ادلنک

Adalank is a synthetic peptide analogue of selank, with targeted chemical alteration.

 

 

اپنی محبت بانٹیں۔

Adalank is a synthetic peptide analogue of selank, with targeted chemical alteration.

The peptide is designed as a derivative of the nootropic drug Selank, with the addition of an acetylated N-terminal function that enhances its adamantane-like sterically-constraining structure.

This modification acts as a powerful synergistic potentiator of the anxiolytic – nootropic compound Selank.

It circumvents Selank’s poor خون دماغ کی رکاوٹ (بی بی بی) penetration, thereby increasing the central nervous system activity of Adalank significantly.

The addition of an acetyl group eliminates the positive charge of the N-terminal free amino group and decreases the net charge of the peptide.

This physicochemical adjustment optimizes the isoelectric point and surface properties of Adalank, reducing non-specific electrostatic interactions.

نتیجے کے طور پر, the drug molecule crosses the blood–brain barrier more easily and reaches the central nervous system.

مزید برآں, acetylation protects Adalank from exopeptidase degradation and significantly increases its in vivo half-life.

This provides the advantage of prolonged therapeutic blood levels and reduces frequent dosing.

The inclusion of adamantane creates a stable “conformation core” in the Adalank peptide.

This imparts a fixed spatial orientation to the initially flexible linear peptide, promoting the stereochemical conformation necessary for biological activity even in its unbound state.

This greatly improves Adalank’s ability to cross the blood-brain barrier.

In addition, Adalank exhibits certain immunomodulatory effects.

ترتیب

ac-thr-lys-pro-arg-pro-gly-pro-Adamantane-nh2

CAS نمبر

/

مالیکیولر فارمولا

C46H75N13O10

سالماتی وزن

970.19

Research Of Adalank:

1.Mechanism of Action

Efficacy-wise, Adalank’s rigid structure more closely corresponds to the allosteric modulation site of the GABA_A receptor alpha subunit, imparting stronger anxiolytic effects.

مزید, the adamantane moiety enables hydrophobic interactions in the NMDA رسیپٹر channel area to moderate calcium influx and protect against excitotoxic injury.

This property has the potential for neuroprotection in models of ischemic brain injury and post-traumatic stress disorder (پی ٹی ایس ڈی).

2.Anxiolytic Effects

As an optimized derivative of Selank, Adalank maintains a high-affinity interaction with the benzodiazepine site on the GABA_A receptor α-subunit.

تاہم, the N-terminal acetylation and adamantane scaffold shift the binding mode from “flexible induced fit” to “rigid precise docking”.

This enhances GABAergic inhibitory neurotransmission, promoting chloride influx and rapid reduction of activity in hyperactive amygdala-prefrontal cortex neural circuits.

In contrast to benzodiazepines, Adalank shows high receptor subtype selectivity, enabling sustained anxiolytic effects without the sedation, muscle relaxation, or addiction potential associated with traditional drugs.

Its therapeutic index is 3 کو 5 times wider, supporting long-term management of generalized anxiety disorder and situational anxiety disorders.

3.Cognitive Enhancement and Memory Improvement

Adalank effectively inhibits the activation of the NF-κB inflammatory pathway and increases بی ڈی این ایف mRNA expression by 50%-80% in the hippocampus.

This leads to activation of downstream Akt/CREB signaling pathways, facilitating LTP induction and maintenance.

It significantly improves memory retention in passive avoidance ٹیسٹ, enhances spatial learning in the مورس واٹر بھولبلییا, and counteracts scopolamine-induced cholinergic damage.

Preclinical data indicate that Adalank reduces working memory errors by 40%-60% and mitigates natural memory decline in aged animals, suggesting applicability in learning disorders, mild cognitive impairment, and age-related memory decline.

4.نیورو پروٹیکٹو اثرات

The adamantane structure in Adalank mimics the action of memantine, acting as a non-competitive NMDA رسیپٹر antagonist that causes voltage-dependent blockade of open channels and physiological regulation of calcium influx.

It reduces pathological Ca²⁺ influx by 60–70% without impairing physiological synaptic Ca²⁺ signaling, achieving a selective neuroprotective profile without disrupting normal function.

اس طرح, preclinical studies highlight Adalank’s significant translational potential for early intervention in acute stroke, spinal cord injury, اور neurodegenerative بیماریوں.

COA

HPLC

MS

(1) Doyno, سی. آر; سفید, سی. ایم. Sedative-Hypnotic Agents That Impact Gamma-Aminobutyric Acid Receptors: Focus on Flunitrazepam, Gamma-Hydroxybutyric Acid, Phenibut, and Selank. J Clin Pharmacol 2021, 61 Suppl 2, S114-S128. ڈی او آئی: 10.1002/jcph.1922 From NLM M

(2) Kasian, اے۔; Kolomin, ٹی۔; اینڈریوا, ایل۔; Bondarenko, ای۔; میاسوڈوف, ن; Slominsky, پی۔; Shadrina, ایم. Peptide Selank Enhances the Effect of Diazepam in Reducing Anxiety in Unpredictable Chronic Mild Stress Conditions in Rats. Behav Neurol 2017, 2017, 50910

(3) Kolik, ایل. جی۔; Nadorova, اے. وی; Antipova, ٹی. اے۔; Kruglov, ایس. وی; کدرین, وی. ایس۔; Durnev, اے. ڈی. سیلانک, Peptide Analogue of Tuftsin, Protects Against Ethanol-Induced Memory Impairment by Regulating of BDNF Content in the Hippocampus and Prefrontal Cortex

(4) Kolik, ایل. جی۔; Nadorova, اے. وی; Seredenin, ایس. بی. Selank Inhibits Ethanol-Induced Hyperlocomotion and Manifestation of Behavioral Sensitization in DBA/2 Mice. Bull Exp Biol Med 2016, 162 (1), 56-59. ڈی او آئی: 10.1007/s10517-016-3544-6 From NLM Medline.

(5) لاگت, ن. وی; سوکولوف, اے; گابایوا, ایم. وی; Grivennikov, میں. اے۔; اینڈریوا, ایل. اے۔; میاسوڈوف, ن. ایف۔; زوزولیا, اے. اے. [Semax اور selank انسانی سیرم سے enkephalin-degrading enzymes کو روکتے ہیں۔]]. بائیورگ کھیم 2001, 27 (3), 180-183. ڈی او آئی: 10.1023/a:10113730028

(6) Neznamov, جی. جی۔; Teleshova, ای. ایس۔; Bochkarev, وی. کے; Koschelev, وی. وی; Syunyakov, ٹی. ایس. P.3.036 Novel anxiolytic Selank: Results of thePhase II clinical trials. European Neuropsychopharmacology 2005, 15, S159-S160. ڈی او آئی: 10.1016/s0924-977x(05)80332-3.

(7) Slominsky, پی. اے۔; Shadrina, ایم. میں; Kolomin, ٹی. اے۔; Stavrovskaya, اے. وی; Filatova, ای. وی; اینڈریوا, ایل. اے۔; Illarioshkin, ایس. ن; میاسوڈوف, ن. ایف. Peptides semax and selank affect the behavior of rats with 6-OHDA induced PD-like parkinsonism. Dokl Biol Sc

(8) Sollertinskaja, ٹی. ن; Shorochov, ایم. وی; میاسوڈوف, ن. ایف. The cerebroprotective effects of Semax and Selank in primates at different types of neurosis. International Journal of Psychophysiology 2008, 69 (3). ڈی او آئی: 10.1016/j.ijpsycho.2008.05.356.

ترتیب:

ac-thr-lys-pro-arg-pro-gly-pro-Adamantane-nh2

سی اے ایس:

N/A

ایم ڈبلیو:

970.19 g/mol

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