2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

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There are three main classes of neurokinin receptors: NK1R (the substance P preferring receptor), NK2R, and NK3R. These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family. The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R. These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops. Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger. Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein. The neurokinin receptors are expressed on many cell types and tissues.

Neurokinin Receptor Isoform Specific Products:

Neurokinin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-116958
    SCH 206272
    		Antagonist
    SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (Ki = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active.
    SCH 206272
  • HY-19670
    Befetupitant
    		Antagonist
    Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
    Befetupitant
  • HY-117216
    L-703606
    		Antagonist
    L-703606 is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
    L-703606
  • HY-106910R
    Saredutant (Standard)
    		Antagonist
    Saredutant (Standard) is the analytical standard of Saredutant. This product is intended for research and analytical applications. Saredutant is a selective NK2 receptor antagonist.
    Saredutant (Standard)
  • HY-P0061B
    Vapreotide diacetate
    		Antagonist
    Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide diacetate
  • HY-G0012S
    Monohydroxy Netupitant-d6
    		Agonist
    Monohydroxy Netupitant-d6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant.
    Monohydroxy Netupitant-d<sub>6</sub>
  • HY-159842
    Fosrolapitant
    		Antagonist
    Fosrolapitant is a neurokinin 1 (NK1) receptor antagonist.
    Fosrolapitant
  • HY-14407AR
    Fosaprepitant dimeglumine (Standard)
    		Antagonist
    Fosaprepitant (dimeglumine) (Standard) is the analytical standard of Fosaprepitant (dimeglumine). This product is intended for research and analytical applications. Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
    Fosaprepitant dimeglumine (Standard)
  • HY-G0012
    Netupitant metabolite Monohydroxy Netupitant
    		Agonist
    Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
    Netupitant metabolite Monohydroxy Netupitant
  • HY-118356
    WIN 62,577
    		Antagonist
    WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
    WIN 62,577
  • HY-14552A
    Talnetant hydrochloride
    		Antagonist
    Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies.
    Talnetant hydrochloride
  • HY-P0255
    Physalaemin
    Physalaemin, a non-mammalian tachykinin, binds selectively to neurokinin-1 (NK1) receptor with high affinity.
    Physalaemin
  • HY-P0250
    Kassinin
    Kassinin is a peptide derived from the Kassina frog. It belongs to tachykinin family of neuropeptides. It is secreted as a defense response, and is involved in neuropeptide signalling.
    Kassinin
  • HY-P0236
    Neurokinin A(4-10)
    		Agonist
    Neurokinin A (4-10) is a tachykinin NK2 receptor agonist.
    Neurokinin A(4-10)
  • HY-U00207
    MEN11467
    		Antagonist
    MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.
    MEN11467
  • HY-U00392
    Tachykinin angatonist 1
    		Antagonist
    Tachykinin angatonist 1 is a neurokinin receptor antagonist extracted from patent US5968923, compound example 32.
    Tachykinin angatonist 1
  • HY-U00320
    Neurokinin antagonist 1
    		Antagonist
    Neurokinin antagonist 1 is a Neurokinin antagonist extracted from patent WO1998045262A1.
    Neurokinin antagonist 1
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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