[Nphe1]Nociceptin(1-13)NH2

Product Name:[Nphe1]Nociceptin(1-13)NH2

CAS No:267234-08-2

Purity:95%

Molar Mass:1381.6

Chemical Formula:C61H100N22O15

Storage:Store at -20 degrees Celsius

Sequence:GGGFTGARKSARK

Target:nociceptin receptor

Application:

[Nphe¹]Nociceptin(1-13)NH₂ is a synthetic analog of the nociceptin/orphanin FQ peptide, modified at the first position with 1-naphthylalanine (Nphe) and truncated to the first 13 amino acids with an amidated C-terminus. This modification enhances the peptide's stability and selectivity in binding to the nociceptin receptor (NOP or ORL-1). As a selective agonist, [Nphe¹]Nociceptin(1-13)NH₂ is used in research to study the NOP receptor's role in pain modulation, anxiety, and various neurophysiological processes. The peptide is valuable for exploring the therapeutic potential of NOP receptor-targeted treatments for conditions like chronic pain, depression, and other neuropsychiatric disorders.

Current Research:

[Nphe¹]Nociceptin(1-13)NH₂ is a synthetic analog of nociceptin/orphanin FQ (N/OFQ), designed to selectively antagonize the nociceptin receptor (NOP). It features a substitution of the N-terminal phenylalanine residue with 1-naphthylalanine (Nphe), which confers enhanced receptor binding specificity and altered pharmacological activity.

Mechanism of Action
Receptor Specificity:
[Nphe¹]Nociceptin(1-13)NH₂ binds selectively to the NOP receptor, competitively inhibiting the interaction of endogenous nociceptin. This antagonism blocks NOP receptor-mediated signaling, thereby modulating physiological processes regulated by nociceptin.

Pharmacological Profile:
The Nphe¹ substitution enhances the peptide's stability and binding affinity to the NOP receptor while maintaining its ability to function as a potent antagonist. This modification also minimizes off-target effects on other opioid receptors, ensuring specificity.

Physiological and Research Applications
Pain Modulation:
[Nphe¹]Nociceptin(1-13)NH₂ is widely used in research to study the role of the NOP receptor in pain pathways. By blocking nociceptin-induced hyperalgesia, it provides insights into the development of novel analgesics.

Stress and Anxiety Research:
NOP receptors play a critical role in stress response and emotional regulation. This antagonist is used to investigate the impact of nociceptin signaling on anxiety-like behaviors and stress-related disorders.

Addiction Studies:
The NOP receptor is implicated in substance abuse and reward mechanisms. [Nphe¹]Nociceptin(1-13)NH₂ is a valuable tool for exploring the therapeutic potential of NOP receptor antagonism in addiction management.

Drug Development:
As a selective NOP receptor antagonist, it serves as a reference compound for the development and validation of NOP-targeting drugs.

Handling and Storage
Store the lyophilized peptide at -20°C in a desiccated environment to maintain stability.
Reconstitute in sterile water or an appropriate buffer for experimental use.
Conclusion
[Nphe¹]Nociceptin(1-13)NH₂ is a powerful tool for studying the physiological and pathological roles of the NOP receptor. Its selective antagonistic properties make it indispensable in research focused on pain modulation, stress, and the development of therapeutic interventions targeting the nociceptin system.

Reference:

Corradini, L., Briscini, L., Ongini, E., & Bertorelli, R. (2001). The putative OP4 antagonist,[Nphe1] nociceptin (1-13) NH2, prevents the effects of nociceptin in neuropathic rats. Brain research, 905(1-2), 127-133.