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-P1276A
    Men 10376 TFA
    		Antagonist 98.95%
    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 99.69%
    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-P0006
    Eledoisin
    		99.05%
    Eledoisin (Eledone peptide) is a specific agonist of NK2 and NK3 receptors.
    Eledoisin
  • HY-107691
    GR 159897
    		Antagonist 99.60%
    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
    GR 159897
  • HY-P3890A
    Substance P (5-11) (TFA)
    Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (Substance P (HY-P0201)), is a neuropeptide. Substance P (5-11) TFA TFA binds to NK-1 tachykinin receptor.
    Substance P (5-11) (TFA)
  • HY-16732
    Tradipitant
    		Antagonist 99.66%
    Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.
    Tradipitant
  • HY-B2078A
    Eprazinone dihydrochloride
    		Inhibitor ≥98.0%
    Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.
    Eprazinone dihydrochloride
  • HY-117216B
    L-703606 oxalate hydrate
    		Antagonist 99.4%
    L-703606 oxalate hydrate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
    L-703606 oxalate hydrate
  • HY-18006
    NKP608
    		Antagonist 99.88%
    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.
    NKP608
  • 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-P1492
    Substance P (7-11)
    		98.47%
    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-P1192
    GR-73632
    		Agonist 99.93%
    GR-73632 is a novel tachykinin neurokinin 1 (NK-1) receptor agonist. GR-73632 acts directly on the peripheral terminals of primary sensory neurons through NK1 receptor which convey itch signals.
    GR-73632
  • HY-P3862
    [MePhe7]-Neurokinin B
    		Inhibitor 98.87%
    [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
  • HY-P1194B
    [D-Pro2] Spantide I TFA
    		99.15%
    [D-Pro2] Spantide I TFA is a Spantide analog. Spantide I is a selective NK1 receptor antagonist.
    [D-Pro2] Spantide I TFA
  • 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-16436
    Rolapitant hydrochloride hydrate
    		Antagonist 98.25%
    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-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-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-14407
    Fosaprepitant
    		Antagonist
    Fosaprepitant (L-785298) is a proagent of Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
    Fosaprepitant
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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