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-108480
    SDZ NKT 343
    		Antagonist
    SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity.
    SDZ NKT 343
  • HY-P1186
    Eledoisin Related Peptide
    		Activator 98.96%
    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-P1198A
    Hemokinin 1, human TFA
    		Agonist
    Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia.
    Hemokinin 1, human TFA
  • HY-19633
    CS-003 Free base
    		Antagonist
    CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
    CS-003 Free base
  • HY-P4709
    (Trp7,β-Ala8)-Neurokinin A (4-10)
    		Antagonist
    (Trp7,β-Ala8)-Neurokinin A (4-10) is a potent neurokinin-3 (NK3) antagonist.
    (Trp7,β-Ala8)-Neurokinin A (4-10)
  • HY-P10599
    Scyliorhinin I
    		Agonist
    Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum.
    Scyliorhinin I
  • HY-114673
    Benzomalvin B
    		Inhibitor
    Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P.
    Benzomalvin B
  • HY-106659
    SCH 900978
    		Antagonist
    SCH 900978 (NK-1 Antagonist 1) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression.
    SCH 900978
  • HY-P3802
    [D-Trp2,7,9] Substance P
    		Antagonist
    [D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with Ki values of 1 μM, 1.3 μM, and ~9 μM for NK-1, NK-2,and NK-3 receptor, respectively.
    [D-Trp2,7,9] Substance P
  • 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-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-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-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 (Substance P (HY-P0201)) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (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-P3888
    Gly-Leu-Met-NH2
    Gly-Leu-Met-NH2 is a C-terminal tripeptide of Substance P (Substance P (HY-P0201)). Substance P is a neuropeptide.
    Gly-Leu-Met-NH2
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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