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-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-P1494
    Substance P (1-9)
    		98.47%
    Substance P (1-9) is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder.
    Substance P (1-9)
  • 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-117380
    SB 235375
    		Antagonist 98.13%
    SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models.
    SB 235375
  • HY-P3925
    [His11]Substance P
    		98.97%
    [His11]Substance P is an analog of Substance P (HY-P0201). Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [His11]Substance P
  • 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-105462
    MDL 105212A
    		Antagonist
    MDL 105212A is a potent and orally active nonpeptide neurokinin receptor (NK-1/NK-2) tachykinin receptor antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma.
    MDL 105212A
  • 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-P11312
    [S5K, F6Y, L9mL, M10Mox] neurokinin A (4–10)
    [S5K, F6Y, L9mL, M10Mox] neurokinin A (4–10) is a neuropeptide A analog and a peptide fragment of HY-P10746. [S5K, F6Y, L9mL, M10Mox] neurokinin A (4–10) is highly selective for mouse tachykinin receptors and human tachykinin receptor NK1R and has an in vivo half-life of 10.3 hours in mice.
    [S5K, F6Y, L9mL, M10Mox] neurokinin A (4–10)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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