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-107691
    GR 159897
    		Antagonist 99.60%
    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-P3849
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
    		Agonist 99.83%
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues.
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
  • HY-P2546
    Biotin-Substance P
    		Modulator 99.91%
    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-P0197A
    Neurokinin A TFA
    		99.57%
    Neurokinin A TFA (Substance K TFA), 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.
    Neurokinin A TFA
  • 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-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-P1192
    GR-73632
    		Agonist 99.93%
    GR-73632 is a novel tachykinin neurokinin 1 (NK-1) receptor agonist. GR-73632 acts directly on the peripheral terminals of primary sensory neurons through NK1 receptor which convey itch signals.
    GR-73632
  • HY-P1194
    Spantide I
    		Antagonist 99.72%
    Spantide I, 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
  • HY-P3890A
    Substance P (5-11) (TFA)
    Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (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-16732
    Tradipitant
    		Antagonist 99.66%
    Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.
    Tradipitant
  • HY-16436
    Rolapitant hydrochloride hydrate
    		Antagonist 98.25%
    Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
    Rolapitant hydrochloride hydrate
  • HY-117216B
    L-703606 oxalate hydrate
    		Antagonist 99.4%
    L-703606 oxalate hydrate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
    L-703606 oxalate hydrate
  • HY-18006
    NKP608
    		Antagonist 99.88%
    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.
    NKP608
  • HY-117088
    LM11A-31
    		Modulator
    LM11A-31, a non-peptide p75NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
    LM11A-31
  • HY-P1186
    Eledoisin Related Peptide
    		Activator 98.96%
    Eledoisin Related Peptide is a Substance P analog that excites neurons and triggers behavioral responses. Eledoisin Related Peptide is also a tachykinin receptor ligand.
    Eledoisin Related Peptide
  • 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-P3862
    [MePhe7]-Neurokinin B
    		Inhibitor 98.87%
    [MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R).
    [MePhe7]-Neurokinin B
  • 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-P1031
    [bAla8]-Neurokinin A(4-10)
    		Agonist
    [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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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