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

Neurokinin Receptor

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 Related Products (68):

Cat. No. Product Name Effect Purity
  • HY-P0201
    Substance P Modulator 99.60%
    Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-10052
    Aprepitant Inhibitor 99.93%
    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
  • HY-P0201A
    Substance P TFA Modulator 99.60%
    Substance P TFA (Neurokinin P TFA) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-P0187
    Senktide Agonist 99.14%
    Senktide is a tachykinin NK3 receptor agonist.
  • HY-14751
    Rolapitant Antagonist 98.43%
    Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
  • 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.
  • 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.
  • HY-19632
    Fezolinetant Antagonist 98.29%
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  • HY-16346
    Netupitant Antagonist 99.93%
    Netupitant (CID-6451149) is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.
  • HY-15722
    SB-222200 Antagonist 99.85%
    SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.
  • HY-P0197
    Neurokinin A
    Neurokinin A acts via neurokinin 2 (NK-2) receptor.
  • HY-14432
    Pavinetant Antagonist 99.74%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  • HY-14552
    Talnetant Antagonist 99.43%
    Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  • HY-14407A
    Fosaprepitant dimeglumine Antagonist >99.0%
    Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
  • HY-10053
    Maropitant Antagonist 99.00%
    Maropitant is a neurokinin (NK1) receptor antagonist.
  • HY-P0061
    Vapreotide Antagonist 98.83%
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
  • HY-18006
    NKP608 Antagonist 99.38%
    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=2.6 nM) and in vivo.
  • HY-P0242A
    Neurokinin B TFA Agonist
    Neurokinin B TFA belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
  • 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.
  • HY-P1012
    [Sar9,Met(O2)11]-Substance P Agonist 98.45%
    [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
Isoform Specific Products

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