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Avacopan, a Novel Competitive C5a Receptor Antagonist, for Severe Antineutrophil Cytoplasmic Autoantibody-Associated Vasculitis
Avacopan is a relatively novel drug with complement antagonizing properties, and it has demonstrated promising outcomes in treating antineutrophil...
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Comparison of the effects of the GPIIb-IIIa antagonist Zalunfiban and the P2Y12 antagonist Selatogrel on Platelet Aggregation
Understanding the pharmacodynamic effects of platelet inhibitors is standard for develo** more effective antithrombotic therapies. An example is...
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Vitamin D receptor antagonist activity in wastewater effluents—potential for endocrine disruption
BackgroundEndocrine disrupting chemicals have been identified for a number of human endocrine systems, but there are no reports on vitamin...
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The Study of Biological Activity of a New Thieno[2,3-D]-Pyrimidine-Based Neutral Antagonist of Thyrotropin Receptor
The development of low-molecular-weight antagonists of thyroid-stimulating hormone (TSH) receptor is a promising trend in the treatment of autoimmune...
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A novel prostaglandin E receptor 4 (EP4) small molecule antagonist induces articular cartilage regeneration
Articular cartilage repair and regeneration is an unmet clinical need because of the poor self-regeneration capacity of the tissue. In this study, we...
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Interleukin 1 receptor antagonist relation to cardiovascular disease risk in patients with rheumatoid arthritis
Interleukin (IL) 1, and its family member, IL-1 receptor antagonist (IL-1ra), are involved in the pathogenesis and inflammation perpetuation of...
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Anti-Apoptotic Effects of AMPA Receptor Antagonist Perampanel in Early Brain Injury After Subarachnoid Hemorrhage in Mice
This study was aimed to investigate if acute neuronal apoptosis is induced by activation of AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazole propionate)...
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Apelin receptor antagonist boosts dendritic cell vaccine efficacy in controlling angiogenic, metastatic and apoptotic-related factors in 4T1 breast tumor-bearing mice
AbstractApelin/APJ axis plays a critical role in cancer progression, thus its targeting inhibits tumor growth. However, blocking of Apelin/APJ axis...
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P2X3 Receptor Antagonist Eliapixant in Phase I Clinical Trials: Safety and Inter-ethnic Comparison of Pharmacokinetics in Healthy Chinese and Japanese Participants
BackgroundAfferent neuronal hypersensitization via P2X3 receptor signaling has been implicated as a driver of several disorders, including refractory...
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The V2 receptor antagonist tolvaptan counteracts proliferation and invasivity in human cancer cells
PurposeHyponatremia, the most frequent electrolyte alteration in clinical practice, has been associated with a worse prognosis in cancer patients. On...
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Gene polymorphisms of TACR1 serve as the potential pharmacogenetic predictors of response to the neurokinin-1 receptor antagonist-based antiemetic regimens: a candidate-gene association study in breast cancer patients
PurposeThe current candidate gene association study aims to investigate tag SNPs from the TACR1 gene as pharmacogenetic predictors of response to...
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The effects of novel macrocyclic chelates on the targeting properties of the 68Ga-labeled Gastrin releasing peptide receptor antagonist RM2
BackgroundThe gastrin-releasing peptide receptor (GRPr) is a molecular target for the visualization of prostate cancer. Bombesin (BN) analogs are...
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H1-Receptor Antagonist Olopatadine Inhibits MUC5AC Secretion by Conjunctival Goblet Cells
The study examined the effect of H1-receptor antagonist olopatadine on the secretory function of cultured rat conjunctival goblet cells (CGC)...
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Glial cell reactivity and oxidative stress prevention in Alzheimer’s disease mice model by an optimized NMDA receptor antagonist
In Alzheimer's disease pathology, several neuronal processes are dysregulated by excitotoxicity including neuroinflammation and oxidative stress...
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Development of Purinergic Receptor Agonists and Antagonists
Adenosine, P2Y, and P2X receptors have been the focus of purinergic ligand development in the pharmaceutical sector and academic medicinal chemistry...
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Effect of the Topical External Formulation of the Low-Affinity NMDA Receptor Antagonist Hemantane on Peripheral Sensitization Induced by TRPV1 Receptor Agonist Capsaicin in Mice
The effect of the noncompetitive low-affinity NMDA receptor antagonist hemantane [ N -(2-adamantyl)hexamethyleneimine hydrochloride) in two topical...
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Treatment of nonarteritic anterior ischemic optic neuropathy with an endothelin antagonist: ENDOTHELION (ENDOTHELin antagonist receptor in Ischemic Optic Neuropathy)—a multicentre randomised controlled trial protocol
BackgroundNonarteritic anterior ischemic optic neuropathy (NAAION) is a major cause of blindness in individuals over 50 years of age, with no...
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GnRH antagonist weakens endometrial stromal cells growth ability by decreasing c-kit receptor expression
BackgroundSeveral surveys have reported that patients treated with gonadotropin-releasing hormone antagonist (GnRH-ant) protocol showed a...
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Predictors of placebo response in three large clinical trials of the V1a receptor antagonist balovaptan in autism spectrum disorder
High rates of placebo response are increasingly implicated in failed autism spectrum disorder (ASD) clinical trials. Despite this, there are limited...
