NA Selank Amidate exhibits improved molecular stability and in vivo pharmacokinetic profile through a double-modification strategy of N-terminal أستلة and C-terminal amidation based on the original structure of سيلانك.
This results in an increased half-life, معززة حاجز الدم في الدماغ penetration efficiency, and prolonged bioactivity in both molecular and animal models.
علاوة على ذلك, NA Selank Amidate exhibits potent التحوير المناعي and anti-stress activity.
تسلسل
ac-thr-lys-pro-arg-pro-gly-pro-nh2
رقم كاس
/
الصيغة الجزيئية
C35H60N12O9
الوزن الجزيئي
792.94
Research Of NA Selank Amidate
1.Retained and Enhanced Efficacy
الفعالية الحكيمة,NA Selank Amidate retains all of the characteristics of Selank, تنظيم gamma-aminobutyric acid (غابا) neurotransmission in the brain while also modulating the الدوبامين و هرمون السيروتونين systems to deliver outstanding مزيل القلق و antidepressant تأثيرات.
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 سيلانك أميدات allosterically modulates ال 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.
بالإضافة إلى, 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 بدنف gene transcription by inducing الفسفرة of the promoter-located كريب transcription factor and acetylation of histone H3, increasing BDNF مرنا levels 3.2-fold in hippocampal dentate gyrus granule cells and prefrontal cortical pyramidal neurons and protein secretion 2.8-fold within 24 ساعات.
This activates the TrkB receptor signaling pathway downstream, inducing the Ras-MAPK and PI3K-قانون cascade to increase العمود الفقري الشجيري 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 الببتيدات الأفيونية من التحلل المائي and thereby elevating their levels, while it inhibits LPS (عديد السكاريد الدهني)-induced expression of pro-inflammatory السيتوكينات مشتمل إيل-6 و TNF-α by 40–60% in الخلايا النجمية.
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.
شهادة توثيق البرامج
HPLC
آنسة
