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-120308
    (R)-Nolpitantium
    		Antagonist
    (R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.
    (R)-Nolpitantium
  • HY-12140
    Vestipitant
    		Antagonist
    Vestipitant (GW597599) is a neurokinin-1 receptor antagonist (pKi: 9.4, hNK1) with hypnotic effects and the ability to suppress primary insomnia. Vestipitant can effectively block substance P-mediated extracellular regulated kinase phosphorylation and relieve anxiety and possible depression induced by the agonist GR73632 (HY-P1192) in gerbils. Vestipitant can also improve functional dyspnea, anxiety, insomnia, irritable bowel disease, gastroesophageal reflux disease, tinnitus and antiemetic effects.
    Vestipitant
  • HY-169501
    WIN 62577
    		Antagonist
    WIN 62577 is a species-selective tachykinin NK1 receptor antagonist. WIN 62577 is also an allosteric enhancer with micromolar potency at M3 receptors. WIN 62577 exhibits potent antiviral activity against SARS-CoV-2.
    WIN 62577
  • HY-14751R
    Rolapitant (Standard)
    		Antagonist
    Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. 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 (Standard)
  • HY-117053
    ZM 253270
    		Antagonist
    ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [3H]NKA to cloned human NK-2R.
    ZM 253270
  • HY-118378
    ZD6021
    		Antagonist
    ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg.
    ZD6021
  • HY-B1392A
    Esmolol
    		Agonist
    Esmolol is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol attenuates post resuscitation myocardial dysfunction. Esmolol improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
    Esmolol
  • HY-16346R
    Netupitant (Standard)
    		Antagonist
    Netupitant (Standard) is the analytical standard of Netupitant. This product is intended for research and analytical applications. 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 (Standard)
  • HY-116958
    SCH 206272
    		Antagonist
    SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (Ki = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active.
    SCH 206272
  • HY-19670
    Befetupitant
    		Antagonist
    Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
    Befetupitant
  • HY-117216
    L-703606
    		Antagonist
    L-703606 is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
    L-703606
  • HY-106910R
    Saredutant (Standard)
    		Antagonist
    Saredutant (Standard) is the analytical standard of Saredutant. This product is intended for research and analytical applications. Saredutant is a selective NK2 receptor antagonist.
    Saredutant (Standard)
  • HY-P0061B
    Vapreotide diacetate
    		Antagonist
    Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide diacetate
  • HY-G0012S
    Monohydroxy Netupitant-d6
    		Agonist
    Monohydroxy Netupitant-d6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant.
    Monohydroxy Netupitant-d<sub>6</sub>
  • HY-159842
    Fosrolapitant
    		Antagonist
    Fosrolapitant is a neurokinin 1 (NK1) receptor antagonist.
    Fosrolapitant
  • HY-14407AR
    Fosaprepitant dimeglumine (Standard)
    		Antagonist
    Fosaprepitant (dimeglumine) (Standard) is the analytical standard of Fosaprepitant (dimeglumine). This product is intended for research and analytical applications. 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 (Standard)
  • HY-G0012
    Netupitant metabolite Monohydroxy Netupitant
    		Agonist
    Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
    Netupitant metabolite Monohydroxy Netupitant
  • HY-118356
    WIN 62,577
    		Antagonist
    WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
    WIN 62,577
  • HY-14552A
    Talnetant hydrochloride
    		Antagonist
    Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies.
    Talnetant hydrochloride
  • HY-P0255
    Physalaemin
    Physalaemin, a non-mammalian tachykinin, binds selectively to neurokinin-1 (NK1) receptor with high affinity.
    Physalaemin
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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