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.

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-P1031
    [bAla8]-Neurokinin A(4-10)
    		Agonist 98.78%
    [bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist.
    [bAla8]-Neurokinin A(4-10)
  • 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-P1492
    Substance P (7-11)
    		98.47%
    Substance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration.
    Substance P (7-11)
  • HY-151413
    MEN 10207
    		Antagonist 99.69%
    MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
    MEN 10207
  • HY-P2546
    Biotin-Substance P
    		Modulator 98.70%
    Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
    Biotin-Substance P
  • HY-B2078A
    Eprazinone dihydrochloride
    		Inhibitor ≥98.0%
    Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.
    Eprazinone dihydrochloride
  • HY-P0061A
    Vapreotide acetate
    		Antagonist 99.67%
    Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide acetate
  • HY-133206A
    Fosnetupitant chloride monohydrochloride
    		Antagonist 99.70%
    Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant.
    Fosnetupitant chloride monohydrochloride
  • 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-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-107691
    GR 159897
    		Antagonist ≥99.0%
    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
    GR 159897
  • 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-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 >98.0%
    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-14406A
    L-733060 hydrochloride
    		Antagonist ≥99.0%
    L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent.
    L-733060 hydrochloride
  • HY-P3801
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
    		Modulator
    [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 99.45%
    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
Cat. No. Product Name / Synonyms Application Reactivity