S (Nowemapa 2019). "Nā Neurosteroids e like me nā antidepressants novel a me nā kūpikipikiʻi: nā mea loaʻa ʻo GABA-A a ʻoi aku". Neurobiology o ke koʻikoʻi. 11: 100196. doi: 10.1016 / j.ynstr.2019.100196. PMC 6804800. PMID 31649968.

[4] Warner, MD; Peabody, CA; Whiteford, HA; Hollister, LE (ʻApelila 1988). "Alprazolam ma ke ʻano he antidepressant". ʻO ka Ka Nūpepa o ka Psychiatry Clinical. 49 (4): 148-150. ISSN 0160-6689. PMID 3281931.

[5] Srisurapanont, M .; Boonyanaruthee, V. (1997). Alprazolam a me nā antidepressants maʻamau i ka mālama ʻana i ke kaumaha: kahi meta-analysis o ka hopena antidepressant. Ke kikowaena no nā loiloi a me ka hoʻolaha ʻana (UK). PMID 9175386.

[6] Reddy DS (2010). Neurosteroids: hopena endogenous i ka lolo o ke kanaka a me nā pono therapeutic. Prog. ʻO Brain Res. Ka holomua i ka noiʻi ʻana i ka lolo 186. pp. 113–37. hana: 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. (Iune 1997). "Hoʻololi nā Neurosteroids i ka hana o nā receptor nikotinic i ka striatal striatal a me thalamic synaptosomes". Pai no Neurochemistry. 68 (6): 2412–23. hana: 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 a me nā ʻano like ʻole me ka fennanolone i hoʻololi ʻia i ke apo C: synthesi a me ka hana. ʻO J Med Chem. 2013 Mar 28; 56 (6): 2323-36. hana: 10.1021 / jm3016365. ʻO PubMed PMID: 23421641.


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