ArticleDrug design, development and therapy2020
The NK-1R Antagonist Aprepitant Prevents LPS-Induced Oxidative Stress and Inflammation in RAW264.7 Macrophages.
Article in Drug design, development and therapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 28 citations in OpenAlex.
- Anti-Inflammatory Evaluation of Pyrazino[2,1-Pharmaceuticals (Basel, Switzerland) · 2026Article
- Neuro-Immune Crosstalk: Molecular Mechanisms, Biological Functions, Diseases, and Therapeutic Targets.MedComm · 2026Review
- Mast cells shape early pulmonary inflammation and regulate dendritic cell abundance and localization after chemical induced lung injury.Frontiers in immunology · 2026Article
- Targeting sirtuin 1/nuclear factor erythroid 2-related factor 2/tumor necrosis factor-α pathway to modulate hepatic ischemia reperfusion-induced injury.World journal of hepatology · 2025Article
- The role of substance P in Th17/Treg imbalance and ocular surface damage in chronic allergic conjunctivitis.Journal of translational medicine · 2025Article
- Aprepitant alleviates acute lung injury in a rat model of hepatic ischemia-reperfusion via NLRP3/IL-1β signaling pathway.Scientific reports · 2025Article
- Colon-Targeted Mucoadhesive PLGA Microspheres Loaded withMolecules (Basel, Switzerland) · 2025Article
- Tachykinin Receptors and their Antagonists: Unraveling Their Role in Metabolic Disorders and Therapeutic Innovations.Current drug targets · 2025Review
- Role of Sensory Nerves in Pulmonary Fibrosis.International journal of molecular sciences · 2024Review
- Advances in the research and application of neurokinin-1 receptor antagonists.Journal of Zhejiang University. Science. B · 2024Review
- Aprepitant Restores Corneal Sensitivity and Reduces Pain in DED.Translational vision science & technology · 2024Article
- The In Vitro Pro-inflammatory Functions of the SP/NK1R System in Prostate Cancer: a Focus on Nuclear Factor-Kappa B (NF-κB) and Its Pro-inflammatory Target Genes.Applied biochemistry and biotechnology · 2023Article
- Blocking SP/NK1R signaling improves spinal cord hemisection by inhibiting the release of pro-inflammatory cytokines in rabbits.The journal of spinal cord medicine · 2023Article
- Neurotransmitters: promising immune modulators in the tumor microenvironment.Frontiers in immunology · 2023Review
- Downregulation of p300/CBP-associated factor inhibits cardiomyocyte apoptosis via suppression of NF-κB pathway in ischaemia/reperfusion injury rats.Journal of cellular and molecular medicine · 2021Article
- Pathogenic role of the SP/ NK1R system in GBM cells through inhibiting the thioredoxin system.Iranian journal of basic medical sciences · 2021Article
- Aprepitant Inhibits JNK and p38/MAPK to Attenuate Inflammation and Suppresses Inflammatory Pain.Frontiers in pharmacology · 2021Article
- The Neurokinin-1 Receptor Antagonist Aprepitant: An Intelligent Bullet against Cancer?Cancers · 2020Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe macrophage is one of the most important types of immune cells that protect against harmful stimuli. Macrophage activation plays a pivotal role in the progression and development of various inflammatory diseases. The neurokinin 1 receptor (NK-1R) is a G protein-coupled receptor that plays an important role in inflammatory diseases. Aprepitant is a kind of NK-1R antagonist. The purpose of this study is to determine the protective effect of aprepitant in lipopolysaccharide (LPS)-induced inflammatory responses in macrophages.
methodsWe examined the anti-inflammatory and anti-oxidant effects of aprepitant in LPS-treated RAW264.7 macrophages by using real-time PCR, ELISA, and Western blot analysis. We also assessed cellular oxidative stress signaling by measuring the levels of cellular MDA, total ROS, and NADPH oxidase expression. Cellular NO production was measured by DAF-FM DA staining. The inhibitory effect of aprepitant against NF-κB signaling was evaluated by luciferase assay and Western blot analysis.
resultsThe expression of NK-1R is increased in LPS-induced macrophages, suggesting a potential role of the receptor in the inflammatory response. We show that aprepitant protects macrophages against oxidative stress by reducing the generation of ROS and the expression of NOX-4. Furthermore, aprepitant inhibits the secretion of pro-inflammatory cytokines and chemotactic factors by mediating the NF-κB signaling pathway.
conclusionThe NK-1R receptor antagonist aprepitant acts as an anti-inflammatory agent, indicating that the blockage of the NK-1R pathway in macrophages has the potential to suppress inflammation.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.