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

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

Related Products

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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-P1186
    Eledoisin Related Peptide
    		Activator 99.55%
    Eledoisin Related Peptide is a Substance P analog that excites neurons and triggers behavioral responses. Eledoisin Related Peptide is also a tachykinin receptor ligand.
    Eledoisin Related Peptide
  • HY-P1012
    [Sar9,Met(O2)11]-Substance P
    		Agonist 98.65%
    [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
    [Sar9,Met(O2)11]-Substance P
  • HY-P1194
    Spantide I
    		Antagonist 99.64%
    Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
    Spantide I
  • HY-16732
    Tradipitant
    		Antagonist 99.95%
    Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.
    Tradipitant
  • HY-10053
    Maropitant
    		Antagonist 99.39%
    Maropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.
    Maropitant
  • HY-P1485A
    Substance P(1-7) TFA
    		99.14%
    Substance P(1-7) TFA is a fragment of the neuropeptide, substance P (SP). Substance P(1-7) TFA gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
    Substance P(1-7) TFA
  • HY-P1492
    Substance P (7-11)
    		99.08%
    Substance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration.
    Substance P (7-11)
  • HY-P3849
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
    		Agonist 99.89%
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues.
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
  • HY-12143
    Vofopitant dihydrochloride
    		Antagonist 99.56%
    Vofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting.
    Vofopitant dihydrochloride
  • HY-P1278
    GR 64349
    		Agonist 99.12%
    GR 64349 is a potent and highly selective NK2 receptor peptide agonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
    GR 64349
  • HY-P0006
    Eledoisin
    		99.06%
    Eledoisin (Eledone peptide) is a specific agonist of NK2 and NK3 receptors.
    Eledoisin
  • HY-16436
    Rolapitant hydrochloride hydrate
    		Antagonist 98.36%
    Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
    Rolapitant hydrochloride hydrate
  • HY-P1030
    Hemokinin 1 (mouse)
    		Agonist 98.38%
    Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
    Hemokinin 1 (mouse)
  • HY-P0061A
    Vapreotide acetate
    		Antagonist 99.85%
    Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide acetate
  • HY-P1031
    [bAla8]-Neurokinin A(4-10)
    		Agonist
    [bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist.
    [bAla8]-Neurokinin A(4-10)
  • HY-18006
    NKP608
    		Antagonist 99.88%
    NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.
    NKP608
  • HY-P1276A
    Men 10376 TFA
    		Antagonist 99.67%
    Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
    Men 10376 TFA
  • HY-151413
    MEN 10207
    		Antagonist 99.80%
    MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
    MEN 10207
  • HY-P3862
    [MePhe7]-Neurokinin B
    		Inhibitor 98.76%
    [MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R).
    [MePhe7]-Neurokinin B
  • HY-133206A
    Fosnetupitant chloride monohydrochloride
    		Antagonist 99.70%
    Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant.
    Fosnetupitant chloride monohydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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