GR 94800

Product Name:GR 94800

Synonyms:N-alpha-Benzoylalanyl-alanyl-tryptophyl-phenylalanyl-prolyl-prolyl-norleucinamide

CAS No:141636-65-9

Purity:95%

Molar Mass:904.1

Chemical Formula:C49H61N9O8

Storage:Store at -20 degrees Celsius

Sequence:AAWFPPX

Target:neurokinin NK2 receptor

Application:GR 94800 is a synthetic peptide known for its role as a selective antagonist of neurokinin NK2 receptors. This peptide is particularly valuable in research focused on the modulation of neurokinin-mediated responses, including those related to smooth muscle contraction, pain perception, and inflammatory processes. GR 94800 is essential for exploring the therapeutic potential of targeting NK2 receptors in conditions such as asthma, irritable bowel syndrome, and certain pain disorders. With its high purity and consistent activity, GR 94800 ensures reliable and reproducible results, making it a critical tool in neuropharmacological and physiological studies.

Current Research:

GR 94800 is a potent and selective antagonist of the tachykinin NK₂ receptor, exhibiting high affinity with a pKᵦ value of 9.6 for NK₂ receptors, while displaying significantly lower affinities for NK₁ and NK₃ receptors, with pKᵦ values of 6.4 and 6.0, respectively.

The compound's selectivity has been demonstrated in various studies. For instance, in isolated tissue assays, GR 94800 effectively inhibited NK₂ receptor-mediated responses without significantly affecting NK₁ or NK₃ receptor activities. This specificity makes GR 94800 a valuable tool for investigating the physiological and pathological roles of NK₂ receptors, particularly in smooth muscle contraction and inflammatory processes.

Despite its utility in research, GR 94800 has been withdrawn from commercial sale for unspecified reasons. Researchers interested in utilizing this compound may need to explore alternative sources or consider other NK₂ receptor antagonists with similar profiles.

In summary, GR 94800 has contributed significantly to the understanding of NK₂ receptor functions due to its high potency and selectivity. Its application has provided insights into the receptor's role in various physiological processes, although its current unavailability may necessitate the use of alternative compounds in future research endeavors.

Reference:

Alvarez‐Berdugo, D., Espin, F., Arenas, C., López, I., Clavé, P., & Gallego, D. (2015). Changes in the response to excitatory antagonists, agonists, and spasmolytic agents in circular colonic smooth muscle strips from patients with diverticulosis. Neurogastroenterology & Motility, 27(11), 1600-1612.