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-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-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-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-14406A
    L-733060 hydrochloride
    		Antagonist 99.30%
    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-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-10053
    Maropitant
    		Antagonist 99.52%
    Maropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.
    Maropitant
  • 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-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-P0061
    Vapreotide
    		Antagonist 99.87%
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide
  • HY-14432
    Pavinetant
    		Antagonist 99.83%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant
  • 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-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
  • HY-P0006
    Eledoisin
    		99.05%
    Eledoisin (Eledone peptide) is a specific agonist of NK2 and NK3 receptors.
    Eledoisin
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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