Signaling Pathway

Neurokinin Receptor

Neurokinin Receptor

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Tachykinins are a family of neuropeptides that share the same hydrophobic C-terminal region with the amino acid sequence Phe-X-Gly-Leu-Met-NH2, where X represents a hydrophobic residue that is either an aromatic or a beta-branched aliphatic. The N-terminal region varies between different tachykinins. The term tachykinin originates in the rapid onset of action caused by the peptides in smooth muscles. SP is the most researched and potent member of the tachykinin family. SP binds to all three of the tachykinin receptors, but it binds most strongly to the NK1 receptor. Tachykinin NK1 receptor, often referred to as NK1 receptor, is a member of family 1 (rhodopsin-like) of G protein-coupled receptors and binds to the Gαq protein. The NK2 and NK3 receptors are also targets for novel classes of medications, and also show prominent antidepressive and anxiolytic effects.

Neurokinin Receptor Inhibitors & Modulators (11)

Product Name Catalog No. Brief Description
Aprepitant

HY-10052

Aprepitant is an antiemetic chemical compound that belongs to a class of drugs called substance P antagonists (SPA).

Fosaprepitant

HY-14407

Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.

Fosaprepitant dimeglumine

HY-14407A

Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.

Maropitant

HY-10053

Maropitant is a neurokinin (NK1) receptor antagonist.

Monohydroxy Netupitant D6

HY-G0012S

Monohydroxy Netupitant D6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant.

Netupitant

HY-16346

Netupitant(CID-6451149) is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.

Netupitant D6

HY-16346S

Netupitant D6 is the deuterium labeled Netupitant(CID-6451149), which is a highly potent and selective, orally active neurokinin-1 receptor antagonist.

NKP608

HY-18006

NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.

SB-222200

HY-15722

SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.

Talnetant

HY-14552

Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.

Talnetant hydrochloride

HY-14552A

Talnetant Hcl(SB 223412 Hcl) is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.