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-17615
    Fosnetupitant
    		Inhibitor
    Fosnetupitant (Pronetupitant) a methylene phosphate proagent of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for human NK1 receptor.
    Fosnetupitant
  • HY-108482
    CP-96,345
    		Inhibitor ≥99.0%
    CP-96,345 is a specific, highly potent, and orally active tachykinin and substance P receptor non-peptide inhibitor. CP-96,345 prevents the drop in blood pressure evoked by substance P and neurokinin A. CP-96,345 can be used for researching neurogenic inflammation.
    CP-96,345
  • HY-P1485
    Substance P(1-7)
    Substance P(1-7) is a fragment of the neuropeptide, substance P (SP). Substance P(1-7) gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
    Substance P(1-7)
  • HY-101704
    Y1 receptor antagonist 1
    		Antagonist 99.69%
    Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist.
    Y1 receptor antagonist 1
  • HY-P1012A
    [Sar9,Met(O2)11]-Substance P TFA
    		Agonist 98.58%
    [Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK1 receptor selective agonist.
    [Sar9,Met(O2)11]-Substance P TFA
  • HY-16346S
    Netupitant-d6
    		Antagonist 99.56%
    Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].
    Netupitant-d<sub>6</sub>
  • HY-P1194A
    Spantide I TFA
    		Antagonist 99.32%
    Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
    Spantide I TFA
  • HY-108479
    Nolpitantium
    		Antagonist
    Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.
    Nolpitantium
  • HY-P3801
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
    		Modulator 99.01%
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats.
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
  • HY-P1278
    GR 64349
    		Antagonist 99.92%
    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
  • HY-P3069
    γ-Neuropeptide (rabbit)
    		Agonist 99.99%
    γ-Neuropeptide (rabbit) can be isolated from rabbit intestine. γ-Neuropeptide is an endogenous neurokinin peptide that acts as a neurokinin 2 (NK2) receptor agonist. γ-Neuropeptide mediates hypothalamic-pituitary-adrenal (HPA) axis, as well as reproductive hormone release.
    γ-Neuropeptide (rabbit)
  • HY-P2000
    Septide
    		Agonist 98.97%
    Septide ((Pyr6,Pro9)-Substance P) is a potent NK1 receptor agonist with a Kd value of 0.55 nM.
    Septide
  • HY-12114
    Serlopitant
    		Antagonist
    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
    Serlopitant
  • HY-108481
    L-760735
    		Antagonist ≥99.0%
    L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects.
    L-760735
  • HY-P0242
    Neurokinin B
    		Agonist
    Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
    Neurokinin B
  • HY-107692
    SB 218795
    		Antagonist 99.86%
    SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.
    SB 218795
  • HY-12142
    Vofopitant
    		Antagonist 99.82%
    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.
    Vofopitant
  • HY-P3889
    Substance P (6-11)
    Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (Substance P (HY-P0201)). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect.
    Substance P (6-11)
  • HY-P3861
    Biotin-NeurokininA
    Biotin-NeurokininA is a biotinylated NeurokininA (HY-P0197). Neurokinin A (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues.
    Biotin-NeurokininA
  • HY-P3598
    Substance P(1-4)
    		Antagonist
    Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation.
    Substance P(1-4)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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