Basic Hunhu

Product Name	Allopregnanolone
CAS Number	516-55-2
Molecular Formula	C21H34O2
Formula Weight	318.5
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-imwe
Kuonekwa	White powder
Kuchengeta uye Kubata	Kuoma, kusviba uye pa0 - 4 C kwenguva pfupi (mazuva kusvika kumavhiki) kana -20 C kwenguva refu (mwedzi kusvika makore).

 

Allopregnanolone Tsanangudzo

Allopregnanolone, inozivikanwawo seSepranolone uye Isopregnanolone, inonzi GABA receptor modulating steroid antagonist uye 11-betahydroxysteroid dehydrogenase mhando 1 (11β-HSD1). Sepranolone isimba ine mutsinga, inogadzirwa zvakasikwa mumuviri, iyo inogadzirisa mhedzisiro yeAllopregnanolone (ALLO). ALLO ane simba neurosteroid inosanganisirwa mukushushikana- uye nemamiriro ekumanikidza ane hukama kubva kuTourette kuenda kuOCD, PTSD, kumanikidza kubhejera, kupindwa muropa, PMDD, Menstrual Migraine.

 

Allopregnanolone Maitiro Ekuita

Kubatana kweMoleky

Allopregnanolone inogumira yekudzivirira nhumbu neurosteroid. Yakagadzirwa kubva progesterone, uye inoyevedza allosteric modulator yechiito che γ-aminobutyric acid (GABA) kuGABAA receptor. Allopregnanolone ine mhedzisiro yakafanana neyeye mamwe akanaka allosteric modulators eGABA chiito paGABAA receptor senge benzodiazepines, kusanganisira anxiolytic, sedative, uye anticonvulsant chiitiko. Zvisingagumi zvakaburitswa allopregnanolone ine neurophysiological basa nekunyatso gadzira GABAA receptor uye modulating maitiro eanoverengeka akanaka allosteric modulators uye agonists kuGABAA receptor.

Allopregnanolone inoshanda senge yakasimba kwazvo allosteric modulator yeGABAA receptor. Ipo allopregnanolone, semamwe inhibitory neurosteroids senge THDOC, inonyatsogadzirisa ese eGABAA receptor isoforms, iwo maofofomu ane δ subunits anoratidza kugona kukuru. Allopregnanolone yakawanikwawo ichiita seyakanaka allosteric modulator yeGABAA-ρ receptor, asi zvinorehwa nechiito ichi hazvina kujeka. Pamusoro pezviito zvayo paGABA receptors, allopregnanolone, senge progesterone, inozivikanwa kunge isina kunaka allosteric modulator yeNACh receptors, uye zvakare inoita senge isina kunaka allosteric modulator yeiyo 5-HT3 receptor. Pamwe pamwe nezvimwe zvinodzivirira neurosteroids, allopregnanolone inoita kunge isina zvishoma kana kusaita pane mamwe magandon-gated ion chiteshi, kusanganisira iyo NMDA, AMPA, kainate, uye glycine receptors.

 

Anodzvinyirira mhedzisiro

Iyo mashandiro ayo neurosteroid GABAA receptor PAMs kunge brexanolone ane antidipressant mhedzisiro hazvizivikanwe Mamwe maGABAA receptor PAMs, senge benzodiazepines, haafungidzirwe seanodzvinyirira uye haana hunobudirira, kunyangwe varapi vachirayira Alprazolam yekushungurudzika munguva yakapfuura. Neurosteroid GABAA receptor PAMs inozivikanwa kuti inosangana neGABAA receptors uye sub-populations zvakasiyana pane benzodiazepines. Semuenzaniso, GABAA receptor-potentiating neurosteroids inogona kusarudzika - subunit-ine GABAA receptors, uye kusimudzira zvese tonic uye phasic inhibition inopindirana neGABAA receptors. Izvo zvakare zvinoita kuti neurosteroids senge allopregnanolone inogona kuita pane zvimwe zvinangwa, zvinosanganisira membrane progesterone receptors, T-mhando voltage-gated calcium chiteshi, uye nevamwe, kuyananisa antidepressant mhedzisiro.

 

Allopregnanolone Kunyorera

Allopregnanolone ndeye yakasikwa inogadzirwa steroid inoshanda pauropi. Semushonga, inotengeswa pasi pezita rekuti Zulresso uye inoshandiswa kurapa kusununguka kwekusununguka. Iyo inoshandiswa nejekiseni kupinda mutsinga pamusoro pemaawa makumi matanhatu yenguva pasi pekutarisirwa kwechiremba

Mhedzisiro yeAllopregnanolone inogona kusanganisira sedation, kurara, kuoma muromo, kupisa kupisa, uye kurasikirwa kwekuziva. Iyo neurosteroid uye inoshanda seyakanaka allosteric modulator yeGABAA receptor, iyo hombe yekuzvarwa tarisiro yeanodzivirira neurotransmitter γ-aminobutyric acid (GABA).

Allopregnanolone yakabvumidzwa kushandiswa kwekurapa muUnited States muna 2019. IU.S. Food and Drug Administration (FDA) inoitora semushonga wekutanga-mukirasi. Iyo yakareba nguva yekutonga, pamwe nemubhadharo wekurapwa kamwe-kamwe, zvakasimudza kunetsekana nezvekuwanika kwevakadzi vazhinji.

 

Reference

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