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

Neurokinin Receptor

NK receptor; Tachykinin 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 (102):

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 99.67%
    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
  • HY-19632
    Fezolinetant
    Antagonist 98.64%
    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, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect.
  • HY-P0187
    Senktide
    Agonist 99.14%
    Senktide is a tachykinin NK3 receptor agonist.
  • HY-20167A
    H-Glu(OtBu)-OtBu hydrochloride
    ≥98.0%
    H-Glu(OtBu)-OtBu hydrochloride is a glutamate derivative that can be used for substance P antagonist synthesis.
  • 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.
  • HY-108482
    CP-96,345
    Inhibitor
    CP-96,345 is a specific, highly potent, and orally active tachykinin and substance P receptor non-peptide inhibitor. CP-96,345 prevents the drop in blood pressure evoked by substance P and neurokinin A. CP-96,345 can be used for researching neurogenic inflammation.
  • HY-14432
    Pavinetant
    Antagonist 99.78%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  • HY-P0197A
    Neurokinin A TFA
    99.25%
    Neurokinin A TFA (Substance K TFA), 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.
  • HY-106910
    Saredutant
    Antagonist 98.02%
    Saredutant is a selective NK2 receptor antagonist.
  • HY-14751
    Rolapitant
    Antagonist 98.65%
    Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model.
  • HY-14407A
    Fosaprepitant dimeglumine
    Antagonist 98.05%
    Fosaprepitant dimeglumine (MK-0517) is a prodrug of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
  • HY-15722
    SB-222200
    Antagonist 99.85%
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.
  • 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-14552
    Talnetant
    Antagonist 99.43%
    Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.
  • HY-10053
    Maropitant
    Antagonist 99.79%
    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.
  • HY-101249
    L-732138
    Antagonist 99.43%
    L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action.
  • HY-12143
    Vofopitant dihydrochloride
    Antagonist 99.11%
    Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent.
  • 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.