2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

Related Products

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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-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 (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)
  • HY-17012
    Dapitant
    Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation.
    Dapitant
  • HY-105215
    FK888
    		Antagonist
    FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration.
    FK888
  • HY-P3905
    [Glp5,Sar9] Substance P (5-11)
    [Glp5,Sar9] Substance P (5-11) is an analogue of Substance P (HY-P0201).
    [Glp5,Sar9] Substance P (5-11)
  • HY-14405
    Casopitant
    		Antagonist
    Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant
  • HY-P991323
    MEDI-1912
    		Inhibitor
    MEDI-1912 is a human monoclonal antibody (mAb) targeting NGF/bNGF. MEDI-1912 inhibits signaling through TrkA and p75 receptors. MEDI-1912 can be used in chronic pain research.
    MEDI-1912
  • HY-14405B
    (R)-Casopitant
    		98.60%
    (R)-Casopitant ((R)-GW679769) is the isomer of Casopitant (HY-14405). Casopitant is a NK(1)-receptor antagonist. Casopitant can be used for the research of chemotherapy-induced nausea and vomiting.
    (R)-Casopitant
  • HY-P1498
    Substance P, Free Acid
    		Control
    Substance P, Free Acid is a native substance P analog, but shows no biological activity of substance P.
    Substance P, Free Acid
  • HY-161835
    SR140333B
    		Inhibitor
    SR140333B is a selective NK1 receptor inhibitor that can reduce LPS-induced fever and mitigate LPS (HY-D1056)-induced changes in brain tissue in rats.
    SR140333B
  • HY-118463
    Benzomalvin A
    Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively.
    Benzomalvin A
  • HY-P3927
    [MePhe8,Sar9] Substance P
    [MePhe8,Sar9] Substance P ([MePhe8-MeGly9] Substance P) is an analog of Substance P (Substance P (HY-P0201)).Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [MePhe8,Sar9] Substance P
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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