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-P1738
    [Sar9] Substance P
    		Agonist 98.14%
    [Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.
    [Sar9] Substance P
  • 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-U00382
    Substance P Receptor Antagonist 1
    		Antagonist 99.42%
    Substance P Receptor Antagonist 1 has the potential function in central nervous system disorders, respiratory, inflammatory diseases and gastrointestinal disorders.
    Substance P Receptor Antagonist 1
  • HY-12142
    Vofopitant
    		Antagonist 99.82%
    Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
    Vofopitant
  • HY-P3889
    Substance P (6-11)
    Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (HY-P0201). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect.
    Substance P (6-11)
  • HY-P3861
    Biotin-NeurokininA
    Biotin-NeurokininA is a biotinylated Neurokinin A (HY-P0197). Neurokinin A (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues.
    Biotin-NeurokininA
  • HY-P3598
    Substance P(1-4)
    		Antagonist
    Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation.
    Substance P(1-4)
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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