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-12143
    Vofopitant dihydrochloride
    		Antagonist 99.11%
    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-P0197A
    Neurokinin A TFA
    		99.84%
    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-P0242A
    Neurokinin B TFA
    		Agonist 98.59%
    Neurokinin B TFA 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 TFA
  • HY-P1485A
    Substance P(1-7) TFA
    		99.02%
    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-P0201A
    Substance P TFA
    		Modulator 99.79%
    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-14432
    Pavinetant
    		Antagonist 99.83%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant
  • 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-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-P1030
    Hemokinin 1 (mouse)
    		Agonist 99.30%
    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 98.95%
    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-P0236A
    Neurokinin A(4-10) TFA
    		Agonist 98.85%
    Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist.
    Neurokinin A(4-10) TFA
  • HY-18006
    NKP608
    		Antagonist 99.89%
    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-P0061
    Vapreotide
    		Antagonist 98.06%
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide
  • HY-P1012
    [Sar9,Met(O2)11]-Substance P
    		Agonist 98.84%
    [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
    [Sar9,Met(O2)11]-Substance P
  • HY-P1194
    Spantide I
    		Antagonist 99.85%
    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-P1494
    Substance P (1-9)
    		99.75%
    Substance P (1-9) is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder.
    Substance P (1-9)
  • 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-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)
Cat. No. Product Name / Synonyms Application Reactivity