[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2

Product Name:[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2

Synonyms:BDBM50472729

CAS No:213130-17-7

Purity:95%

Molar Mass:1367.6

Chemical Formula:C61H102N22O14

Storage:Store at -20 degrees Celsius

Sequence:GGFTGARKSARK

Application:

[Phe¹Ψ(CH₂-NH)Gly²]Nociceptin(1-13)NH₂ is a modified synthetic peptide that mimics the N-terminal fragment of nociceptin, a neuropeptide involved in pain modulation and various neurological processes. The substitution at the first position (Phe¹) with a ψ(CH₂-NH) bond between Phe¹ and Gly² enhances the peptide's stability by making it resistant to enzymatic degradation, while the amide group at the C-terminus (NH₂) further contributes to its stability and bioactivity. This peptide is particularly useful in research focused on the nociceptin/orphanin FQ receptor (NOP) system, enabling the study of pain pathways, mood disorders, and potential therapeutic interventions. [Phe¹Ψ(CH₂-NH)Gly²]Nociceptin(1-13)NH₂ is a critical tool for advancing our understanding of nociceptin's role in the central nervous system.

Current Research:

[Phe¹Ψ(CH₂-NH)Gly²]Nociceptin(1-13)NH₂ is a synthetic peptide analog of nociceptin, the endogenous ligand for the nociceptin/orphanin FQ receptor (NOP). This analog features a reduced peptide bond (Ψ(CH₂-NH)) between the first phenylalanine (Phe¹) and second glycine (Gly²) residues, enhancing its metabolic stability.

Initially characterized as a potent NOP receptor agonist, [Phe¹Ψ(CH₂-NH)Gly²]Nociceptin(1-13)NH₂ has demonstrated both agonistic and antagonistic properties in various biological assays. In vitro studies have shown its ability to inhibit cyclic AMP accumulation and modulate ion channel activity, indicating agonist activity. Conversely, in vivo experiments have reported its capacity to block nociceptin-induced effects, suggesting antagonist behavior.

The dual activity of this peptide makes it a valuable tool for investigating NOP receptor pharmacology and the physiological roles of nociceptin. Its enhanced stability and unique pharmacological profile provide insights into receptor-ligand interactions and aid in the development of therapeutic agents targeting the NOP receptor system.

In summary, [Phe¹Ψ(CH₂-NH)Gly²]Nociceptin(1-13)NH₂ is a significant compound in neuropharmacological research, offering a deeper understanding of nociceptin signaling pathways and potential therapeutic applications for disorders involving the NOP receptor.

Reference:

Candeletti, S., Guerrini, R., Caló, G., Romualdi, P., & Ferri, S. (1999). Supraspinal and spinal effects of [Phe1ψ (CH2-NH) Gly2]-nociceptin (1–13)-NH2 on nociception in the rat. Life sciences, 66(3), 257-264.