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Antagonist - DOAJ

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Last Updated: 10 December 2022

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A Comparison among Nonvitamin K Antagonist Oral Anticoagulants in Asian Patients with Venous Thromboembolism: A Multi-Institutional Study

The comparison of clinical results and safety in Asian patients with venous thromboembolism remains uncertain. From the Chang Gung Research Database between 1 January 2012 and 31 December 2019, a cohort of 1480 patients with VTE was identified from the Chang Gung Research Database. According to real-world applications in Asian patients with VTE, the DOAC type was not associated with the risk of recurrent VTE or major bleeding within 12 months of treatment initiation.

Source link: https://doi.org/10.3390/jcm11237159


Efficacy of Serotonin Type 3 Receptor Antagonist Ramosetron on Diarrhea-Predominant Irritable Bowel Syndrome (IBS-D)-Like Symptoms in Patients with Quiescent Inflammatory Bowel Disease: A Randomized, Double-Blind, Placebo-Controlled Trial

Patients with a chronic inflammatory bowel disease suffer frequently have diarrhea-predominant irritable bowel syndrome -like signs such as abdominal pain or stool irregularities. Patients with chronic IBD, who met the Rome III diagnostic criteria for IBS-D, were randomly assigned either ramosetron or a placebo, orally every four weeks for four weeks. In the ramosetron group, the response rate for relief from general IBS-D-like symptoms at the final evaluation point was much higher than in the placebo group. In the ramosetron group, the responder rate for improvement of bowel habits was significantly higher than in the placebo group compared to the placebo group.

Source link: https://doi.org/10.3390/jcm11236882


A Novel Aryl Hydrocarbon Receptor Antagonist HBU651 Ameliorates Peripheral and Hypothalamic Inflammation in High-Fat Diet-Induced Obese Mice

Obesity is a chronic peripheral inflammation disease that is largely related to neurodegenerative diseases and environmental exposure. The aryl hydrocarbon receptor is a ligand-activated nuclear receptor activated by environmental chemical, such as dioxins, and acts as a mediator of inflammation by interfering with nuclear factor -u03baB. HBU651 successfully blocked lipopolysaccharide-mediated nuclear localization of NF-u03baB and the manufacture of NF- based inflammatory cytokines, such as tumor necrosis factor -u03b1, interleukin -1u03b2, and IL-6 in BV2 microglia cells, as shown by HBU651 in BV2 microglia cells, including tumor necrosis factor -u03b1u03bbaB-u03baB-mediated -mediated nuclear localization of -u03baB and production of &u03baB-u03baB-dependent proinflammatory cytokines, -u03b1u03b1 u03b1u03b2 u03b2 u03b2u03b1 u03b1u03b1, -u03b1, tu03b1; u03b1aB2u03b1 -u03b1-U03 Microglial activity in the arcuate nucleus in the hypothalamus in the hypothalamus had also decreased.

Source link: https://doi.org/10.3390/ijms232314871


Pharmacological characterization of a novel potent, selective, and orally active orexin 2 receptor antagonist, SDM‐878

Abstract Aims We recently found a novel orexin 2 receptor antagonist, SDMu2010878. Methods SDM2010878 was tested for in vitro potency and selectivity of human orexin 1, human orexin 2, rat OX1, and rat OX2receptors in CHO cells that have stable expression of human orexin 1, human orexin 2, rat OX1, and rat OX2receptors. The target engagement of SDMu2010878 in the rat brain was investigated using the antagonistic effect of hyperlocomotion caused by intracerebroventricular administration of the OX2 receptor agonist, ADLu2010OXB. SDM2010878 demonstrated potent inhibitory activities for human and rat OX2 receptors with IC values of 10. 6 and 8. 8 nM, respectively, with a selectivity against the OX1receptor that was almost 1000fold. In a rats EEG study, SDMu2010878 demonstrated a potent sleepu2010promoting activity at the same dose. Conclusions The SDMu2010878 is expected to be a useful pharmacological instrument for investigating the role of the OX2receptor, and it may have therapeutic potential for insomnia treatment.

Source link: https://doi.org/10.1002/npr2.12105


Non-steroidal Mineralocorticoid Receptor Antagonist Eliciting Cardiorenal Protection is a New Option for Patients with Chronic Kidney Disease

Chronic kidney disease has been limited by adverse events, especially when combined with renin-angiotensin system inhibitors, and guideline-recommend drugs for CKD patients. Patients with CKD have a promising alternative after the introduction of non-steroidal MRAs. Non-steroidal MRAs are based on the molecular configuration of the mineralocorticoid receptor, and differ in structure from spironolactone, a progesterone derivative. Non-steroidal MRAs' design determines their more effective and selective inhibition of MR patients, providing patients with more benefits without fewer adverse effects than MRAs. Finerenone reduces the cardiovascular and kidney composite outcomes in diabetic patients with CKD, prompting a cardioprotective response, according to the main message. In diabetic patients with CKD, Esaxerenone can effectively reduce blood pressure in hypertensive patients and albuminuria. A safer and more cost-effective option may be a combination therapy with sodium glucose cotransport-2 inhibition or a new potassium binder.

Source link: https://doi.org/10.1159/000528066


Gel-forming antagonist provides a lasting effect on CGRP-induced vasodilation

Due to their important roles in causing migraine headaches, migraine treatment has been aimed at CGRP and its receptor, the CLR/RAMP1 receptor complex. However, some patients with migraines persist, perhaps due to the inability of anti-CGRP drugs to completely reduce CGRP levels or hit target cells. We have recently discovered that several chimeric adrenomedullin/adrenomedullin 2 peptides are potent CLR/RAMP receptor antagonists and self-assemble to create liquid gels, which is serendipity. ADE651 gel in rats subcutaneously led to the persistent presence of ADE651 in circulation for more than a week, according to a survey. In addition, an investigation of vascular blood flow in rat hindlimbs revealed that ADE651 significantly reduced CGRP-induced vaping. Since gel-forming antagonists have direct and sustained access to target cells, ADE651 and related CLR/RAMP receptor antagonists may be promising candidates for migraine patients with CGRP- and/or adrenomedullin-mediated headaches.

Source link: https://doi.org/10.3389/fphar.2022.1040951


Effects of letrozole co-treatment on the cumulative live-birth rate among normal responders in gonadotropin-releasing hormone antagonist cycles

Letrozole cotherapy has been shown to enhance clinical outcomes in both high and poor responders in the GnRH-antagonist protocol, according to studies. To investigate the clinical value of letrozole cotreatment in vitro fertilization for normal ovarian reserve patients treated with the GnRH antagonist protocol from 1 January to December 2017, we conducted a retrospective analysis based on data from 1 January to 31 December 2017 for all IVF-related GnRH-antagonist protocols. The initial gonadotropin dose and total Gn dosage were significantly lower, and the number of days of Gn therapy in the letrozole group was considerably less than that of non-letrozole group compared to the non-letrozole group. Letrozole's combination with a GnRH antagonist may have no effect on the clinical birth rate or cumulative live-birth rate in patients with a normal ovarian reserve. In addition, the decreased estradiol level in the ovarian simulation by letrozole supports letrozole as a safe option for fertility preservation in estrogen-related cancer patients.

Source link: https://doi.org/10.3389/fmed.2022.1070583


SCH58261, the antagonist of adenosine A2A receptor, alleviates cadmium-induced preeclampsia via sirtiun-1/hypoxia-inducible factor-1α pathway in rats

OBJECTIVE: To determine the role of adenosine A2A receptor in cadmium-induced preeclampsia rats and the potential molecular mechanism. PATIENTS AND METHODS: The expression of A2AR in placentae obtained from PE women and normal pregnant women was measured. To create a PE rat model in PE and SCH+PE rats, the 0. 125 mg/kg/d CdCl2 was used. With a dose of 0. 2 mg/kg in SCH+NP and SCH+PE rats, SCH58261 was used as the specific antagonist of A2AR. A2AR and HIF-1u03b1 increased, and sirt1 decreased in placenta in both PE women and cadmium-induced PE rats, according to the researchers.

Source link: https://doaj.org/article/b7ec58955b7d4660a2021e77a5333fd0


Matrilin-3 alleviates extracellular matrix degradation of nucleus pulposus cells via induction of IL-1 receptor antagonist

NP cells were isolated from the patient's disc samples and exposed to recombinant human -Matrilin-3 protein, and IL-1b2 is used as a reducer of nucleus pulposus cell degeneration. In addition, MATN3 could upregulate Collagen II and aggrecan expressions, as well as inhibit MMP-13 and Collagen X production of NP cells. In addition, IL-1u03b2 downregulated the Collagen II and aggrecan, but maintained the MMP-13 and Collagen X levels of NP cells, which had been antagonized by MATN3's intervention. The protective effects of ECM in NP cells were significantly reduced by silencing of IL-1Ra, surprisingly. CONCLUSIONS: This paper provides a novel view of Matrilin-3 in the ECM stability of NP thanks to its ability to promote IL-1Ra. MATN3 has been shown to effectively guard human NP cells in a variety of ways, including Collagen II and aggrecan, as well as inflammation inhibition.

Source link: https://doaj.org/article/ed56bbcf69f042f8ad3fda181b4a1a63

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions