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-P3800
    [Glp5] Substance P (5-11)
    [Glp5] Substance P (5-11) is an octapeptide. [Glp5] Substance P (5-11) is one of the main substance P fragments in rat central nervous system (CNS). [Glp5] Substance P (5-11) locally modulates dopamine release in rat striatum.
    [Glp5] Substance P (5-11)
  • HY-10049
    CP 122721
    		Antagonist
    CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS).
    CP 122721
  • HY-108483
    RP 67580
    		Antagonist
    RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation.
    RP 67580
  • HY-P1279
    [Lys5,MeLeu9,Nle10]-NKA(4-10)
    		Agonist
    [Lys5,MeLeu9,Nle10]-NKA(4-10) is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.
    [Lys5,MeLeu9,Nle10]-NKA(4-10)
  • HY-14770
    Ibodutant
    		Antagonist
    Ibodutant (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
    Ibodutant
  • HY-125304
    L 363851
    		Agonist
    L 363851 is a Neurokinin 2 receptor agonist, and induces the contractile response of tracheal smooth muscle devoid of epithelium (IC50 of 3.2 nM) and phosphoinositide hydrolysis (IC50 of 36 μM).
    L 363851
  • HY-P3891
    Substance P (4-11)
    Substance P (4-11), the C-terminus fragment of Substance P (HY-P0201), is a Substance P agonist that shows highly selective for NK1 receptors.
    Substance P (4-11)
  • HY-19665
    Lanepitant
    		Antagonist
    Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis.
    Lanepitant
  • HY-P3809
    [D-Pro2,D-Phe7,D-Trp9] Substance P
    [D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly.
    [D-Pro2,D-Phe7,D-Trp9] Substance P
  • HY-P1379
    C14TKL-1
    		Agonist
    C14TKL-1 is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).
    C14TKL-1
  • HY-105534
    TAK-637
    		Antagonist
    TAK-637 is an orally active neurokinin-1 receptor antagonist. TAK-637 increases bladder storage capacity. TAK-637 can be used for research of functional bowel diseases such as irritable bowel syndrome.
    TAK-637
  • HY-116822
    SSR 146977
    		Antagonist
    SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM.
    SSR 146977
  • HY-14751A
    Rolapitant hydrochloride
    		Antagonist
    Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model.
    Rolapitant hydrochloride
  • HY-P3852
    Neurokinin Receptor (393-407), rat
    Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation.
    Neurokinin Receptor (393-407), rat
  • HY-117216A
    L-703606 oxalate
    		Antagonist
    L-703606 oxalate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
    L-703606 oxalate
  • HY-P1379A
    C14TKL-1 acetate
    		Agonist
    C14TKL-1 acetate is the acetate salt form of C14TKL-1 (HY-P1379). C14TKL-1 acetate is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).
    C14TKL-1 acetate
  • HY-10052R
    Aprepitant (Standard)
    		Inhibitor
    Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant (Standard)
  • HY-10053S1
    Maropitant-13C,d3
    		Antagonist
    Maropitant-13C,d3 is the 13C- and 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-10049A
    CP 122721 hydrochloride
    		Antagonist
    CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects.
    CP 122721 hydrochloride
  • HY-P3885
    Substance P (alligator)
    		Modulator
    Substance P (alligator), a Substance P (HY-P0201) extracted from alligator, is a neuropeptide. The primary structure of Substance P (alligator) is: Arg-Pro-Arg-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
    Substance P (alligator)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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