NA Selank Amidate exhibits improved molecular stability and in vivo pharmacokinetic profile through a double-modification strategy of N-terminal 아세틸화 and C-terminal amidation based on the original structure of 셀랑크.
This results in an increased half-life, enhanced 혈액뇌장벽 penetration efficiency, and prolonged bioactivity in both molecular and animal models.
게다가, NA Selank Amidate exhibits potent immunomodulation and anti-stress activity.
순서
ac-thr-lys-pro-arg-pro-gly-pro-nh2
CAS 번호
/
분자식
C35H60N12O9
분자량
792.94
Research Of NA Selank Amidate
1.Retained and Enhanced Efficacy
효능면에서,NA Selank Amidate retains all of the characteristics of Selank, regulating gamma-aminobutyric acid (GABA) neurotransmission in the brain while also modulating the dopaminergic 그리고 serotonergic systems to deliver outstanding 불안 완화제 그리고 antidepressant 효과.
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 셀랑크 아미데이트 allosterically modulates 그만큼 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.
뿐만 아니라, 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 인산화 of the promoter-located 크렙 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 시간.
This activates the TrkB receptor signaling pathway downstream, inducing the Ras-MAPK and PI3K-Akt cascade to increase dendritic spine 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 opioid peptides ~에서 가수 분해 and thereby elevating their levels, while it inhibits LPS (지질다당류)-induced expression of pro-inflammatory cytokines 포함 IL-6 그리고 TNF-α by 40–60% in astrocytes.
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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