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-P1379A
    C14TKL-1 acetate
    		Agonist
    C14TKL-1 acetate is the acetate salt form of C14TKL-1 (HY-P1379). C14TKL-1 acetate is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).
    C14TKL-1 acetate
  • HY-10052R
    Aprepitant (Standard)
    		Inhibitor
    Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant (Standard)
  • HY-10053S1
    Maropitant-13C,d3
    		Antagonist
    Maropitant-13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
    Maropitant-<sup>13</sup>C,d<sub>3</sub>
  • HY-10049A
    CP 122721 hydrochloride
    		Antagonist
    CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects.
    CP 122721 hydrochloride
  • HY-P3885
    Substance P (alligator)
    		Modulator
    Substance P (alligator), a Substance P (Substance P (HY-P0201)) extracted from alligator, is a neuropeptide. The primary structure of Substance P (alligator) is: Arg-Pro-Arg-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
    Substance P (alligator)
  • HY-17012
    Dapitant
    Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation.
    Dapitant
  • HY-105215
    FK888
    		Antagonist
    FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration.
    FK888
  • HY-P3069
    γ-Neuropeptide (rabbit)
    		Agonist
    γ-Neuropeptide (rabbit) can be isolated from rabbit intestine. γ-Neuropeptide is an endogenous neurokinin peptide that acts as a neurokinin 2 (NK2) receptor agonist. γ-Neuropeptide mediates hypothalamic-pituitary-adrenal (HPA) axis, as well as reproductive hormone release.
    γ-Neuropeptide (rabbit)
  • 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-108481
    L-760735
    		Antagonist ≥99.0%
    L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects.
    L-760735
  • 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-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 (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-107692
    SB 218795
    		Antagonist 99.86%
    SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.
    SB 218795
  • 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 (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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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