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-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)
  • HY-116620
    Benzomalvin C
    Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/mL in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It is isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
    Benzomalvin C
  • HY-P3853
    GR 87389
    		Inhibitor
    GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra.
    GR 87389
  • HY-P2603
    Bz-Dab(NBD)-AwFpP-Nle-NH2
    		Antagonist
    Bz-Dab(NBD)-AwFpP-Nle-NH2 (Compound 5B) is a potent fluorescent antagonist of NK2 receptor, with a pKi of 8.87 nM (Ex=340 nm, Em=505 nm).
    Bz-Dab(NBD)-AwFpP-Nle-NH2
  • HY-101704A
    Y1 receptor antagonist 1 formic
    		Antagonist 99.84%
    Y1 receptor antagonist 1 (H 409-22 isomer) formic (Example 4) is a neuropeptide Y1 receptor antagonist. Y1 receptor antagonist 1 can be used for the study of cardiovascular diseases, such as vasoconstriction.
    Y1 receptor antagonist 1 formic
  • HY-P2436
    L-659837
    		Antagonist
    L-659837 is a NK2 receptor antagonist, and can antagonize GR 64349 (HY-P1278)-induced contraction. L-659837 can be used for study of urinary bladder disorders.
    L-659837
  • HY-12142S
    rac-Vofopitant-d3
    		Antagonist
    rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142). Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
    rac-Vofopitant-d<sub>3</sub>
  • HY-120167
    YM-44778
    		Antagonist
    YM-44778 is a neurokinin receptor antagonist. The pKi values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats.
    YM-44778
  • HY-P3880
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
    		Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P is a neuropeptide Substance P (HY-P0201) antagonist.
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
  • HY-P3808
    [D-Pro2,D-Trp7,9] Substance P
    		Antagonist
    [D-Pro2,D-Trp7,9] Substance P, a Substance P (HY-P0201) analogue, is a weak agonist and a potent, specific, competitive Substance P antagonist.
    [D-Pro2,D-Trp7,9] Substance P
  • HY-W370556
    (Rac)-LM11A-31
    		Control
    (Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist.
    (Rac)-LM11A-31
  • HY-P3848
    Tyr0-Neurokinin A
    		Agonist
    Tyr0-Neurokinin A is a neuropeptide belongs to tachykinin peptide family. Tyr0-Neurokinin A is an agonist of Tacr2. Tyr0-Neurokinin A can be used in the research of insulin resistance, obesity, diabetes.
    Tyr0-Neurokinin A
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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