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-P0201
    Substance P
    		Modulator 99.82%
    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).
    Substance P
  • HY-10052
    Aprepitant
    		Inhibitor 99.91%
    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant
  • HY-P0187
    Senktide
    		Agonist 99.72%
    Senktide is a tachykinin NK3 receptor agonist.
    Senktide
  • HY-19632
    Fezolinetant
    		Antagonist 99.19%
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
    Fezolinetant
  • HY-14407A
    Fosaprepitant dimeglumine
    		Antagonist 98.02%
    Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
    Fosaprepitant dimeglumine
  • 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-P10746
    EB1002
    		Agonist
    EB1002 is a selective NK2R agonist. EB1002 significantly raises the expression levels of mitochondrial biosynthesis-related genes (like PGC-1α) in obese mice, indicating that it promotes energy expenditure by boosting mitochondrial activity. EB1002 also increases the insulin sensitivity and improves glycolipid metabolism of the mice. EB1002 is promising for research of obesity and type 2 diabetes.
    EB1002
  • HY-P10599
    Scyliorhinin I
    		Agonist
    Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum.
    Scyliorhinin I
  • HY-16346
    Netupitant
    		Antagonist 99.93%
    Netupitant (CID-6451149) is a highly potent, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect.
    Netupitant
  • HY-14751
    Rolapitant
    		Antagonist 99.22%
    Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model.
    Rolapitant
  • HY-109171
    Elinzanetant
    		Antagonist 99.82%
    Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can improve vascular dilation and schizophrenia, and reduce levels of estradiol and progesterone.
    Elinzanetant
  • HY-106910
    Saredutant
    		Antagonist 98.09%
    Saredutant is a selective NK2 receptor antagonist.
    Saredutant
  • HY-P0197
    Neurokinin A
    		99.68%
    Neurokinin A (Substance K), 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
  • HY-15722
    SB-222200
    		Antagonist 99.85%
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.
    SB-222200
  • 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-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-20167A
    H-Glu(OtBu)-OtBu hydrochloride
    		≥98.0%
    H-Glu(OtBu)-OtBu hydrochloride is a glutamate derivative that can be used for substance P antagonist synthesis.
    H-Glu(OtBu)-OtBu hydrochloride
  • HY-10053
    Maropitant
    		Antagonist 99.52%
    Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.
    Maropitant
  • HY-14405A
    Casopitant mesylate
    		Antagonist 99.84%
    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. 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 98.08%
    Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.
    Osanetant
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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