NA Selank Amidate exhibits improved molecular stability and in vivo pharmacokinetic profile through a double-modification strategy of N-terminal アセチル化 and C-terminal amidation based on the original structure of セランク.
This results in an increased half-life, 強化された 血液脳関門 penetration efficiency, and prolonged bioactivity in both molecular and animal models.
さらに, NA Selank Amidate exhibits potent immunomodulation and anti-stress activity.
順序
ac-thr-lys-pro-arg-pro-gly-pro-nh2
CAS番号
/
分子式
C35H60N12O9
分子量
792.94
Research Of NA Selank Amidate
1.Retained and Enhanced Efficacy
Efficacy-wise,NA Selank Amidate retains all of the characteristics of Selank, regulating gamma-aminobutyric acid (GABA) neurotransmission in the brain while also modulating the ドーパミン作動性 そして セロトニン作動性 systems to deliver outstanding 抗不安薬 そして antidepressant effects.
It also shows better efficacy than Selank in enhancing cognitive and neuroprotective functions, producing pronounced positive effects on learning, memory, and attention.
2.Anxiolytic and Mood-Stabilizing Effects
In a concentration-dependent and subtype-selective manner, NA セランクアミデート allosterically modulates の GABA-A receptor by potentiating the binding efficacy of GABA to its receptor or enhancing chloride ion channel opening efficiency.
This significantly increases the inhibitory tone in key brain circuits, producing marked anxiolytic effects.
さらに, the side effects of this anxiolytic action are significantly milder than those of conventional anxiolytic drugs, making NA Selank Amidate a more attractive mood-stabilizing compound.
3.Cognitive Enhancement and Neuroprotection
NA Selank Amidate directly activates BDNF gene transcription by inducing リン酸化 of the promoter-located クレブ transcription factor and acetylation of histone H3, increasing BDNF mRNA levels 3.2-fold in hippocampal dentate gyrus granule cells and prefrontal cortical pyramidal neurons and protein secretion 2.8-fold within 24 時間.
This activates the TrkB receptor signaling pathway downstream, inducing the Ras-MAPK and PI3K-Akt cascade to increase 樹状突起スパイン density by 39%, upregulate synaptophysin expression by 45%, and restore LTP amplitude to baseline.
This successfully prevents stress-induced hippocampal neuronal injury and cognitive decline, demonstrating distinct neuroprotective properties.
4.Immunomodulatory and Anti-Stress Effects
NA Selank Amidate is a competitive inhibitor of enkephalin-degrading enzyme, protecting endogenous オピオイドペプチド から 加水分解 and thereby elevating their levels, while it inhibits LPS (リポ多糖類)-induced expression of pro-inflammatory cytokines 含む IL-6 そして TNF-α by 40–60% in アストロサイト.
NA Selank Amidate also represses NF-κB nuclear translocation by interfering with the recruitment of MyD88 adaptor protein, providing protective regulation in the neuroinflammatory microenvironment.
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