N-Actetyl Selank Amidate

Research Overview

N-Acetyl Selank Amidate serves as a valuable research tool for investigating enhanced anxiolytic mechanisms, prolonged cognitive modulation, and sustained neurotransmitter system effects in laboratory settings. This modified heptapeptide represents a second-generation analog of Selank, incorporating N-terminal acetylation (Ac-) and C-terminal amidation (-NH₂) to dramatically improve metabolic stability and extend duration of biological activity.

The peptide’s development focused on addressing the rapid enzymatic degradation that limits the duration of action of unmodified peptides. N-terminal acetylation blocks aminopeptidase attack, while C-terminal amidation prevents carboxypeptidase degradation, resulting in substantially extended plasma half-life and tissue persistence. Laboratory studies investigate NA-Selank’s effects on anxiety-related behaviors, cognitive performance markers, neurotransmitter systems, and stress response mechanisms in preclinical models.

NA-Selank research demonstrates pharmacological effects qualitatively similar to Selank but with markedly extended duration of action. This enhanced stability profile allows researchers to investigate long-term modulation of neurotransmitter systems, sustained behavioral effects, and cumulative neuroplastic changes with simplified dosing regimens in experimental protocols.

Molecular Characteristics

Complete Specifications:

• CAS Registry Number: 864070-44-0
• Molecular Weight: 793.93 Da
• Molecular Formula: C₃₅H₆₀N₁₂O₉
• Amino Acid Sequence: Ac-Thr-Lys-Pro-Arg-Pro-Gly-Pro-NH₂
• Peptide Classification: Modified synthetic tuftsin analog
• Modifications: N-terminal acetylation, C-terminal amidation
• Appearance: White to off-white lyophilized powder
• Solubility: Water, bacteriostatic water, phosphate buffered saline
• Net Charge: +2 at physiological pH

The peptide’s modified structure incorporates an acetyl group (CH₃CO-) at the N-terminus and an amide group (-NH₂) at the C-terminus, replacing the free amino and carboxyl groups present in unmodified Selank. These terminal modifications create a more lipophilic molecule with enhanced membrane permeability and resistance to enzymatic degradation. The core sequence maintains three proline residues and two basic amino acids (lysine, arginine) that contribute to biological activity and receptor interactions.

Pharmacokinetic Profile in Research Models

NA-Selank pharmacokinetic characterization in preclinical research reveals substantially enhanced properties compared to unmodified Selank:

Enhanced Stability Profile:

• Plasma half-life: Approximately 200-300 minutes (vs. 20-30 minutes for Selank)
• Enzymatic resistance: 8-10 fold increased stability vs. unmodified peptide
• Brain tissue persistence: Extended detection in CNS tissue
• Biological activity duration: Effects observed for 8-12 hours post-administration

Absorption and Distribution:

• Multiple administration routes investigated: intranasal, subcutaneous, intraperitoneal
• Blood-brain barrier penetration: Enhanced vs. unmodified Selank
• Tissue distribution: Broader and more sustained tissue exposure
• Peak plasma concentrations: 30-60 minutes post-administration

Metabolic Considerations:

• Primary degradation: Slower enzymatic cleavage at internal peptide bonds
• Metabolites: Similar profile to Selank but with delayed formation
• Excretion: Primarily renal following metabolism

These enhanced pharmacokinetic characteristics enable research protocols with extended observation periods, reduced dosing frequency, and investigation of cumulative effects over extended timeframes.

Research Applications

Extended Anxiolytic Mechanism Studies

NA-Selank serves as a research tool for investigating sustained anxiolytic mechanisms:

• Prolonged GABAergic Modulation: Investigation of extended GABA system effects without tolerance development
• Sustained Stress Response: Analysis of long-term HPA axis regulation and cortisol dynamics
• Chronic Stress Models: Examination of repeated exposure paradigms with sustained anxiolytic activity
• Circadian Rhythm Integration: Studies on anxiety behavior across multiple light/dark cycles
• Long-Term Receptor Changes: Investigation of chronic receptor expression and sensitivity adaptations

Research protocols employ extended behavioral testing paradigms, serial neurochemical sampling, and longitudinal assessment of anxiety-related measures to characterize NA-Selank’s prolonged anxiolytic profile.

Sustained Cognitive Enhancement Research

Laboratory studies investigate NA-Selank in prolonged cognitive modulation research:

• Multi-Day Learning Protocols: Investigation of sustained effects on acquisition and consolidation
• Working Memory Research: Analysis of extended improvement in working memory performance
• Attention Span Studies: Examination of sustained attention and vigilance over extended periods
• Cognitive Endurance: Research on mental fatigue resistance and sustained cognitive performance
• Neuroplasticity Investigations: Studies on cumulative effects on synaptic plasticity markers

Experimental models include multi-day cognitive testing batteries, chronic dosing paradigms, and longitudinal assessment of cognitive performance to leverage NA-Selank’s extended duration of action.

Chronic Neuroprotection Research

Research applications extend to sustained neuroprotective mechanism investigation:

• Cumulative Antioxidant Effects: Examination of long-term oxidative stress reduction
• Sustained Anti-Inflammatory Activity: Investigation of chronic neuroinflammation modulation
• Repeated Injury Models: Studies on protection against repeated or ongoing neural insults
• Neurodegenerative Models: Research in chronic progressive neurodegeneration paradigms
• Long-Term Neurotrophic Support: Investigation of sustained BDNF and growth factor expression

Laboratory protocols investigate NA-Selank’s neuroprotective effects in chronic exposure models, repeated injury paradigms, and long-term neurodegeneration studies where sustained activity provides experimental advantages.

Prolonged Neurotransmitter Modulation

NA-Selank provides a research tool for investigating extended neurotransmitter system effects:

• Sustained Monoamine Levels: Studies on prolonged serotonin, dopamine, and norepinephrine modulation
• Chronic Enzyme Expression: Investigation of long-term changes in metabolic enzyme expression
• Receptor Adaptation Research: Analysis of receptor sensitivity and density changes with chronic exposure
• Synaptic Remodeling: Research on structural synaptic changes with sustained neurotransmitter modulation
• Homeostatic Plasticity: Investigation of compensatory mechanisms in response to prolonged modulation

Laboratory investigations examine NA-Selank’s extended effects through longitudinal neurochemical analysis, repeated behavioral assessment, and molecular analysis of chronic adaptations.

Stress Resilience Research

NA-Selank facilitates investigation of sustained stress resistance mechanisms:

• Chronic Stress Paradigms: Research in repeated stress exposure models
• Stress Recovery Studies: Investigation of accelerated recovery and resilience building
• Behavioral Sensitization: Analysis of stress-induced behavioral sensitization prevention
• Neuroendocrine Adaptation: Studies on HPA axis adaptation to chronic stress
• Stress-Related Pathology: Research on prevention of stress-induced structural and functional changes

Research protocols examine NA-Selank’s effects in chronic unpredictable stress, repeated restraint stress, and other long-term stress paradigms where extended activity duration provides experimental utility.

Laboratory Handling and Storage Protocols

Lyophilized Powder Storage:

• Store at -20°C to -80°C in original sealed vial
• Protect from light exposure and moisture
• Desiccated storage environment required
• Stability data available for 12+ months at -20°C
• Enhanced stability vs. unmodified Selank even in lyophilized form

Reconstitution Guidelines:

• Reconstitute with sterile water, bacteriostatic water (0.9% benzyl alcohol), or appropriate buffer
• Add solvent slowly down vial side to minimize foaming
• Gentle swirling motion recommended (avoid vigorous shaking)
• Allow complete dissolution before use (typically 1-2 minutes)
• Final pH should be 6.0-7.5 for optimal stability

Reconstituted Solution Storage:

• Short-term storage: 4°C for up to 14 days (extended vs. Selank)
• Long-term storage: -20°C in aliquots to avoid freeze-thaw cycles
• Single-use aliquots recommended to maintain peptide integrity
• Improved stability allows more flexible handling vs. unmodified peptide
• Avoid repeated freeze-thaw cycles (maximum 3-4 cycles)

Stability Advantages:
NA-Selank demonstrates significantly enhanced stability compared to unmodified Selank. The terminal modifications provide resistance to enzymatic degradation even at room temperature for short periods, though standard peptide handling protocols should still be followed.

Quality Assurance and Analytical Testing

Each NA-Selank batch undergoes comprehensive analytical characterization:

Purity Analysis:

• High-Performance Liquid Chromatography (HPLC): ≥98% purity
• Analytical method: Reversed-phase HPLC with UV detection at 214nm
• Verification of acetylation and amidation modifications

Structural Verification:

• Electrospray Ionization Mass Spectrometry (ESI-MS): Confirms molecular weight 793.93 Da
• Amino acid analysis: Verifies sequence composition
• Terminal modification confirmation: Validates acetylation and amidation
• Peptide content determination: Quantifies actual peptide content by weight

Contaminant Testing:

• Bacterial endotoxin: <5 EU/mg (LAL method)
• Heavy metals: Below detection limits per USP standards
• Residual solvents: TFA and acetonitrile within acceptable limits
• Water content: Karl Fischer titration (<8%)

Documentation:

• Certificate of Analysis (COA) provided with each batch
• Third-party analytical verification available upon request
• Stability data documented for recommended storage conditions
• Batch-specific QC results traceable by lot number

Research Considerations

Experimental Design Factors:

Researchers should consider several factors when designing NA-Selank experiments:

1. Extended Activity Profile: NA-Selank’s prolonged duration of action allows for once-daily or less frequent administration in research protocols, simplifying experimental design.

2. Concentration Selection: Due to enhanced potency and duration, lower effective concentrations may be appropriate compared to unmodified Selank. Dose-response relationships should be established.

3. Temporal Assessment: Design measurement timelines to capture extended effects. Assessment points at 4, 8, 12, and 24 hours may reveal sustained activity.

4. Chronic vs. Acute Paradigms: NA-Selank is particularly suited for chronic administration studies where sustained effects are desired.

5. Comparative Studies: Direct comparison with unmodified Selank can illuminate the specific advantages of terminal modifications.

Mechanism Investigation:

NA-Selank’s mechanisms of action are expected to parallel Selank but with extended temporal dynamics:

• Prolonged GABAergic system modulation
• Sustained monoamine neurotransmitter effects
• Extended BDNF upregulation
• Cumulative gene expression changes
• Long-term synaptic plasticity effects

The enhanced stability allows investigation of mechanisms requiring sustained peptide presence.

Compliance and Safety Information

Regulatory Status:
N-Acetyl Selank Amidate is provided as a research chemical for in-vitro laboratory studies and preclinical research only. This product has not been approved by the FDA for human therapeutic use, dietary supplementation, or medical applications.

Intended Use:

• In-vitro cell culture studies
• In-vivo preclinical research in approved animal models
• Laboratory investigation of biological mechanisms
• Academic and institutional research applications

NOT Intended For:

• Human consumption or administration
• Therapeutic treatment or diagnosis
• Dietary supplementation
• Veterinary therapeutic applications without appropriate oversight

Safety Protocols:
Researchers should follow standard laboratory safety practices when handling NA-Selank:

• Use appropriate personal protective equipment (lab coat, gloves, safety glasses)
• Handle in well-ventilated areas or fume hood
• Follow institutional biosafety guidelines
• Dispose of waste according to local regulations for biological/chemical waste
• Consult material safety data sheet (MSDS) for additional safety information

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