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-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-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-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 (Substance P (HY-P0201)).Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [Gly11] Substance P
  • HY-117380
    SB 235375
    		Antagonist
    SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models.
    SB 235375
  • HY-P3925
    [His11]Substance P
    [His11]Substance P is an analog of Substance P (Substance P (HY-P0201)).Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [His11]Substance P
  • 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 (Substance P (HY-P0201)), is a Substance P agonist.
    [Sar4] Substance P (4-11)
  • 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-101704A
    Y1 receptor antagonist 1 formic
    		Antagonist 99.84%
    Y1 receptor antagonist 1 formic (H 409-22 isomer formic) is the formic salt form of Y1 receptor antagonist 1 (HY-101704). Y1 receptor antagonist 1 formic is a neuropeptide Y1 receptor antagonist.
    Y1 receptor antagonist 1 formic
  • HY-120167
    YM-44778
    		Antagonist
    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-P3851
    (β-Ala8)-Neurokinin A (4-10)
    		Agonist
    (β-Ala8)-Neurokinin A (4-10), a neuropeptide, is a potent and selective NK-2 tachykinin receptor (Neurokinin Receptor) agonist.
    (β-Ala8)-Neurokinin A (4-10)
  • HY-109171R
    Elinzanetant (Standard)
    		Antagonist
    Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can be used in vasomotor and schizophrenia studies.
    Elinzanetant (Standard)
  • HY-N7574
    WS9326A
    		Antagonist
    WS9326A is a tachykinin receptor antagonist that can be isolated from Streptomyces violaceus.
    WS9326A
  • HY-P10588
    WIN 66306
    		Antagonist
    WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both NK1 and NK2 receptors.
    WIN 66306
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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