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-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
    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-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-P1277
    GR 94800
    		Antagonist
    GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively.
    GR 94800
  • 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-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-131463
    ASN-1377642
    		Antagonist
    ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression.
    ASN-1377642
  • HY-120522
    L-659877
    		Antagonist
    L-659877 (Cyclo(Gln-Trp-Phe-Gly-Leu-Met)) is a compound used to study the chemical properties of peptide fragments in collision-induced dissociation. A series of experiments were conducted to study the structural changes of b-fragment ions of different lengths in collision-induced dissociation.
    L-659877
  • HY-157743
    SCH 60057
    		Inhibitor
    SCH 60057 (Compound 7) is a neurokinin (NK) receptor inhibitor that can be isolated from Acremonium sp., with IC50 values of 6 μM and 12 μM for NK1 and NK2, respectively.
    SCH 60057
  • HY-105436
    FR 113680
    		Antagonist
    FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.
    FR 113680
  • HY-P3225
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
    		Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation.
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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