2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

Related Products

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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-108483
    RP 67580
    		Antagonist 99.05%
    RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation.
    RP 67580
  • HY-P3801
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
    		Modulator 99.61%
    [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-P1494
    Substance P (1-9)
    		99.48%
    Substance P (1-9) is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder.
    Substance P (1-9)
  • HY-108482
    CP-96,345
    		Inhibitor 99.9%
    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-P3890A
    Substance P (5-11) TFA
    Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (HY-P0201), is a neuropeptide. Substance P (5-11) TFA TFA binds to NK-1 tachykinin receptor.
    Substance P (5-11) TFA
  • HY-12142
    Vofopitant
    		Antagonist 99.82%
    Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting.
    Vofopitant
  • HY-P1738
    [Sar9] Substance P
    		Agonist 98.14%
    [Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.
    [Sar9] Substance P
  • HY-P1198
    Hemokinin 1, human
    		Agonist 98.11%
    Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia.
    Hemokinin 1, human
  • HY-W017933
    Octahydroisoindole
    		Antagonist 99.09%
    Octahydroisoindole (Perhydroisoindole) is a substance P antagonist that can cross the blood-brain barrier and is useful for the study of movement disorders associated with central nervous system diseases.
    Octahydroisoindole
  • HY-14407
    Fosaprepitant
    		Antagonist
    Fosaprepitant (L-785298) is a proagent of Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
    Fosaprepitant
  • 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-P3895A
    Substance P (3-11) acetate
    Substance P (3-11) acetate is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) acetate has contracting activities on guinea pig ileum. Substance P (3-11) acetate also promotes human monocyte chemotaxis.
    Substance P (3-11) acetate
  • HY-P1194B
    [D-Pro2] Spantide I TFA
    		99.15%
    [D-Pro2] Spantide I TFA is a Spantide analog. Spantide I is a selective NK1 receptor antagonist.
    [D-Pro2] Spantide I TFA
  • 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) (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
  • 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-P3888
    Gly-Leu-Met-NH2
    		99.76%
    Gly-Leu-Met-NH2 is a C-terminal tripeptide of Substance P (HY-P0201). Substance P is a neuropeptide.
    Gly-Leu-Met-NH2
  • 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.
    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-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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