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-119552
    Acetylaszonalenin
    		Inhibitor
    Acetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent neurokinin-1 (NK1) receptor antagonist. Acetylaszonalenin shows inhibition of [3H]-SP binding to human astrocytoma cells with a Ki of 170 μM.
    Acetylaszonalenin
  • HY-P3896
    Substance P (2-11)
    Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers.
    Substance P (2-11)
  • HY-116268
    GSK256471
    		Inhibitor
    GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.
    GSK256471
  • HY-P3886
    Substance P-Gly-Lys-Arg
    Substance P-Gly-Lys-Arg, also known as β-Preprotachykinin (58-71), is an analog of Substance P (HY-P0201).
    Substance P-Gly-Lys-Arg
  • HY-P3881
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P
    		Antagonist
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK1 receptor antagonist.
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P
  • HY-117670
    PD-161182
    		Antagonist
    PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases.
    PD-161182
  • HY-131463
    ASN-1377642
    		Antagonist
    ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression.
    ASN-1377642
  • HY-120522
    L-659877
    		Antagonist
    L-659877 (Cyclo(Gln-Trp-Phe-Gly-Leu-Met)) is a compound used to study the chemical properties of peptide fragments in collision-induced dissociation. A series of experiments were conducted to study the structural changes of b-fragment ions of different lengths in collision-induced dissociation.
    L-659877
  • HY-157743
    SCH 60057
    		Inhibitor
    SCH 60057 (Compound 7) is a neurokinin (NK) receptor inhibitor that can be isolated from Acremonium sp., with IC50 values of 6 μM and 12 μM for NK1 and NK2, respectively.
    SCH 60057
  • HY-105436
    FR 113680
    		Antagonist
    FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.
    FR 113680
  • HY-P3225
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
    		Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation.
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
  • HY-P3850
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B
    		Antagonist
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B shows no influence on Substance P or Neurokinin A.
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B
  • HY-P3895
    Substance P (3-11)
    Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guinea pig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
    Substance P (3-11)
  • HY-P2475
    [Pro9]-Substance P
    		Agonist
    [Pro9]-Substance P is a potent, reversible and selective agonist of NK-1 tachykinin receptors with an EC50 of 0.93 nM.
    [Pro9]-Substance P
  • HY-P1279A
    [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA
    		Agonist
    [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.
    [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA
  • HY-P3799
    [Glp6] Substance P (6-11)
    [Glp6] Substance P (6-11) is an analogue of substance P (6-11). Substance P (6-11) stimulates [3H]-inositol monophosphate ([3H]-IP1) formation in rat urinary bladder by acting on the 'septide-sensitive' tachykinin receptors.
    [Glp6] Substance P (6-11)
  • HY-109147A
    Imnopitant dihydrochloride
    		Antagonist
    Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist.
    Imnopitant dihydrochloride
  • HY-P3922
    [Gly11] Substance P
    [Gly11] Substance P is an analog of Substance P (HY-P0201). Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [Gly11] Substance P
  • HY-12144
    CP-99994
    		Antagonist
    CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.
    CP-99994
  • HY-P3932
    [Sar4] Substance P (4-11)
    [Sar4] Substance P (4-11) is an analog of Substance P (4-11). Substance P (4-11), the C-terminus fragment of Substance P (HY-P0201), is a Substance P agonist.
    [Sar4] Substance P (4-11)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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