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-105346
    WIN 51708
    		Antagonist
    WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor.
    WIN 51708
  • HY-177079S
    Dazodeunetant
    		Inhibitor
    Dazodeunetant (Example 56) is a nitrogen-containing fused ring derivative. Dazodeunetant is an inhibitor of neurokinin (NK). Dazodeunetant has an IC50 0f 75.99 nM against NK3R in HEK293-NK3 (IP1). Dazodeunetant can be studied in research for menopausal hot flashes.
    Dazodeunetant
  • HY-172514
    (1R,2S,3R)-Aprepitant
    		Antagonist
    (1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive human neurokinin-1 (NK-1) receptor antagonist. (1R,2S,3R)-Aprepitant is promising for research of cancers and postoperative nausea and vomiting.
    (1R,2S,3R)-Aprepitant
  • HY-10053B
    Maropitant citrate
    		Antagonist
    Maropitant citrate is an orally active NK1 receptor antagonist. Maropitant citrate prevents vomiting and inhibits ulcerative dermatitis.
    Maropitant citrate
  • HY-119005A
    YM-49598 iodide
    		Antagonist
    YM-49598 iodide is a tachykinin NK-1 receptor antagonist. YM-49598 iodide can inhibit drug-induced bladder contraction in rats, with IC50 of 11 μg/kg.
    YM-49598 iodide
  • HY-14551C
    Osanetant monohydrochloride
    		Antagonist
    Osanetant (SR142801) monohydrochloride is a selective NK3 receptor antagonist. Osanetant monohydrochloride produces anxiolytic- and antidepressant-like effects.
    Osanetant monohydrochloride
  • HY-N7574
    WS9326A
    		Antagonist
    WS9326A is a tachykinin receptor antagonist that can be isolated from Streptomyces violaceus.
    WS9326A
  • HY-19429A
    SLV-317
    		Antagonist
    SLV-317 is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 can effective antagonist of substance P-induced effects.
    SLV-317
  • HY-10053R
    Maropitant (Standard)
    		Antagonist
    Maropitant (Standard) is the analytical standard of Maropitant. This product is intended for research and analytical applications. 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 (Standard)
  • HY-14432R
    Pavinetant (Standard)
    		Antagonist
    Pavinetant (Standard) is the analytical standard of Pavinetant. This product is intended for research and analytical applications. Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant (Standard)
  • HY-109171S
    Elinzanetant-d3
    		Antagonist
    Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women.
    Elinzanetant-d<sub>3</sub>
  • HY-107693
    SSR 146977 hydrochloride
    		Antagonist
    SSR 146977 hydrochloride is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 hydrochloride can be used in the study of psychiatric disorders and airway inflammation.
    SSR 146977 hydrochloride
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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