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 (149):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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).
    Substance P
  • HY-10052
    Aprepitant
    Inhibitor 99.91%
    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant
  • HY-P0187
    Senktide
    Agonist 99.59%
    Senktide is a tachykinin NK3 receptor agonist.
    Senktide
  • HY-19632
    Fezolinetant
    Antagonist 98.64%
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
    Fezolinetant
  • 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.
    Netupitant
  • HY-P3890A
    Substance P (5-11) (TFA)
    Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (Substance P (HY-P0201)), is a neuropeptide. Substance P (5-11) TFA TFA binds to NK-1 tachykinin receptor.
    Substance P (5-11) (TFA)
  • HY-135108
    QWF Peptide
    Antagonist
    QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM.
    QWF Peptide
  • HY-N7312
    Ditryptophenaline
    Inhibitor
    Ditryptophenaline ((-)-Ditryptophenaline) is the metabolites of Aspergillus flavus. Ditryptophenaline inhibits substance P receptor and has anti-inflammatory activity.
    Ditryptophenaline
  • HY-14407A
    Fosaprepitant dimeglumine
    Antagonist 98.02%
    Fosaprepitant dimeglumine (MK-0517) is a proagent 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).
    Fosaprepitant dimeglumine
  • 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.
    SB-222200
  • HY-101249
    L-732138
    Antagonist 99.75%
    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.
    L-732138
  • 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.
    Rolapitant
  • HY-14552
    Talnetant
    Antagonist 99.48%
    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.
    Talnetant
  • HY-106910
    Saredutant
    Antagonist 98.02%
    Saredutant is a selective NK2 receptor antagonist.
    Saredutant
  • HY-10053
    Maropitant
    Antagonist 99.52%
    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
  • HY-14405A
    Casopitant mesylate
    Antagonist 99.84%
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant mesylate
  • 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.
    Vofopitant dihydrochloride
  • HY-P0197A
    Neurokinin A TFA
    99.84%
    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.
    Neurokinin A TFA
  • HY-109171
    Elinzanetant
    Antagonist 98.36%
    Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can be used in vasomotor and schizophrenia studies.
    Elinzanetant
  • HY-14432
    Pavinetant
    Antagonist 99.83%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant