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-P3905
    [Glp5,Sar9] Substance P (5-11)
    [Glp5,Sar9] Substance P (5-11) is an analogue of Substance P (HY-P0201).
    [Glp5,Sar9] Substance P (5-11)
  • HY-14405
    Casopitant
    		Antagonist
    Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant
  • HY-19429
    SLV-317 free base
    		Antagonist
    SLV-317 (free base) is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects.
    SLV-317 free base
  • HY-P991323
    MEDI-1912
    		Inhibitor
    MEDI-1912 is a human monoclonal antibody (mAb) targeting NGF/bNGF. MEDI-1912 inhibits signaling through TrkA and p75 receptors. MEDI-1912 can be used in chronic pain research.
    MEDI-1912
  • HY-P11075
    [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)
    		Agonist
    [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7  nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research.
    [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)
  • HY-14405B
    (R)-Casopitant
    		98.60%
    (R)-Casopitant ((R)-GW679769) is the isomer of Casopitant (HY-14405). Casopitant is a NK(1)-receptor antagonist. Casopitant can be used for the research of chemotherapy-induced nausea and vomiting.
    (R)-Casopitant
  • HY-P1498
    Substance P, Free Acid
    		Control 98.07%
    Substance P, Free Acid is a native substance P analog, but shows no biological activity of substance P.
    Substance P, Free Acid
  • HY-161835
    SR140333B
    		Inhibitor
    SR140333B is a selective NK1 receptor inhibitor that can reduce LPS-induced fever and mitigate LPS (HY-D1056)-induced changes in brain tissue in rats.
    SR140333B
  • HY-118463
    Benzomalvin A
    Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively.
    Benzomalvin A
  • HY-137462
    Leucyl-phenylalanine amide
    Leucyl-phenylalanine amide (L-Leucyl-L-phenylalaninamide) is a dipeptide analog. Leucyl-phenylalanine amide is a ligand of SP1-7 with a Ki value of 10.2 nM. Leucyl-phenylalanine amide shows no binding activity to human NK-1 or NK-3 receptors.
    Leucyl-phenylalanine amide
  • HY-10053A
    Maropitant citrate hydrate
    		Antagonist 99.19%
    Maropitant citrate hydrate is the citrate hydrate of Maropitant (HY-10053). Maropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.
    Maropitant citrate hydrate
  • HY-P3927
    [MePhe8,Sar9] Substance P
    [MePhe8,Sar9] Substance P ([MePhe8-MeGly9] Substance P) is an analog of Substance P (HY-P0201). Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [MePhe8,Sar9] Substance P
  • HY-120928
    S 16474
    		Antagonist
    S 16474 is a cyclic peptide with antagonistic effects on NK1 and NK2 receptors. S 16474 can be used in the study of neurogenic inflammation.
    S 16474
  • HY-119552
    Acetylaszonalenin
    		Inhibitor
    Acetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent neurokinin-1 (NK1) receptor antagonist. Acetylaszonalenin shows inhibition of [3H]-SP binding to human astrocytoma cells with a Ki of 170 μM.
    Acetylaszonalenin
  • HY-P3896
    Substance P (2-11)
    Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers.
    Substance P (2-11)
  • HY-19632S
    Fezolinetant-d4
    		Antagonist
    Fezolinetant-d4 (ESN-364-d4) is the deuterium labeled Fezolinetant (HY-19632). Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
    Fezolinetant-d<sub>4</sub>
  • HY-116268
    GSK256471
    		Inhibitor
    GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.
    GSK256471
  • HY-P3886
    Substance P-Gly-Lys-Arg
    Substance P-Gly-Lys-Arg, also known as β-Preprotachykinin (58-71), is an analog of Substance P (HY-P0201).
    Substance P-Gly-Lys-Arg
  • HY-P3881
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P
    		Antagonist
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK1 receptor antagonist.
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P
  • HY-117670
    PD-161182
    		Antagonist
    PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases.
    PD-161182
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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