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-P10619
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11)
    		Antagonist
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11) is a tachykinin NK1 receptor antagonist that antagonizes Histamine (HY-B1204) induced hyperalgesia.
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11)
  • HY-181682
    NK3R antagonist-1
    		Antagonist
    NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes.
    NK3R antagonist-1
  • HY-P3883
    [DAla4] Substance P (4-11)
    [DAla4] Substance P (4-11) is an analog of Substance P (HY-P0201) that inhibits the binding of 125I-Bolton Hunter-conjugated 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-151413A
    MEN 10207 acetate
    		Antagonist
    MEN 10207 (acetate) is a selective antagonist of the NK-2 tachykinin receptor. MEN 10207 (acetate) induces tachykinin-induced contractions in rat bladder and guinea pig airways in vivo. MEN 10207 (acetate) inhibits [β-Ala 8 ]-NKA (4-10)-induced enhancement of bladder motility in anesthetized rats and [β-Ala 8 ]-NKA (4-10)-induced enhancement of bronchoconstriction in anesthetized guinea pigs.
    MEN 10207 acetate
  • HY-122286
    SB 414240
    		Antagonist
    SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.
    SB 414240
  • 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-P10268
    Neuropeptide K (human, porcine, rat)
    Neuropeptide K, human, porcine, rat exhibits bioactivity in gallbladder contraction, protein extravasation, hypotension and brcnchial smooth muscle spasm. Neuropeptide K, human, porcine, rat is concentrated in brain and acts as tachykinin neuromessenger.
    Neuropeptide K (human, porcine, rat)
  • 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).
    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
    		Agonist
    GR 64349 is a potent and highly selective NK2 receptor peptide agonist, 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 (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
  • HY-P3854
    GR 83074
    		Antagonist
    GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity.
    GR 83074
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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