1. GPCR/G Protein
    Neuronal Signaling
  2. 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 (37):

Cat. No. Product Name Effect Purity
  • HY-10052
    Aprepitant Inhibitor
    Aprepitant is a specific NK-1R antagonist, used as an antiemetic agent.
  • HY-P0201
    Substance P Modulator
    Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-15722
    SB-222200 Antagonist
    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-14751
    Rolapitant Antagonist
    Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
  • HY-16346
    Netupitant Antagonist
    Netupitant (CID-6451149) is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.
  • HY-P1588
    Scyliorhinin II Agonist
    Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a Ki of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.
  • HY-P1276
    Men 10376 Antagonist
    Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
  • HY-P1506
    [Nle11]-Substance P Agonist
    [Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems.
  • HY-14407A
    Fosaprepitant dimeglumine Antagonist
    Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
  • HY-P1012
    [Sar9,Met(O2)11]-Substance P Agonist
    [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
  • HY-P0187
    Senktide Agonist
    Senktide is a tachykinin NK3 receptor agonist.
  • HY-18006
    NKP608 Antagonist
    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-10053
    Maropitant Antagonist
    Maropitant is a neurokinin (NK1) receptor antagonist.
  • HY-P1031
    [bAla8]-Neurokinin A(4-10) Agonist
    [bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist.
  • HY-19632
    Fezolinetant Antagonist
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  • HY-14432
    MLE-4901 Antagonist
    MLE-4901 is a neurokinin-3 receptor (NK3R) antagonist.
  • HY-16346S
    Netupitant D6 Antagonist
    Netupitant D6 is the deuterium labeled Netupitant(CID-6451149), which is a highly potent and selective, orally active neurokinin-1 receptor antagonist.
  • HY-P1485
    Substance P 1-7
    Substance P (7-11) is a fragment of the neuropeptide, substance P (SP). Substance P (7-11) gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
  • HY-14552
    Talnetant Antagonist
    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-14407
    Fosaprepitant Antagonist
    Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.