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-P1277A
    GR 94800 TFA
    		Antagonist
    GR 94800 TFA 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 TFA
  • HY-N7312
    Ditryptophenaline
    		Inhibitor
    Ditryptophenaline ((-)-Ditryptophenaline) is the metabolites of Aspergillus flavus. Ditryptophenaline inhibits substance P receptor and has anti-inflammatory activity.
    Ditryptophenaline
  • HY-19456
    SSR-241586
    		Antagonist
    SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).
    SSR-241586
  • HY-B2078
    Eprazinone
    Eprazinone can enhance lung function and arterial oxygen levels and can be used in the study of chronic bronchitis. Higher doses of eprazinone increased phospholipid levels and decreased neutral lipid content in bronchoalveolar lavage (BAL) fluid, but had no effect on protein and cell levels in BAL. Eprazinone dose-dependently reduced short-circuit current (Isc), primarily by reducing chloride secretion at lower concentrations and affecting sodium and chloride transport at higher doses. Eprazinone may exert its anti-inflammatory effects by regulating BAL lipid composition and airway ion transport.
    Eprazinone
  • HY-12145
    CP-99994 hydrochloride
    		Inhibitor
    CP-99994 hydrochloride is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 hydrochloride prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 hydrochloride reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.
    CP-99994 hydrochloride
  • HY-P1017
    MDL 29913
    		Antagonist
    MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66.
    MDL 29913
  • HY-176546
    NK3R-IN-2
    		Inhibitor
    NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM for human NK3R. NK3R-IN-2 can pass through the blood-brain barrier. NK3R-IN-2 has excellent NK3R binding affinity (IC50 = 87.31 nM) in CHO-K1 cells. NK3R-IN-2 effectively inhibits the level of luteinizing hormone (LH). NK3R-IN-2 can be used for research on hormone related conditions.
    NK3R-IN-2
  • HY-P2052
    AWL 60
    		Antagonist
    AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
    AWL 60
  • HY-19182
    CJ-12255
    		Antagonist
    CJ-12255 is a selective NK1-R antagonist. CJ-12255 has no affinity for the NK-2 or NK-3 receptors. CJ-12255 blocks an substance P (SP)-induced chronic ulcerative colitis (CUC) in rats. CJ-12255 also reduces intraabdominal adhesion formation during abdominal surgery in rats.
    CJ-12255
  • HY-W755425
    Senktide TFA
    		Agonist
    Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC50=35 µM). Senktide TFA is promising for research of neurological disease.
    Senktide TFA
  • HY-10053S
    Maropitant-d3
    		Antagonist
    Maropitant-d3 is the 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.
    Maropitant-d<sub>3</sub>
  • HY-P10619
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11)
    		Antagonist
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11) is a tachykinin NK1 receptor antagonist that antagonizes Histamine (HY-B1204) induced hyperalgesia.
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11)
  • HY-P3883
    [DAla4] Substance P (4-11)
    [DAla4] Substance P (4-11) is an analog of Substance P (HY-P0201) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (HY-P0006) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes.
    [DAla4] Substance P (4-11)
  • HY-151413A
    MEN 10207 acetate
    		Antagonist
    MEN 10207 (acetate) is a selective antagonist of the NK-2 tachykinin receptor. MEN 10207 (acetate) induces tachykinin-induced contractions in rat bladder and guinea pig airways in vivo. MEN 10207 (acetate) inhibits [β-Ala 8 ]-NKA (4-10)-induced enhancement of bladder motility in anesthetized rats and [β-Ala 8 ]-NKA (4-10)-induced enhancement of bronchoconstriction in anesthetized guinea pigs.
    MEN 10207 acetate
  • HY-122286
    SB 414240
    		Antagonist
    SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.
    SB 414240
  • HY-P1276
    Men 10376
    		Antagonist
    Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
    Men 10376
  • HY-P3092
    Phyllomedusin
    		Agonist
    Phyllomedusin, an tachykinin decapeptide, is a NK1 receptor agonist. Phyllomedusin has vasodilating activity and provokes the contraction of the pylorus.
    Phyllomedusin
  • HY-105137
    Lanepitant dihydrochloride
    		Antagonist
    Lanepitant dihydrochloride (LY303870 dihydrochloride) is a non-peptide neurokinin-1 receptor antagonist. Lanepitant dihydrochloride has analgesic and anti-inflammatory activities.
    Lanepitant dihydrochloride
  • HY-P3805
    [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)
    		Antagonist
    [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent neurokinin NK1 antagonist. [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) inhibits the effects of gold-protein-substance P (GPSP) and substance P (SP).
    [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)
  • HY-P10268
    Neuropeptide K (human, porcine, rat)
    Neuropeptide K, human, porcine, rat exhibits bioactivity in gallbladder contraction, protein extravasation, hypotension and brcnchial smooth muscle spasm. Neuropeptide K, human, porcine, rat is concentrated in brain and acts as tachykinin neuromessenger.
    Neuropeptide K (human, porcine, rat)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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