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-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 99.59%
    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-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-P10619
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11)
    		Antagonist
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11) is a tachykinin NK1 receptor antagonist that antagonizes Histamine (HY-B1204) induced hyperalgesia.
    [Tyr6,D-Phe7,D-His9]-Substance P (6-11)
  • 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 98.65%
    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 98.02%
    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-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-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-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-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-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
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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