Articles tagged with Antagonists
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ISM0676 demonstrates excellent metabolic stability, superior efficacy at low doses, and a favorable safety profile, leading to significant body weight reduction and improved body composition. The compound's synergistic efficacy with Semaglutide supports its further clinical development as an obesity treatment.
A study by Helmholtz Munich researchers found that GIPR agonism and antagonism decrease body weight and food intake via different mechanisms. GIPR agonists use GABAergic neurons to exert their effect, while antagonists rely on the GLP-1 receptor signal.
Researchers discovered that FGFR antagonists can effectively rescue impaired bone repair in mouse models of osteochondrodysplasia. The treatments promote chondrocyte differentiation and increase apoptosis rates, enhancing bone formation and mineralization. This breakthrough offers new hope for individuals with skeletal disorders caused...
Long-term treatment with the nonsteroidal mineralocorticoid receptor antagonist finerenone is estimated to extend event-free survival by up to 3 years among people with heart failure. The FINEARTS-HF randomized clinical trial found this benefit in patients with mildly reduced or preserved ejection fraction.
Elinzanetant, a selective neurokinin-1,3 receptor antagonist, demonstrated significant reductions in vasomotor symptoms frequency and severity vs placebo in postmenopausal individuals with moderate to severe VMS. The treatment also improved sleep disturbances and menopause-related quality of life, with a favorable safety profile.
Researchers discovered MIA-602's effectiveness against Doxorubicin-resistant acute myeloid leukemia (AML), demonstrating reduced cell viability and tumor volume. The study suggests MIA-602 as a potential alternative treatment approach for AML, potentially circumventing chemotherapy side effects.
A small molecule called YM022 has been discovered to block aversive memory formation in mice, offering a new direction for developing anti-depressants. The study found that YM022 suppressed neuroplasticity-caused aversive memory formation and reduced depressive behaviors in mice.
A randomized clinical trial found that avoiding aspirin as part of an antithrombotic regimen reduces bleeding events without increasing thromboembolism risk in patients with advanced heart failure treated with left ventricular assist devices. The study suggests that aspirin avoidance may be a viable option for these patients.
A MU study found that providing educational information about naltrexone to healthcare professionals increases patient prescriptions for the drug. The study resulted in a 36% increase in patients leaving the facility with a prescription for naltrexone, suggesting better-informed decisions by healthcare professionals.
Researchers at Kanazawa University used high-speed atomic force microscopy to study the TRPV1 protein's structural fluctuations in response to stimulating and suppressing ligands. They found that ligand binding increases conformational fluctuations, while suppression decreases them.
The study calls for easier access to naloxone, including over-the-counter distribution, to address the US opioid epidemic. With millions lacking access, health providers are urged to include naloxone in treatment programs and counsel patients' families on its use.
The new guideline provides evidence-based recommendations for managing patients on warfarin, DOACs, and antiplatelet drugs before and after surgeries. It aims to minimize preventable bleeding and thrombotic events by standardizing approaches and protocols.
Higher aldosterone concentrations are associated with lower eGFR, lower potassium levels in blood, and higher potassium and protein concentrations in urine. The risk of CKD worsening was independent of diabetes status. Finerenone may help prevent CKD progression by targeting aldosterone's action.
Researchers at the University of Cologne investigated UPF3A and UPF3B proteins involved in nonsense-mediated mRNA decay (NMD), a quality control mechanism preventing defective mRNA from being processed into harmful proteins. The study shows that both proteins have partially overlapping functions, enabling fault-tolerant activation of NMD.
Scientists have developed a non-hormonal male contraceptive that effectively prevents pregnancy in mice, targeting the retinoic acid receptor alpha protein. The compound YCT529 was found to be 99% effective in preventing pregnancy without observable side effects, paving the way for human clinical trials.
A retrospective cohort study of patients with atrial fibrillation and diabetes found that non-vitamin K antagonist oral anticoagulants (NOAC) were associated with a lower risk of diabetes complications and mortality than warfarin. The study suggests that NOAC may be a better therapeutic choice for this patient population.
Scientists from Japan discover IL-36Ra plays a pivotal role in wound healing, and Cl-amidine normalizes exacerbated I/R injury. The study's findings suggest IL-36Ra as a potential therapeutic target for cutaneous I/R injuries.
A new analysis of 27 randomised trials involving nearly 11,000 patients found that interleukin-6 antagonists reduce the risk of death and mechanical ventilation in hospitalised COVID-19 patients. Administering one of these drugs with corticosteroids reduces the risk of death by 17% compared to using corticosteroids alone.
The collaboration aims to develop a small molecule drug targeting inflammatory cell trafficking in the gut, offering a safe alternative to current treatments for IBD. The company will apply its proprietary approach to develop antagonists of integrin targets.
Researchers at Ruhr-University Bochum discovered that certain drugs can activate glutamate receptors, rather than inhibiting them, due to their binding to specific receptor subtypes. This potentiation effect can lead to a stronger response and longer-lasting effects.
A study investigated the association between icatibant, a bradykinin 2 receptor antagonist, and improved oxygenation in COVID-19 patients. The findings suggest that icatibant may be beneficial in treating COVID-19 by improving oxygenation, and more research is needed to confirm these results.
A new study analyzed data from an international registry of 528 IBD patients with COVID-19, finding that increasing age, comorbidities, and corticosteroids are associated with severe illness. The study also suggests that steroid-sparing treatments may be crucial for maintaining remission in IBD patients during the pandemic.
A fast-fail trial has identified the kappa opioid receptor (KOR) as a potential target for treating anhedonia. The study found that participants who received a KOR antagonist showed increased activation in brain circuits involved in reward and pleasure, leading to reduced anhedonia scores.
A new study found that a novel peptide antagonist given in combination with a PD-1 inhibitor is safe and well-tolerated in patients with advanced, refractory pancreatic and rectal cancer. The highest dose tested resulted in no adverse events leading to the recommendation for use in future trials.
The study reveals arginine vasotocin increases aggression, while isotocin boosts egg care, offering insight into vertebrate behavior. The findings have implications for understanding parental care and behavior across the animal kingdom.
A recent study compared two insomnia treatments, brotizolam and suvorexant, finding they improved sleep efficiency but had varying impacts on balance. Orexin receptor antagonists like suvorexant may have fewer side effects than commonly prescribed hypnotics.
A new experimental treatment for stroke has been shown to reduce brain damage and promote motor recovery in mice. The treatment, which uses adrenergic receptor antagonists, was found to normalize brain fluids and lower potassium levels, leading to improved outcomes in stroke models.
Researchers suggest caffeine as a potential therapeutic tool for treating motivational symptoms of depression and cognitive impairments in attention-deficit/hyperactivity disorder. A new study also proposes targeting the adenosine A1R-D1R heteromer to improve spinal cord injury outcomes.
A systematic review of clinical studies on prurigo nodularis treatment found neurokinin-1 receptor antagonists to be the most promising emerging therapies. The study highlights the need for higher-powered studies and randomized controlled trials to better evaluate treatment options.
Experimental inhibition of prostaglandin E2 enhanced the ability of mice to combat infectious colitis, resulting in increased migration of defense cells and production of antimicrobial peptides. Inhibiting PGE2 also favored the expression of defensins, considered natural antibiotics, in the colon.
A new study finds that proton pump inhibitors are associated with a 19% higher risk of hip fractures in dialysis patients, regardless of usage level. Histamine-2 receptor antagonists were not linked to increased fracture risk. The findings highlight the need for individualized assessment and caution in PPI use among hemodialysis patients.
Researchers have developed selective androgen receptor degraders (SARDs) that can degrade all forms of the androgen receptor, potentially providing advanced treatment options for men with castration-resistant prostate cancer. These molecules inhibit the growth of aggressive prostate cancers that are unresponsive to other treatments.
A recent study published in JAMA Network found that nearly 84% of patients with atrial fibrillation who experienced a stroke were not receiving therapeutic anticoagulation prior to their stroke. Therapeutic anticoagulation was associated with lower odds of moderate or severe stroke and lower odds of in-hospital mortality.
A study found a significant association between increased use of antithrombotic drugs and subdural hematoma incidence in Denmark from 2000 to 2015. The risk was highest for patients taking multiple anticoagulant medications, particularly those combining vitamin K antagonists with antiplatelet drugs.
A new treatment targeting COPD and other lung diseases has been identified in a study published in The FASEB Journal. FPS-ZM1, a RAGE antagonist compound, reverses the inflammatory response and has a protective role in COPD, according to researchers.
Researchers have found that somatostatin receptor sst2 antagonist tracers can target a greater number of sst2 sites in non-NET tumors than agonists. The study shows high binding of the antagonist in 12 breast cancers, all renal cell carcinomas, and 5 medullary thyroid cancers, while agonist binding was low or absent in these cases.
Researchers at The Pennsylvania State University College of Medicine discovered that the nuclear export of the opioid growth factor receptor (OGFr) is CRM1 dependent. OGFr must translocate into the nucleus to facilitate its role in cell cycle regulation and does so utilizing nuclear localization signals and β and Ran proteins.
A study of Danish patients undergoing noncardiac surgery found that use of β-blockers was associated with increased risk for major adverse cardiovascular events (MACEs) and death. The results suggest that perioperative management of patients with hypertension should receive specific attention in clinical practice.
The ALBATROSS study found that mineralocortoid receptor antagonists do not provide a benefit to heart attack patients without heart failure. However, in a subgroup of STEMI patients, MRA treatment may have a potential mortality benefit.
Researchers found an association between dicloxacillin treatment and decreased international normalized ratio (INR) levels among patients taking warfarin or phenprocoumon. This finding suggests that physicians should be aware of potential interactions and monitor INR levels accordingly.
The SENRI trial found that NK1 antagonists significantly increased the inhibition rate of vomiting and nausea, especially in females. The three-drug combination therapy of aprepitant, a 5-HT3 receptor antagonist, and dexamethasone may be a good antiemetic treatment option for oxaliplatin-based chemotherapy in patients with colorectal c...
Researchers have identified a new class of dopamine receptor antagonists that selectively target mosquito cells, offering a safer alternative to current insecticides. These chemicals are structurally distinct and target different biochemical paths in mosquitoes, reducing the risk of human exposure.
A Phase 2 clinical trial demonstrates that AF-219, a selective and non-narcotic agent, significantly reduces daytime cough frequency by 75% compared to placebo. The study also shows improvements in secondary endpoints such as severity and urge to cough.
A study found that an endothelin-A antagonist can enhance renal recovery in patients with renovascular disease. The medication, already used for pulmonary hypertension, promotes kidney function and improves responses after renal angioplasty.
Researchers identified OGF-OGFr regulatory pathway as key factor in enhanced cell replication and diabetic wound healing. Topical naltrexone application stimulates cell proliferation, but only when OGFr expression is diminished.
A network meta-analysis of nearly 50 randomized trials compared the efficacy and safety outcomes of eight anticoagulation options for venous thromboembolism. Rivaroxaban and apixaban were associated with the lowest bleeding risk, while UFH-vitamin K antagonist combination was linked to higher recurrent venous thromboembolism rates.
A study of over 56,000 patients with inflammatory bowel disease found no association between TNF inhibitor use and increased cancer risk. However, the authors emphasize the need for continued long-term follow-up to monitor potential risks.
Researchers have found that caffeine can positively affect tau deposits in Alzheimer's disease, improving spatial memory and reducing pathogenic processes in genetically altered mice. The study suggests a new class of drugs may be developed for the treatment of Alzheimer's disease using an A2A antagonist.
A recent study found that obese women may require a higher or adjusted dose of GnRH antagonist medication for successful IVF egg harvesting due to faster clearance rates and rebound hormone responses. This could improve fertility treatment outcomes for overweight and obese women.
A large population-based study found that long-term use of proton pump inhibitors and histamine 2 receptor antagonists increases the risk of vitamin B12 deficiency. The association was strongest in women and younger age groups with potent acid suppression, and decreased after discontinuation.
A study published in The FASEB Journal reveals that obesity is associated with an abnormal amount of the inflammatory protein PAR2 on abdominal fat tissues, which can be blocked by a new oral drug. This finding suggests that obesity may be an inflammatory disease and that controlling inflammation could lead to weight loss.
Thioperamide significantly decreases brain water content and malondialdehyde levels while increasing histamine levels and superoxide dismutase activity, preventing oxidative damage and brain edema. Thioperamide's effects are mediated by postsynaptic H1 receptors.
Researchers have discovered that medications used to treat heart failure and high blood pressure can also aid in reducing obesity by preventing weight gain and increasing the production of energy-burning fat cells. The study found that these drugs helped increase brown fat cells, which burn energy to prevent weight gain.
A UNC School of Medicine study found that cold perception is enhanced when nerve circuitry for heat is inactivated, impacting how people with chronic pain experience temperature sensations. The research also has implications for why some patients taking pain relief drugs shiver before hyperthermia sets in.
Two studies investigate heart failure therapies, finding varying outcomes regarding mortality rates among older patients. RAS antagonists are associated with improved survival in patients with preserved ejection fraction, while aldosterone antagonist therapy shows limited effectiveness.
Researchers found fewer benefits associated with aldosterone antagonist drugs, including no difference in deaths or hospital readmissions for cardiovascular events. However, patients taking the drugs were at higher risk of hyperkalemia and less likely to be readmitted to the hospital for heart failure.
Researchers found that a high-saturated-fat, high-cholesterol diet elevated microglial activation and reduced neuronal development in middle-aged laboratory rats. However, treatment with IL-1Ra alleviated these effects, suggesting potential use in neurological disorders involving neuroinflammation.
A retrospective study found that methylnaltrexone (MNTX) restored bowel function and improved feeding outcomes in critically ill patients with opioid-induced constipation. MNTX was well-tolerated and showed immediate effects, improving enteral feeding and reducing gastric residual volumes.
Recent studies have shown that aldosterone antagonists reduce mortality and cardiovascular complications in patients with heart failure. The benefits of these drugs are clear, with a 24% reduction in cardiovascular death and a 42% reduction in hospitalization for heart failure.
An international research team has shown that an investigational agent that sticks onto the surface of tumor cells can effectively image tumors. The 'antagonist', 111In-DOTA-BASS, outperformed the widely used 'agonist' agent, OctreoScan, in detecting neuroendocrine tumors.