Neurokinin Receptor
NK receptor; Tachykinin receptor
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
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Neurokinin Receptor Inhibitors
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Neurokinin Receptor Agonists
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Neurokinin Receptor Antagonists
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Neurokinin Receptor Activator
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Neurokinin Receptor Modulators
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Neurokinin Receptor Related Products (276)
Related Products (276)
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Antibodies (4)
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Neurokinin Receptor Isoform Comparison
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Aprepitant
0 ImagesSynonyms: MK-0869; MK-869; L-754030Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
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Senktide
0 ImagesSenktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide less potently agonizes the NK1 receptor (EC50=35 µM). Senktide is promising for research of neurological disease.
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EB1002
0 ImagesEB1002 is a highly selective, long-acting NK2R agonist. EB1002 exerts central appetite suppression, increases peripheral energy expenditure and enhances insulin sensitivity, which effectively reduces body weight, improves glucose and lipid metabolism, with favorable safety profiles. EB1002 can be used for research on diseases such as obesity and type 2 diabetes.
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L-659874
0 ImagesCat. No.: HY-P2593CAS No.: 125989-15-3L-659874 is a selective NK2 receptor antagonist with an IC50 value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses.
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Ranakinin
0 ImagesCat. No.: HY-P2139CAS No.: 139446-71-2Ranakinin is a NK1R agonist. Ranakinin inhibits the binding of selective NK1 radioligands to NK1 receptors. Ranakinin activates phospholipase C (Phospholipase C), thereby enhancing polyphosphoinositide hydrolysis. Ranakinin stimulates inositol phosphate production and reduces membrane polyphosphoinositide levels. Ranakinin stimulates corticosterone and aldosterone secretion.
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Neurokinin A
0 ImagesSynonyms: Substance K; Neurokinin α; Neuromedin L; NKANeurokinin 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.
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Anti-Mouse NK1.1 Antibody (PK136)
0 ImagesCat. No.: HY-P99143Purity: 98.57%Anti-Mouse NK1.1 Antibody (PK136) is an anti-mouse NK1.1 IgG2a monoclonal antibody. Anti-Mouse NK1.1 Antibody (PK136) can deplete natural killer (NK) cells. Anti-Mouse NK1.1 Antibody (PK136) inhibits the JAK-STAT and NF-κB signaling pathways. Anti-Mouse NK1.1 Antibody (PK136) can be used for research on inflammation conditions such as non-alcoholic steatohepatitis (NASH).
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Fosaprepitant dimeglumine
0 ImagesSynonyms: MK-0517; L785298Fosaprepitant 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).
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Netupitant
0 ImagesSynonyms: CID 6451149Netupitant (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.
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N-Acetyl-L-tryptophan
0 ImagesN-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases.
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Saredutant
0 ImagesSynonyms: SR 48968; SR 48968CSaredutant is a selective NK2 receptor antagonist.
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Elinzanetant
0 ImagesSynonyms: NT-814; BAY3427080Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause.
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H-Glu(OtBu)-OtBu hydrochloride
0 ImagesH-Glu(OtBu)-OtBu hydrochloride is a key intermediate that can be used to synthesize prostate-specific membrane antigen (PSMA) targeting probes. H-Glu(OtBu)-OtBu hydrochloride can reduce nonspecific background binding through negatively charged linkers, improve tumor/background contrast, and can be used in prostate cancer PET/SPECT imaging studies.
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Neurokinin B TFA
0 ImagesNeurokinin B TFA is a tachykinin family peptide that preferentially binds to and activates NK3R over other tachykinin receptors. Neurokinin B TFA preferentially binds to the substance P receptor (SP-N receptor) and mediates acetylcholine release from cholinergic neurons. Neurokinin B TFA regulates the pulsatile release of Kisspeptin and GnRH, stimulates or inhibits the secretion of luteinizing hormone (HY-P2293), regulates reproductive function via metabolic signals, and drives the onset of puberty. Neurokinin B TFA exerts vasoactive effects and induces contraction of isolated guinea pig ileum. Neurokinin B TFA can be used in studies related to hypogonadotropic hypogonadism.
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LM11A-31
0 ImagesLM11A-31, a non-peptide p75NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
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L-733060 hydrochloride
0 ImagesL-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain.
