NA Selank Amidate

NA Selank Amidate

NA Selank Amidate

Hōʻike ʻo NA Selank Amidate i ka hoʻomaikaʻi ʻana i ka molecular stability a me ka vivo pharmacokinetic profile ma o kahi hoʻolālā hoʻololi pālua o ka N-terminal acetylation a me ka C-terminal amidation e pili ana i ke ʻano kumu o Selank.

 

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Hōʻike ʻo NA Selank Amidate i ka hoʻomaikaʻi ʻana i ke kūpaʻa molecular a me ka vivo pharmacokinetic profile ma o ka hoʻolālā hoʻololi pālua o N-terminal acetylation a me C-terminal amidation e pili ana i ka hana kumu o Selank.

Hoʻonui kēia i ka hapalua o ke ola, hoʻonui ʻia pale koko-lolo pono komo, a me ka bioactivity lōʻihi ma nā ʻano molekala a me nā holoholona.

Eia kekahi, Hōʻike ikaika ʻo NA Selank Amidate immunomodulation a me ka hana anti-stress.

Kaʻina

ac-thr-lys-pro-arg-pro-gly-pro-nh2

Helu CAS

/

ʻĀpana Molekala

C35H60N12O9

Kaumaha Molecular

792.94

Noiʻi o NA Selank Amidate

1.Paʻa a hoʻonui i ka pono

ʻO ka pono-naʻauao,Mālama ʻo NA Selank Amidate i nā ʻano āpau o Selank, hooponopono ana ʻakika gamma-aminobutyric (GABA) neurotransmission i loko o ka lolo me ka hoʻololi ʻana i ka dopaminergic a serotonergic nā ʻōnaehana e hāʻawi maikaʻi anxiolytic a antidepressant hopena.

Hōʻike pū ia i ka maikaʻi ʻoi aku ka maikaʻi ma mua o Selank i ka hoʻonui ʻana i nā hana cognitive a me neuroprotective, e hoʻopuka ana i nā hopena maikaʻi i ke aʻo ʻana, hoʻomanaʻo, a me ka noonoo.

2.Nā hopena anxiolytic a me ka hoʻopaʻa ʻana i ka naʻau

Ma kahi ʻano hilinaʻi a me subtype-koho, NA Selank Amidate allosterically modulates ka GABA-A mea hoʻokipa ma ka hoʻoikaika ʻana i ka pono paʻa o GABA i kāna mea loaʻa a hoʻonui paha chloride ion channel pono wehe.

Hoʻonui nui kēia i ka leo inhibitory i nā kaapuni lolo kī, ka hana ʻana i nā hopena anxiolytic.

Eia kekahi, ʻoi aku ka maʻalahi o nā hopena o kēia hana anxiolytic ma mua o nā lāʻau anxiolytic maʻamau, e hana ana iā NA Selank Amidate i mea hoʻohuihui hoʻopaʻa naʻau.

3.Hoʻonui i ka naʻau a me ka Neuroprotection

Hoʻōla pololei ʻo NA Selank Amidate BDNF gene transcription ma ka hooulu ana phosphorylation o ka mea hoʻolaha i loaʻa CREB mea unuhi a me ka acetylation o ka histone H3, hoʻonui i ka BDNF mRNA pae 3.2-fold i loko o ka hippocampal dentate gyrus granule cell a prefrontal cortical pyramidal neurons a me ka protein huna 2.8-fold i loko 24 hola.

Hoʻoikaika kēia i ka TrkB alaloa hōʻailona hōʻailona i lalo, hoʻokomo i ka Ras-MAPK a PI3K-Kanawai cascade e hoʻonui iwi kuamoʻo dendritic mānoanoa e 39%, upregulate synaptophysin olelo e 45%, a hoʻihoʻi hou i ka amplitude LTP i ka papa kuhikuhi.

Mālama maikaʻi kēia i ka hōʻeha hippocampal neuronal a me ka emi ʻana o ka cognitive, e hōʻike ana i nā waiwai neuroprotective ʻokoʻa.

4.Ka Immunomodulatory a me ka Anti-Stress Effects

ʻO NA Selank Amidate kahi mea hoʻokūkū hoʻokūkū o ka enkephalin-degrading enzyme, pale ʻana i ka endogenous nā peptide opioid mai hydrolysis a ma laila e hoʻokiʻekiʻe ai i ko lākou pae, oiai e keakea ana LPS (lipopolysaccharide)-hōʻike hoʻoulu ʻia o ka pro-inflammatory cytokines komo IL-6 a TNF-α e 40–60% in astrocytes.

Hoʻopiʻi pū ʻo NA Selank Amidate i ka unuhi nuklea NF-κB ma o ka hoʻopili ʻana i ka loaʻa ʻana o ka protein adapter MyD88., ka hāʻawi ʻana i ka hoʻoponopono palekana i ka microenvironment neuroinflammatory.

COA

HPLC

MS

(1) Makemake mākou, C. R.; Keʻokeʻo, C. M. ʻO nā mea hana hoʻomaha-Hypnotic e hoʻopilikia i nā mea hoʻokipa Gamma-Aminobutyric Acid.: E nānā pono iā Flunitrazepam, Gamma-Hydroxybutyric Acid, Phenibut, a me Selank. J Clin Pharmacol 2021, 61 ʻO Suppl 2, S114-S128. DOI: 10.1002/jcph.1922 Mai NLM M

(2) Mea ʻilihune, A.; Kolomin, Ua ʻōlelo ʻo T.; Andreeva, L.; Bondarenko, E.; Myasoedov, N.; Slominsky, P.; Shadrina, M. Hoʻonui ka Peptide Selank i ka hopena o ka Diazepam i ka hoʻohaʻahaʻa ʻana i ka hopohopo i nā kūlana koʻikoʻi ʻoluʻolu ʻole i nā ʻiole.. ʻO Neurol 2017, 2017, 50910

(3) Pin, L. ʻO G.; Nadorova, A. V.; Antipova, ʻO T. A.; Kruglov, S. V.; Kudrin, V. S.; ʻO Durnev, A. D. Selank, Peptide Analogue o Tuftsin, Pale aku i ka Ethanol-Induced Memory Impairment ma ka hooponopono ana i ka BDNF Content ma ka Hippocampus a me Prefrontal Cortex

(4) Pin, L. ʻO G.; Nadorova, A. V.; Seredenin, S. B. Hoʻopaʻa ʻo Selank i ka Hyperlocomotion i hoʻokomo ʻia i ka Ethanol a me ka hōʻike ʻana o ka ʻike ʻana i ka Behavioral Sensitization ma DBA / 2 Mice. Bull Exp Biol Med 2016, 162 (1), 56-59. DOI: 10.1007/s10517-016-3544-6 Mai NLM Medline.

(5) Koina, N. V.; Sokolov, O.; Gabaeva, M. V.; ʻO Grivennikov, I. A.; Andreeva, L. A.; Miasoedov, N. F.; Zozulia, A. A. [Hoʻopaʻa ʻo Semax a me selank i ka enkephalin-degrading enzymes mai ka serum kanaka]]. Bioorg Khim 2001, 27 (3), 180-183. DOI: 10.1023/a:10113730028

(6) ʻaʻole maopopo iaʻu, ʻO G. ʻO G.; Teleshova, E. S.; ʻO Bochkarev, V. K.; Koschelev, V. V.; ʻO Syunyakov, ʻO T. S. P.3.036 Novel anxiolytic Selank: Nā hopena o nā hoʻokolohua lapaʻau Phase II. ʻEulopa Neuropsychopharmacology 2005, 15, S159-S160. DOI: 10.1016/s0924-977x(05)80332-3.

(7) Slominsky, P. A.; Shadrina, M. I.; Kolomin, ʻO T. A.; ʻO Stavrovskaya, A. V.; Filatova, E. V.; Andreeva, L. A.; ʻO Illarishkin, S. N.; Myasoedov, N. F. Hoʻopilikia ka peptides semax a me selank i ka ʻano o nā ʻiole me ka parkinsonism like me 6-OHDA. A hiki i ka Biol Sc

(8) Sollertinskaja, ʻO T. N.; Shorokhov, M. V.; Myasoedov, N. F. ʻO nā hopena cerebroprotective o Semax a me Selank i nā primates i nā ʻano neurosis like ʻole. Ka Nupepa International no Psychophysiology 2008, 69 (3). DOI: 10.1016/j.ijpsycho.2008.05.356.

Kaʻina:

ac-thr-lys-pro-arg-pro-gly-pro-nh2

CAS:

/

M.W:

792.94 g/mol

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