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neurokinin-1 receptor antagonist
Aprepitant is classified as an NK1 antagonist. Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.
- Maya Tokumoto, .et al. , Connect Tissue Res, 2022, Jul 20;1-11 PMID: 35856812
- Kodji X, .et al. , FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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neurokinin-1 receptor antagonist
Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist. -
neurokinin-1 receptor antagonist
Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. -
NK1 receptor antagonist
GR 205171 is a selective neurokinin-1 receptor antagonist -
NK1 receptor antagonist
Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. -
tachykinin NK2 receptor antagonist
Ibodutant is a tachykinin NK2 receptor antagonist for the treatment of Irritable Bowel Syndrome with diarrhoea (IBS-D) -
NK1R antagonist
Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. -
NK1 receptor antagonist
Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis.- Bubak AN, .et al. , J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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NK1 receptor antagonist
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist. It competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). -
NK3 receptor antagonist
Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. -
NK1 receptor antagonist
Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. -
NK2 antagonist
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide antagonist at tachykinin NK2 receptors, inhibits binding of [3H]GR100679 to hNK2-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction, with anxiolytic-like activity. -
NK-1 receptor antagonist
NK-1 Antagonist 1 (Rolapitant intermediate) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression. -
triple tachykinin receptor antagonist
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. -
NK3R antagonist
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. -
neurokinin receptors antagonist
SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS). -
NK3R antagonist
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. -
NK1 receptor antagonist
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist. -
Neurokinin-1 (NK-1) receptor antagonist
Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
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Bioactive Compounds
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Signaling Pathway
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Neurokinin Receptors
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