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-123497
    R116031
    		Antagonist
    R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist with a Ki of 0.45 nM for human NK-1 receptor. R116031 inhibits Substance P (HY-P0201)-induced peripheral effects (skin reactions and plasma extravasation in guinea pigs) and a central effect (thumping in gerbils).R116031 labeled with 3H significantly accumulate in the striatum, olfactory tubercule, olfactory bulb and locus coeruleus in gerbils models. R116031 can be used as a positron emission tomography (PET) ligand for PET imaging.
    R116031
  • HY-P2603
    Bz-Dab(NBD)-AwFpP-Nle-NH2
    		Antagonist
    Bz-Dab(NBD)-AwFpP-Nle-NH2 (Compound 5B) is a potent fluorescent antagonist of NK2 receptor, with a pKi of 8.87 nM (Ex=340 nm, Em=505 nm).
    Bz-Dab(NBD)-AwFpP-Nle-NH2
  • HY-P11429
    [Asp5,6,Me-Phe8] Substance P (5-11)
    		Agonist
    [Asp5,6,Me-Phe8] Substance P (5-11) is a tachykinin NK-3 receptor agonist. [Asp5,6,Me-Phe8] Substance P (5-11) reduces alcohol intake in genetically selected alcohol-preferring rats.
    [Asp5,6,Me-Phe8] Substance P (5-11)
  • HY-P2436
    L-659837
    		Antagonist
    L-659837 is a NK2 receptor antagonist, and can antagonize GR 64349 (HY-P1278)-induced contraction. L-659837 can be used for study of urinary bladder disorders.
    L-659837
  • HY-105334A
    Dilopetine citrate
    Dilopetine citrate is an inhibitor of substance P release. Dilopetine citrate dose-dependently reduces the vocalizing of isolated guinea pig pups. Dilopetine citrate shows good activity as an antidepressant.
    Dilopetine citrate
  • HY-129931
    Phenylalanylphenylalanylamide
    Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) is a ligand for the substance P 1–7 (SP1-7) binding site with a Ki value of 1.5 nM. Phenylalanylphenylalanylamide exerts significant anti-allodynic and anti-hyperalgesic effects in animal models of neuropathic pain following central administratio. Phenylalanylphenylalanylamide shows no distinct effect after peripheral (intraperitoneal) administration. Phenylalanylphenylalanylamide can be used for research on pain-related diseases.
    Phenylalanylphenylalanylamide
  • HY-129423
    Telmapitant
    		Antagonist
    Telmapitant is an orally active NK1R antagonist. Telmapitant has antiemetic effect and can be used for the research of delayed onset emesis.
    Telmapitant
  • HY-12142S
    rac-Vofopitant-d3
    		Antagonist
    rac-Vofopitant-d3 (rac-GR 205171-d3) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting.
    rac-Vofopitant-d<sub>3</sub>
  • HY-120167
    YM-44778
    		Antagonist
    YM-44778 is a neurokinin receptor antagonist. The pKi values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats.
    YM-44778
  • HY-P3880
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
    		Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P is a neuropeptide Substance P (HY-P0201) antagonist.
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
  • HY-P3808
    [D-Pro2,D-Trp7,9] Substance P
    		Antagonist
    [D-Pro2,D-Trp7,9] Substance P, a Substance P (HY-P0201) analogue, is a weak agonist and a potent, specific, competitive Substance P antagonist.
    [D-Pro2,D-Trp7,9] Substance P
  • HY-W370556
    (Rac)-LM11A-31
    		Control
    (Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist.
    (Rac)-LM11A-31
  • HY-180376
    TAC 363
    		Antagonist
    TAC 363 is a selective tachykinin NK-2 receptor antagonist. TAC 363 shows a rightward shift in the contractile response curve induced by Neurokinin A (HY-P0197) with a pA2 of 9.82. TAC 363 has a weak antagonistic effect on NK-1 receptors. TAC 363 can inhibit Neurokinin A-induced bronchoconstriction in guinea pigs with an ED50 of 0.3 mg/kg. TAC 363 can be used for the research of bronchial asthma.
    TAC 363
  • HY-121164
    GSK172981
    		Antagonist
    GSK172981 is a brain-penetrant tachykinin NK3 receptor antagonist with pKi values of 7.7 and 7.8 for human and native guinea pig NK3 receptors, respectively. GSK172981 can be used for the study of schizophrenia.
    GSK172981
  • HY-P3848
    Tyr0-Neurokinin A
    		Agonist
    Tyr0-Neurokinin A is a neuropeptide belongs to tachykinin peptide family. Tyr0-Neurokinin A is an agonist of Tacr2. Tyr0-Neurokinin A can be used in the research of insulin resistance, obesity, diabetes.
    Tyr0-Neurokinin A
  • HY-W777166
    Aprepitant-13C2,d2 (Major)
    		Inhibitor
    Aprepitant-13C2,d2 (Major) (MK-0869-13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant-<sup>13</sup>C<sub>2</sub>,d<sub>2</sub> (Major)
  • HY-109171R
    Elinzanetant (Standard)
    		Antagonist
    Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women.
    Elinzanetant (Standard)
  • HY-N7312
    Ditryptophenaline
    		Inhibitor
    Ditryptophenaline ((-)-Ditryptophenaline) is a secondary metabolite. Ditryptophenaline can be isolated from Aspergillus flavus. Ditryptophenaline inhibits the Substance P receptor. Ditryptophenaline exhibits potential analgesic and anti-inflammatory activities.
    Ditryptophenaline
  • HY-N9554
    WIN-64821
    		Antagonist
    WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The Ki values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca2+ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research.
    WIN-64821
  • HY-177079S
    Dazodeunetant
    		Inhibitor
    Dazodeunetant (Example 56) is a nitrogen-containing fused ring derivative. Dazodeunetant is an inhibitor of neurokinin (NK). Dazodeunetant has an IC50 0f 75.99 nM against NK3R in HEK293-NK3 (IP1). Dazodeunetant can be studied in research for menopausal hot flashes.
    Dazodeunetant
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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