NA Selank Amidate e bonts'a botsitso bo ntlafalitsoeng ba limolek'hule le ka vivo pharmacokinetic profil ka leano la phetoho e habeli ea N-terminal acetylation le C-terminal amidation e thehiloeng ho sebopeho sa pele sa Selank.
Sena se fella ka ho eketseha ha halofo ea bophelo, matlafatsa mokoallo oa mali-boko bokgoni ba ho phunyeletsa, le bioactivity ea nako e telele mefuteng ea limolek'hule le ea liphoofolo.
Ho feta moo, NA Selank Amidate e bonts'a matla immunomodulation le ts'ebetso e khahlanong le khatello ea maikutlo.
Tatelano
ac-thr-lys-pro-arg-pro-gly-pro-nh2
Nomoro ea CAS
/
Foromo ea limolek'hule
Setšoantšo sa C35H60N12O9
Boima ba Molek'hule
792.94
Lipatlisiso tsa NA Selank Amidate
1.E bolokiloe le e Ntlafetseng ea Tšebetso
Katleho-bohlale,NA Selank Amidate e boloka litšobotsi tsohle tsa Selank, laolang asiti ea gamma-aminobutyric (GABA) neurotransmission bokong ha e ntse e etsa modulating dopaminergic le serotonergic litsamaiso tsa ho fana ka thepa e phahameng anxiolytic le sethibela maikutlo liphello.
E boetse e bonts'a ts'ebetso e betere ho feta Selank ho ntlafatseng ts'ebetso ea kelello le methapo, ho hlahisa ditlamorao tse ntle mabapi le ho ithuta, mohopolo, le tlhokomelo.
2.Liphello tsa Anxiolytic le Mood-Stabilizing
Ka mokhoa o itšetlehileng ka mahloriso le subtype-khetho, NA Selank Amidate allosterically modulates the GABA-A receptor ka ho matlafatsa ts'ebetso e tlamang ea GABA ho moamoheli oa eona kapa ho e ntlafatsa mocha oa ion ea chloride tshebetso ya ho bula.
Sena se eketsa haholo molumo oa inhibitory lipotolohong tsa bohlokoa tsa boko, ho hlahisa litlamorao tse hlakileng tsa anxiolytic.
Ho feta moo, litla-morao tsa ketso ena ea anxiolytic li bobebe haholo ho feta tsa lithethefatsi tse tloaelehileng tsa anxiolytic, ho etsa hore NA Selank Amidate e be motsoako o khahlehang oa ho tsitsisa maikutlo.
3.Ntlafatso ea Kelello le Neuroprotection
NA Selank Amidate e sebetsa ka kotloloho BDNF phetolelo ea lefutso ka ho susumetsa phosphorylation ya motshehetsi e leng teng CREB transcription factor le acetylation ea histone H3, BDNF e ntseng e eketseha mRNA maemo a 3.2 ka har'a lisele tsa hippocampal dentate gyrus granule le prefrontal cortical pyramidal neurons le secretion ea protheine ka makhetlo a 2.8 ka har'a 24 lihora.
Sena se kenya tshebetsong ho TrkB tsela ea receptor ho theosa le noka, ho susumetsa Ras-MAPK le PI3K-Molao cascade ho eketseha mokokotlo oa dendritic density ka 39%, upregulate synaptophysin expression by 45%, le ho khutlisetsa amplitude ea LTP boemong ba motheo.
Sena se atleha ho thibela kotsi e bakoang ke khatello ea kelello ea hippocampal neuronal le ho fokotseha ha kelello, e bonts'a likarolo tse ikhethang tsa neuroprotective.
4.Liphello tsa Immunomodulatory le Anti-Stress
NA Selank Amidate ke inhibitor ea tlholisano ea enzyme e senyang enkephalin., ho tshireletsa endogenous li-peptide tsa opioid ho tloha hydrolysis mme ka hona ba phahamisa maemo a bona, ha e ntse e thibela LPS (lipopolysaccharides)-tlhahiso e susumetsang ea pro-inflammatory li-cytokine ho kenyeletsa IL-6 le TNF-α ka 40-60% ka li-astrocyte.
NA Selank Amidate e boetse e hatella phetisetso ea nyutlelie ea NF-κB ka ho kena-kenana le ho hiroa ha MyD88 adapter protein., ho fana ka taolo ea ts'ireletso ho "neuroinflammatory microenvironment"..
COA
HPLC
MOF
