AASraw imapanga ufa wa Cannabidiol (CBD) ndi Hemp Mafuta Ofunika ambiri!

Kuthamanga

mlingo: Category:

Allopregnanolone, yotchedwanso Sepranolone ndi Isopregnanolone, ndi GABA receptor modulating steroid antagonist ndi 11-betahydroxysteroid dehydrogenase type 1 (11β-HSD1)…

Mafotokozedwe Akatundu

Makhalidwe Abwino

Name mankhwala Kuthamanga
Nambala ya CAS 516-55-2
Molecular Formula C21H34O2
Kulemera kwa Fomu 318.5
Mafananidwe Maganizo a NSC-97078; U-0949; UC-1010; NSC97078; U0949; UC1010; NSC 97078; U 0949; UC 1010; Chizolowezi; Zolemba zonse; Zamgululi 516-55-2; 5alpha-Pregnan-3beta-ol-20-m'modzi
Maonekedwe White powder
Kusungirako ndi Kusamalira Youma, mdima ndi 0 - 4 C kwakanthawi kochepa (masiku mpaka masabata) kapena -20 C kwakanthawi (miyezi mpaka zaka).

 

Kufotokozera kwa Allopregnanolone

Allopregnanolone, yotchedwanso Sepranolone ndi Isopregnanolone, ndi GABA receptor modulating steroid antagonist ndi 11-betahydroxysteroid dehydrogenase mtundu 1 (11β-HSD1). Sepranolone ndi njira yamagetsi yamphamvu, yopangidwa mwachilengedwe mthupi, yomwe imathandizira zotsatira za Allopregnanolone (ALLO). ALLO ndi neurosteroid wamphamvu yemwe amakhala ndi nkhawa komanso kukakamizidwa kuyambira ku Tourette kupita ku OCD, PTSD, kutchova juga, chizolowezi, PMDD, Menstrual Migraine.

 

Njira Yopangira Allopregnanolone

Kuyanjana kwa maselo

Allopregnanolone ndi njira yoletsa kupewera mimba yoteteza mimba. Amapangidwa kuchokera ku progesterone, ndipo ndimayendedwe abwino γ-aminobutyric acid (GABA) ku GABAA receptor. Allopregnanolone ili ndi zovuta zofananira ndi zomwe zimapangitsa ena ku GABAA receptor monga benzodiazepines, kuphatikiza nkhawa, kusungunula, komanso ntchito za anticonvulsant. Allopregnanolone yomwe imapanga mosalekeza imakhala ndi gawo la ma neurophysiological poyendetsa bwino GABAA receptor ndikusinthira zochita zama modulators angapo ndi ma agonists ku GABAA receptor.

Allopregnanolone imagwiritsa ntchito njira yabwino kwambiri yolandirira GABAA receptor. Ngakhale allopregnanolone, monga ma neurosteroid ena oletsa monga THDOC, imayendetsa bwino ma GABAA receptor isoforms, ma isoform omwe ali ndi ma subunits amawonetsa kuthekera kwakukulu. Allopregnanolone yapezekanso ngati njira yoyeserera ya GABAA-ρ receptor, ngakhale tanthauzo la izi silikudziwika. Kuphatikiza pa zomwe amachita pa ma GABA receptors, allopregnanolone, monga progesterone, imadziwika kuti ndi yoyeserera yoyeserera ya NACh receptors, komanso imawoneka ngati yoyendetsa molakwika ya 5-HT3 receptor. Pamodzi ndi ma neurosteroids ena oletsa, allopregnanolone imawoneka kuti singachitepo kanthu pena paliponse pazitsulo zina za ion, kuphatikiza ma NMDA, AMPA, kainate, ndi glycine receptors.

 

Zotsatira za antidepressant

Makina omwe ma GAMA receptor PAM amtundu wa neurosteroid monga brexanolone amakhala ndi zothetsa nkhawa sakudziwika. Ma PAM ena a GABAA receptor PAM, monga benzodiazepines, samaganiziridwa ngati oponderezana ndipo alibe chitsimikiziro chothandiza, ngakhale adotolo adalamula Alprazolam kukhumudwa m'mbuyomu. Neurosteroid GABAA receptor PAMs amadziwika kuti amalumikizana ndi ma GABAA receptors ndi anthu ochepa mosiyana ndi benzodiazepines. Monga zitsanzo, GABAA receptor-potentiating neurosteroids itha kukhala yosakira anthu okhala ndi GABAA zolandilira, ndikuwonjezera zoletsa zama tonic ndi phasic zomwe zimayanjanitsidwa ndi ma GABAA receptors. Ndikothekanso kuti ma neurosteroids monga allopregnanolone atha kuchita zina, kuphatikiza nembanemba progesterone receptors, T-mtundu wamagetsi-gated calcium njira, ndi ena, kuti athetse zovuta zowononga.

 

Ntchito ya Allopregnanolone

Allopregnanolone ndi steroid yopangidwa mwachilengedwe yomwe imagwira ubongo. Monga mankhwala, amagulitsidwa pansi pa dzina la Zulresso ndipo amagwiritsidwa ntchito pochiza kukhumudwa pambuyo pobereka. Amagwiritsidwa ntchito ndi jakisoni mumtsempha kwa nthawi yopitilira maola 60 moyang'aniridwa ndi azachipatala.

Zotsatira zoyipa za Allopregnanolone zitha kuphatikizira kukhazikika, kugona tulo, pakamwa pouma, kunyezimira komanso kutaya chidziwitso. Ndi neurosteroid ndipo imagwira bwino ntchito yoyeserera ya GABAA receptor, chandamale chachikulu cha choletsa ma neurotransmitter γ-aminobutyric acid (GABA).

Allopregnanolone idavomerezedwa kuti akagwiritse ntchito zamankhwala ku United States ku 2019. US Food and Drug Administration (FDA) imawona kuti ndi mankhwala oyamba. Nthawi yayitali yoyang'anira, komanso mtengo wothandizira kamodzi, zadzetsa nkhawa zakupezeka kwa azimayi ambiri.

 

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 kusanthula munthawi yomweyo kwa allopregnanolone, epiallopregnanolone, pregnanolone, dehydroepiandrosterone ndi dehydroepiandrosterone 3-sulphate m'madzi am'magazi. Kusanthula Kwachilengedwe. 2017 Mar; 9 (6): 527-539. (Adasankhidwa) onetsani: 10.4155 / bio-2016-0262. Adatuluka PMID: 28207286.

[2] Horishita T, Yanagihara N, Ueno S, Sudo Y, Uezono Y, Okura D, Minami T, Kawasaki T, Sata T. Neurosteroids allopregnanolone sulphate ndi pregnanolone sulphate ali ndi mphamvu zosiyanasiyana pa α subunit ya neuronal voltage-gated sodium njira Nav1.2, Nav1.6, Nav1.7, ndi Nav1.8 zofotokozedwa m'matope a xenopus. Anesthesiology. 2014 Sep; 121 (3): 620-31. onetsani: 10.1097 / ALN.0000000000000296. Adatuluka PMID: 24809977.

[3] Zorumski CF, Paul SM, Covey DF, Mennerick S (Novembala 2019). "Neurosteroids ngati buku la antidepressants and anxiolytics: GABA-A receptors ndi kupitirira". Neurobiology ya Kupsinjika. 11: 100196. onetsani: 10.1016 / j.ynstr.2019.100196. MAFUNSO: PMC 6804800. PMID 31649968.

[4] Warner, MD; Peabody, CA; Whiteford, HA; Hollister, LE (Epulo 1988). "Alprazolam ngati woponderezedwa". Journal of Clinical Psychiatry. 49 (4): 148-150. Kufotokozera: ISSN 0160-6689. PMID 3281931. (Adasankhidwa)

[5] Srisurapanont, M .; Boonyanaruthee, V. (1997). Alprazolam ndi antidepressants wamba pochiza kukhumudwa: meta-kusanthula zakuthana ndi nkhawa. Pulogalamu Yowunika ndi Kufalitsa (UK). PMID 9175386. (Adasankhidwa)

[6] Reddy DS (2010). Neurosteroids: gawo lamkati muubongo wamunthu komanso kuthekera kochizira. Prog. Resin Ubongo. Kupita Patsogolo Pakafukufuku wa Ubongo. 186. mas. 113-37. onetsani: 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, Maliko MJ, et al. (June 1997). "Neurosteroids amayesa nicotinic receptor ntchito mu mbewa striatal ndi thalamic synaptosomes". Zolemba za Neurochemistry. 68 (6): 2412-23. onetsani: 10.1046 / j.1471-4159.1997.68062412.x. PMID 9166735. (Adasankhidwa)

[8] Slavíková B, Bujons J, Matyáš L, Vidal M, Babot Z, Krištofíková Z, Suñol C, Kasal A. Allopregnanolone ndi mafanizidwe a pregnanolone osinthidwa mu mphete ya C: kaphatikizidwe ndi ntchito. J Med Chem. 2013 Mar 28; 56 (6): 2323-36. onetsani: 10.1021 / jm3016365. Adatuluka PMID: 23421641.