Ko te NA Selank Amidate e whakaatu ana i te pai ake o te whakapumautanga ngota me te in vivo pharmacokinetic he tohu i roto i te rautaki whakarereke-rua o te waahanga-N whakakaha me C-terminal amidation i runga i te hanganga taketake o Selank.
Na tenei ka piki ake te haurua o te ora, whakarei arai toto-roro te kaha o te urunga, me te roa o te koiora i roto i nga tauira ngota me nga tauira kararehe.
I tua atu, Ko NA Selank Amidate e whakaatu ana i te kaha immunomodulation me te mahi anti-stress.
Raupapa
ac-thr-lys-pro-arg-pro-gly-pro-nh2
Tau CAS
/
Tātai rāpoi
C35H60N12O9
Taumaha rāpoi
792.94
Rangahau o NA Selank Amidate
1.Te Pumau me te Whakanuia te Whainga
Te kaha-whakaaro,NA Selank Amidate kei te pupuri i nga ahuatanga katoa o Selank, whakahaere waikawa gamma-aminobutyric (GABA) neurotransmission i roto i te roro i te whakarereketanga ano hoki i te dopaminergic a serotonergic nga punaha ki te whakaputa tino pai anxiolytic a rongoā mate pānga.
Ka whakaatu hoki i te pai ake o te whaihua atu i a Selank ki te whakarei ake i nga mahi hinengaro me te neuroprotective, te whakaputa i nga hua pai ki te ako, maharahara, me te aro.
2.Anxiolytic and Mood-Stabilizing Effects
I roto i te kukū-ti'aturi me te momo-iti te tikanga, NA Selank Amidate ka huri i te allosterically te GABA-He kaiwhiwhi na roto i te whakakaha i te kaha here o GABA ki tana kaiwhakawhiwhi, ki te whakarei ake ranei hongere katote pūhaumāota kakama whakatuwhera.
Ka tino whakanui ake tenei i te reo aukati i roto i nga iahiko roro matua, te whakaputa i nga paanga anxiolytic kua tohua.
I tua atu, ko nga paanga o tenei mahi anxiolytic he tino ngawari ake i era o nga raau taero anxiolytic tikanga, hanga NA Selank Amidate he puhui whakapumau te ahua ataahua.
3.Te Whakanui Hinengaro me te Neuroprotection
NA Selank Amidate ka whakahohe tika BDNF te whakawhitinga ira ma te whakaawe phosphorylation o te kaiwhakatairanga-kei CREB te tauwehe whakawhiti me te acetylation o te histone H3, te whakanui ake i te BDNF mRNA taumata 3.2-whakapa i roto i te hippocampal dentate gyrus granule pūtau me nga neuron pyramidal cortical prefrontal me te hunanga pūmua 2.8-fold i roto 24 haora.
Ma tenei ka whakahohe i te TrkB te huarahi tohu tohu whakararo, whakaawe i te Ras-MAPK me PI3K-Te Ture cascade ki te whakanui ake tuawhenua dendritic kiato e 39%, upregulate synaptophysin expression by 45%, me te whakahoki ano i te kaha kaha o te LTP ki te rarangi turanga.
He pai te aukati i te whara o te hippocampal neuronal me te heke o te hinengaro, e whakaatu ana i nga ahuatanga neuroprotective motuhake.
4.Nga Painga Immunomodulatory me te Anti-Stress
Ko NA Selank Amidate he aukati whakataetae o te enkephalin-degrading enzyme, tiaki endogenous peptides opioid mai hauwai na reira ka hiki ake o ratou taumata, i te wa e aukati ana LPS (lipopolysaccharide)-te whakapuakitanga o te pro-inflammatory cytokines tae atu ki IL-6 a TNF-α na 40–60% in astrocytes.
Ko NA Selank Amidate ano hoki ka pehia te whakawhiti karihi NF-κB ma te pokanoa ki te whakauru i te pūmua urutau MyD88, te whakarato i nga ture tiaki i roto i te taiao neuroinflammatory microenvironment.
COA
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