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 (81):

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 ≥98.0%
    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
  • HY-19632
    Fezolinetant
    Antagonist 98.16%
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  • 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-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-109171
    Elinzanetant
    Antagonist 98.04%
    Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia.
  • HY-109147
    Imnopitant
    Antagonist
    Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .
  • HY-107692
    SB 218795
    Antagonist
    SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.
  • 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-14432
    Pavinetant
    Antagonist 99.78%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  • HY-106910
    Saredutant
    Antagonist 99.30%
    Saredutant is a selective NK2 receptor 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-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-P0061
    Vapreotide
    Antagonist 98.83%
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
  • 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-10053
    Maropitant
    Antagonist ≥98.0%
    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-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-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-101249
    L-732138
    Antagonist ≥99.0%
    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.
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