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-117088
    LM11A-31
    		Modulator 99.88%
    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-135108
    QWF Peptide
    		Antagonist 98.51%
    QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM.
    QWF Peptide
  • HY-P1192
    GR-73632
    		Agonist 99.89%
    GR-73632 is a tachykinin NK1 receptor agonist. GR-73632 activates spinal NK1 receptors to induce scratching, biting and licking behaviors. GR-73632 activates peripheral NK1 receptors to trigger lacrimation in guinea pigs, and activates central NK1 receptors to induce repetitive hind paw tapping behavior in gerbils. GR-73632 is applicable to research related to pruritus.
    GR-73632
  • HY-101249
    L-732138
    		Antagonist 99.9%
    L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action.
    L-732138
  • HY-B1392
    Esmolol hydrochloride
    		Agonist 99.69%
    Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol hydrochloride attenuates post resuscitation myocardial dysfunction. Esmolol hydrochloride improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
    Esmolol hydrochloride
  • HY-P0201A
    Substance P TFA
    		Modulator 99.34%
    Substance P TFA (Neurokinin P TFA) is a CNS-penetrant 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).
    Substance P TFA
  • HY-14432
    Pavinetant
    		Antagonist 99.63%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant
  • HY-14552
    Talnetant
    		Antagonist 99.38%
    Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.
    Talnetant
  • HY-14551
    Osanetant
    		Antagonist 98.19%
    Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.
    Osanetant
  • HY-122347A
    Orvepitant maleate
    		Antagonist 99.99%
    Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.
    Orvepitant maleate
  • HY-B2078A
    Eprazinone dihydrochloride
    		Inhibitor 99.05%
    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-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-P0197A
    Neurokinin A TFA
    		99.56%
    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-P0061
    Vapreotide
    		Antagonist 99.72%
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide
  • HY-P1722
    Spantide II
    		Antagonist 99.47%
    Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis.
    Spantide II
  • HY-P0242
    Neurokinin B
    		Agonist 98.48%
    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-P2546
    Biotin-Substance P
    		Modulator 99.66%
    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-P0236A
    Neurokinin A(4-10) TFA
    		Agonist 98.05%
    Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist.
    Neurokinin A(4-10) TFA
  • 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-14405A
    Casopitant mesylate
    		Antagonist 99.83%
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant mesylate
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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