[Arg14,Lys15]Nociceptin

Product Name:[Arg14,Lys15]Nociceptin

Synonyms:AKOS024456687

CAS No:236098-40-1

Purity:95%

Molar Mass:1909.2

Chemical Formula:C82H137N31O22

Storage:Store at -20 degrees Celsius

Sequence:FGGFTGARKSARKRKNQ

Application:

[Arg1?,Lys1?]Nociceptin is a synthetic analog of the endogenous peptide nociceptin/orphanin FQ, where the amino acids at positions 14 and 15 have been substituted with arginine (Arg) and lysine (Lys), respectively. These modifications are designed to alter the peptide's binding affinity and activity at the nociceptin receptor (NOP or ORL-1). [Arg1?,Lys1?]Nociceptin is often used in research to investigate the structure-activity relationships of nociceptin and to explore its role in modulating pain, stress, and other central nervous system functions. This analog provides valuable insights into the development of new therapeutic agents targeting the NOP receptor for pain management and neuropsychiatric conditions.

Current Research:

[Arg14,Lys15]Nociceptin is a synthetic analog of nociceptin/orphanin FQ, a neuropeptide that serves as the endogenous ligand for the nociceptin receptor (NOP, also known as ORL-1). This modified peptide incorporates arginine (Arg) at position 14 and lysine (Lys) at position 15, altering its interaction with the NOP receptor and its downstream signaling pathways. These substitutions are designed to enhance the peptide's binding properties, stability, or receptor selectivity, making it a valuable tool for investigating nociceptin signaling.
Biological Significance and Function
Nociceptin is a critical regulator of various physiological processes, including:
Pain Modulation: It plays a role in both pronociceptive and antinociceptive mechanisms, depending on the context.
Stress and Anxiety: Nociceptin influences behavioral responses to stress and anxiety by acting on central nervous system pathways.
Addiction: It modulates reward pathways, making it a target in studies of substance abuse and addiction.
Research Applications of [Arg14,Lys15]Nociceptin
NOP Receptor Pharmacology: The Arg and Lys substitutions are hypothesized to modify the peptide's affinity or efficacy at the NOP receptor, providing insights into receptor-ligand interactions and potential mechanisms of signal transduction.
Pain Management Studies: This analog is used in preclinical models to better understand nociceptin's dual role in pain modulation, offering pathways to novel analgesics.
Neuropsychiatric Research: Its effects on stress and mood regulation pathways are explored for potential therapeutic applications in anxiety and depression.
Emerging Insights
The structural modifications in [Arg14,Lys15]Nociceptin have sparked interest in designing analogs that can serve as selective NOP receptor agonists or antagonists. Such tools are instrumental in elucidating the complex roles of nociceptin signaling in health and disease.
In summary, [Arg14,Lys15]Nociceptin represents a powerful tool in neuroscience and pharmacology, advancing our understanding of the nociceptin system and its therapeutic potential.

Reference:

Rizzi, D., Rizzi, A., Bigoni, R., Camarda, V., Marzola, G., Guerrini, R., ... & Regoli, D. (2002). [Arg14, Lys15] nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. Journal of Pharmacology and Experimental Therapeutics, 300(1), 57-63.