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 (59):

Cat. No. Product Name Effect Purity
  • HY-P0201
    Substance P Modulator 98.07%
    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-19632
    Fezolinetant Antagonist 98.29%
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  • HY-P0187
    Senktide Agonist 99.56%
    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-14405A
    Casopitant mesylate Antagonist
    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).
  • HY-14551
    Osanetant Antagonist >98.0%
    Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.
  • 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.
  • HY-15722
    SB-222200 Antagonist 99.91%
    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-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-P0197
    Neurokinin A 98.92%
    Neurokinin A acts via neurokinin 2 (NK-2) receptor.
  • 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-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-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-P1012
    [Sar9,Met(O2)11]-Substance P Agonist 98.45%
    [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
  • 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-P1485A
    Substance P (1-7)(TFA) 99.20%
    Substance P (1-7)(TFA) is a fragment of the neuropeptide, substance P (SP). Substance P (1-7)(TFA) gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
  • HY-P1276A
    Men 10376 TFA Antagonist 99.76%
    Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
Isoform Specific Products

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.