| S1189 |
Aprepitant
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Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. This compound reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. It inhibits HIV infection of human macrophages.
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Br J Cancer, 2024, 10.1038/s41416-024-02608-8
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Inflammation, 2023, 46(1):256-269
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Nat Commun, 2022, 13(1):4995
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| S5476 |
Rolapitant
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Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.
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Cell Metabolism, 2025, 1852-1869.e8
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Cell Communication and Signaling, 2024, 195
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Cell Commun Signal, 2024, 22(1):195
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| S4654 |
Netupitant
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Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
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Antimicrobial Agents and Chemotherapy, 2025, e00484-25
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Nature Communications, 2019, 17
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Nat Commun, 2019, 10(1):17
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| S3038 |
Fosaprepitant dimeglumine salt
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Fosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
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Nat Cell Biol, 2024,
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J Immunother Cancer, 2024, 12(11)e009805
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| E4624 |
Tradipitant
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Tradipitant(VLY-686, LY686017) is the 2nd generation antagonist of neurokinin-1 (NK-1). It exhibits potential for treating chemotherapy-induced nausea, depression, alcoholism, social anxiety disorder, and for developing imaging ligands.
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| S0772 |
L-732138
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L-732138 (L-732,138) is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor/substance P (SP) receptor. This compound inhibits the binding of 125I-SP to the human NK-1 receptor stably expressed in CHO cells with IC50 of 2.3 nM.
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| E4853 |
Rolapitant hydrochloride hydrate
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Rolapitant hydrochloride hydrate(SCH619734 hydrochloride hydrate) is a long-acting, extremely selective antagonist of the Nk-1 receptor antagonist (NK-1RA) with antiemetic activity. It significantly penetrates the central nervous system (CNS) and used clinically to prevent chemotherapy-induced nausea and vomiting (CINV) in cancer patients undergoing high and moderate emetogenic chemotherapy.
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| E8168 |
Substance P
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Substance P (Neurokinin P) is an 11-amino-acid neuropeptide and an agonist for the neurokinin-1 receptor (NK1R), binding with high affinity to regulate pain, anxiety, and stress responses. It is present in the CNS and PNS, playing a key role in neurotransmission, neuromodulation, and wound healing research.
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| E3431 |
Asparagus Extract
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Asparagus Extract is extracted from Asparagus officinalis, which contains adaptogenic, neuroprotective, antioxidant, anti-inflammatory, and nootropic activity.
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| E5879New |
Elinzanetant
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Elinzanetant (NT-814; BAY3427080) is a nonhormonal dual antagonist of NK1/NK3 receptor that reduces GnRH pulsatility by blocking neurokinin B (NK3) and substance P (NK1) effects on the reproductive axis in KNDy neurons.
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