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

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

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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 Isoform Specific Products:

Neurokinin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P3802
    [D-Trp2,7,9] Substance P
    		Antagonist
    [D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with Ki values of 1 μM, 1.3 μM, and ~9 μM for NK-1, NK-2,and NK-3 receptor, respectively.
    [D-Trp2,7,9] Substance P
  • HY-P1277A
    GR 94800 TFA
    		Antagonist
    GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively.
    GR 94800 TFA
  • HY-N7312
    Ditryptophenaline
    		Inhibitor
    Ditryptophenaline ((-)-Ditryptophenaline) is the metabolites of Aspergillus flavus. Ditryptophenaline inhibits substance P receptor and has anti-inflammatory activity.
    Ditryptophenaline
  • HY-19456
    SSR-241586
    		Antagonist
    SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).
    SSR-241586
  • HY-P1017
    MDL 29913
    		Antagonist
    MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66.
    MDL 29913
  • HY-P3883
    [DAla4] Substance P (4-11)
    [DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (Eledoisin (HY-P0006)) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes.
    [DAla4] Substance P (4-11)
  • HY-P3888
    Gly-Leu-Met-NH2
    Gly-Leu-Met-NH2 is a C-terminal tripeptide of Substance P (Substance P (HY-P0201)). Substance P is a neuropeptide.
    Gly-Leu-Met-NH2
  • 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.
    Men 10376
  • HY-P3092
    Phyllomedusin
    		Agonist
    Phyllomedusin, an tachykinin decapeptide, is a NK1 receptor agonist. Phyllomedusin has vasodilating activity and provokes the contraction of the pylorus.
    Phyllomedusin
  • HY-105137
    Lanepitant dihydrochloride
    		Antagonist
    Lanepitant dihydrochloride (LY303870 dihydrochloride) is a non-peptide neurokinin-1 receptor antagonist. Lanepitant dihydrochloride has analgesic and anti-inflammatory activities.
    Lanepitant dihydrochloride
  • HY-P3805
    [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)
    		Antagonist
    [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent neurokinin NK1 antagonist. [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) inhibits the effects of gold-protein-substance P (GPSP) and substance P (SP).
    [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)
  • HY-14407AS
    Fosaprepitant-d4 dimeglumine
    		Antagonist
    Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). 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)[1].
    Fosaprepitant-d<sub>4</sub> dimeglumine
  • HY-10051
    GR203040
    		Antagonist
    GR203040 is an orally active NK1 receptor antagonist with a pKi of 10.3. GR203040 shows potent antiemetic activity.
    GR203040
  • HY-145250
    NK1 receptor antagonist 2
    		Antagonist
    NK1 receptor antagonist 2 is a NK1 receptor antagonist. NK1 receptor antagonist 2 can be used for the research of tinnitus and hearing loss.
    NK1 receptor antagonist 2
  • HY-P1278A
    GR 64349 TFA
    		Antagonist
    GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
    GR 64349 TFA
  • HY-109147
    Imnopitant
    		Antagonist
    Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .
    Imnopitant
  • HY-119095
    L-741671
    		Antagonist
    L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with Kis of 64 nM, 0.03 nM and 0.7 nM in rat, human and ferret, respectively.
    L-741671
  • HY-106982
    Ezlopitant
    		Antagonist
    Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research.
    Ezlopitant
  • HY-P3890
    Substance P (5-11)
    Substance P (5-11), the C-terminal heptapeptide of Substance P (Substance P (HY-P0201)), is a neuropeptide. Substance P (5-11) binds to NK-1 tachykinin receptor.
    Substance P (5-11)
  • HY-149358
    NK3R-IN-1
    		Inhibitor
    NK3R-IN-1 (compound 16x), a imidazolepiperazine derivative, is an orally active Neurokinin Receptor NK3R inhibitor. NK3R-IN-1 decreases blood luteinizing hormone levels in ovariectomy (OVX) model.
    NK3R-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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