Date published: 2025-12-13

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NK-1R Inhibitors

NK-1R inhibitors, or Neurokinin-1 Receptor inhibitors, constitute a class of chemical compounds designed to modulate the activity of the NK-1 receptor in the human body. The NK-1 receptor is a G protein-coupled receptor (GPCR) primarily found in the central nervous system and peripheral tissues. Its primary endogenous ligand is substance P, a neuropeptide that plays a pivotal role in various physiological processes, including pain transmission, nausea, vomiting, and inflammation. NK-1R inhibitors are meticulously crafted molecules with diverse chemical structures and mechanisms of action, all aimed at influencing the functioning of this receptor. Within this chemical class, there are different subclasses of NK-1R inhibitors. Small molecules, for instance, typically work by competitively binding to the NK-1 receptor, thereby preventing substance P from interacting with its binding site on the receptor. Peptide-based inhibitors, on the other hand, often mimic the structure of substance P and compete for receptor binding. Monoclonal antibodies designed for NK-1R inhibition specifically target and neutralize the receptor. By obstructing the signaling pathway of the NK-1 receptor, these inhibitors can effectively regulate various physiological processes, though it's important to note that their practical applications extend beyond the scope of this description

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Netupitant

290297-26-6sc-478156
5 mg
$419.00
(0)

Netupitant is combined with palonosetron in a single capsule to form a drug called NEPA, which is used to prevent acute and delayed chemotherapy-induced nausea and vomiting.

Casopitant mesylate

414910-30-8sc-214670
sc-214670B
sc-214670A
1 mg
5 mg
10 mg
$255.00
$495.00
$705.00
1
(0)

Casopitant mesylate functions as a potent antagonist of the neurokinin-1 receptor (NK-1R), characterized by its ability to modulate receptor conformations through specific ligand-receptor interactions. Its unique molecular structure allows for high-affinity binding, influencing the receptor's activation state and subsequent intracellular signaling. The compound's dynamic binding kinetics provide insights into competitive inhibition and receptor desensitization, enhancing our understanding of neurokinin pathways.

Aprepitant

170729-80-3sc-207299
1 mg
$173.00
4
(1)

Aprepitant acts as a selective antagonist of the neurokinin-1 receptor (NK-1R), exhibiting a unique ability to disrupt neurokinin signaling through its specific binding affinity. Its structural features facilitate distinct interactions with the receptor, altering its conformational dynamics. This modulation impacts downstream signaling cascades, providing a deeper understanding of receptor behavior and the intricate balance of neuropeptide interactions within cellular environments.