[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

Product Name:[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

Synonyms:rPKPfQwFwLL-NH2, [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-substance P, Antagonist D

CAS No:96736-12-8

Purity:95%

Molar Mass:1460.76

Chemical Formula:C75H101N19O12

Storage:Store at -20 degrees Celsius

Sequence:D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-Gly-Leu-D-Trp-NH2

Target:NK1 receptor

Application:[D-Arg1,D-Phe?,D-Trp?,?,Leu11]-Substance P is a synthetic analog of Substance P, a neuropeptide known for its role in pain transmission, inflammation, and the regulation of mood. This modified version of Substance P includes substitutions at several positions with D-amino acids (D-Arg, D-Phe, D-Trp) and a Leu at position 11, which significantly enhances its stability and resistance to enzymatic degradation. These modifications also alter the peptide's affinity for neurokinin receptors, particularly the NK1 receptor, allowing researchers to study the effects of Substance P on different biological processes with greater specificity. This analog is particularly useful in research focused on neuropeptide receptor interactions, pain modulation, and the development of potential therapeutic agents for conditions such as chronic pain, depression, and inflammatory diseases.

Current Research:

[D-Arg1,D-Phe?,D-Trp?,?,Leu11]-Substance P is a synthetic analog of the neuropeptide Substance P, engineered to function as a potent antagonist of the neurokinin-1 (NK1) receptor. The strategic incorporation of D-amino acids at positions 1, 5, 7, and 9, along with the substitution of leucine at position 11, enhances its stability against enzymatic degradation and increases its receptor-binding affinity.
Mechanism of Action
By competitively binding to NK1 receptors, [D-Arg1,D-Phe?,D-Trp?,?,Leu11]-Substance P effectively inhibits the interaction of endogenous Substance P with these receptors. This blockade prevents the initiation of downstream signaling pathways associated with NK1 receptor activation, thereby modulating physiological processes such as pain transmission, inflammation, and stress responses.
Pharmacological Applications
The antagonist properties of this peptide have been extensively utilized in research to elucidate the role of NK1 receptors in various biological systems. For instance, studies have demonstrated its efficacy in reducing norepinephrine-induced ventricular arrhythmias in isolated rat hearts, highlighting its potential in cardiovascular research.
Clinical Implications
Given its ability to modulate NK1 receptor activity, [D-Arg1,D-Phe?,D-Trp?,?,Leu11]-Substance P serves as a valuable tool in the development of therapeutic agents targeting conditions such as chronic pain, depression, and emesis, where Substance P and NK1 receptors play a critical role.
Conclusion
As a selective and potent NK1 receptor antagonist, [D-Arg1,D-Phe?,D-Trp?,?,Leu11]-Substance P provides significant insights into the physiological and pathological roles of Substance P. Its application in research continues to advance our understanding of neurokinin-mediated processes and supports the development of targeted therapies for related disorders.

Reference:

Jarpe, M. B., Knall, C., Mitchell, F. M., Buhl, A. M., Duzic, E., & Johnson, G. L. (1998). [D-Arg1, D-Phe5, D-Trp7, 9, Leu11] Substance P acts as a biased agonist toward neuropeptide and chemokine receptors.?Journal of Biological Chemistry,?273(5), 3097-3104.