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-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-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-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-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-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-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-P2603
    Bz-Dab(NBD)-AwFpP-Nle-NH2
    		Antagonist
    Bz-Dab(NBD)-AwFpP-Nle-NH2 (Compound 5B) is a potent fluorescent antagonist of NK2 receptor, with a pKi of 8.87 nM (Ex=340 nm, Em=505 nm).
    Bz-Dab(NBD)-AwFpP-Nle-NH2
  • 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
  • HY-P0250
    Kassinin
    Kassinin is a peptide derived from the Kassina frog. It belongs to tachykinin family of neuropeptides. It is secreted as a defense response, and is involved in neuropeptide signalling.
    Kassinin
  • HY-P0236
    Neurokinin A(4-10)
    		Agonist
    Neurokinin A (4-10) is a tachykinin NK2 receptor agonist.
    Neurokinin A(4-10)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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