NA Selank Amidate exhibits improved molecular stability and in vivo pharmacokinetic profile through a double-modification strategy of N-terminal ацетилләшеү and C-terminal amidation based on the original structure of Селәнк.
This results in an increased half-life, көсәйтелгән ҡан-мейе барьеры penetration efficiency, and prolonged bioactivity in both molecular and animal models.
Ул ғына ла түгел, NA Selank Amidate exhibits potent иммуномодуляция and anti-stress activity.
Эҙмә-эҙлелек
ак-тр-лис-про-арг-про-гли-про-нх2.
CAS номеры
/
Молекуляр формула
C35H60N12O9
Молекуляр ауырлыҡ
792.94
Research Of NA Selank Amidate
1.Retained and Enhanced Efficacy
Efficacy-wise,NA Selank Amidate retains all of the characteristics of Selank, көйләү gamma-aminobutyric acid (ГАМК) neurotransmission in the brain while also modulating the дофаминергик һәм серотонергик systems to deliver outstanding анксиолит һәм 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, Н.А.Селанк Амидате allosterically modulates был 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.
Унан да бигерәк, 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 БДНФ gene transcription by inducing фосфорилләшеү of the promoter-located КРЕБ transcription factor and acetylation of histone H3, increasing BDNF мРНК levels 3.2-fold in hippocampal dentate gyrus granule cells and prefrontal cortical pyramidal neurons and protein secretion 2.8-fold within 24 сәғәт.
This activates the TrkB receptor signaling pathway downstream, inducing the Ras-MAPK and PI3K-Акт cascade to increase дендрит умыртҡа һөйәге 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 опиоид пептидтары йылдан гидролиз and thereby elevating their levels, while it inhibits ЛПС (липополисахарид)-induced expression of pro-inflammatory цитокиндар шул иҫәптән ИЛ-6. һәм ТНФ-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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