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-135108
    QWF Peptide
    		Antagonist 98.15%
    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-B1392
    Esmolol hydrochloride
    		Agonist 99.92%
    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-14552
    Talnetant
    		Antagonist 99.48%
    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-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-P99143
    Anti-Mouse NK1.1 Antibody (PK136)
    		Inhibitor
    Anti-Mouse NK1.1 Antibody (PK136) is an anti-mouse NK1.1 IgG2a monoclonal antibody. Anti-Mouse NK1.1 Antibody (PK136) can deplete natural killer (NK) cells. Anti-Mouse NK1.1 Antibody (PK136) inhibits the JAK-STAT and NF-κB signaling pathways. Anti-Mouse NK1.1 Antibody (PK136) can be used for research on inflammation conditions such as non-alcoholic steatohepatitis (NASH).
    Anti-Mouse NK1.1 Antibody (PK136)
  • 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-10053
    Maropitant
    		Antagonist 99.52%
    Maropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.
    Maropitant
  • 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
  • HY-P0201A
    Substance P TFA
    		Modulator
    Substance P TFA (Neurokinin P TFA) 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).
    Substance P TFA
  • HY-P0236A
    Neurokinin A(4-10) TFA
    		Agonist 98.84%
    Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist.
    Neurokinin A(4-10) TFA
  • HY-P1492
    Substance P (7-11)
    		99.08%
    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-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-14432
    Pavinetant
    		Antagonist 99.83%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant
  • 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-P1485A
    Substance P(1-7) TFA
    		99.14%
    Substance P(1-7) TFA is a fragment of the neuropeptide, substance P (SP). Substance P(1-7) TFA gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
    Substance P(1-7) TFA
  • HY-P1012
    [Sar9,Met(O2)11]-Substance P
    		Agonist 99.60%
    [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
    [Sar9,Met(O2)11]-Substance P
  • HY-12143
    Vofopitant dihydrochloride
    		Antagonist 99.56%
    Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent.
    Vofopitant dihydrochloride
  • 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-P1030
    Hemokinin 1 (mouse)
    		Agonist 99.49%
    Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
    Hemokinin 1 (mouse)
  • HY-P1276A
    Men 10376 TFA
    		Antagonist 99.67%
    Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
    Men 10376 TFA
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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