Articles tagged with Agonists
A global review found that Opioid Agonist Therapy (OAT) is associated with lower risk of multiple causes of death among people with opioid dependence. OAT was linked to reduced overdose-related, suicide, alcohol-related, cancer, and cardiovascular-related mortality.
A novel ghrelin receptor inverse agonist was developed for positron emission tomography (PET) imaging of functional expression in health and disease, particularly in cancer. The compound demonstrated specific binding to the Ghrelin receptor and imaging of tumors and normal tissues expressing the receptor.
Researchers identified systemic inflammation as a potential biomarker for predicting patient response to CD40 immunotherapy in advanced pancreatic cancer. Patients with systemic inflammation had worse overall survival rates than those without, suggesting that immune therapies may be less effective in these cases.
Researchers have identified a promising new compound that activates bitter taste receptors to promote airway relaxation. The most potent compound, T5-8, demonstrates marked effectiveness in human airway smooth muscle cells.
Researchers have discovered stable, synthetic STING agonists that induce anticancer immune responses in mice. These non-nucleotide small molecule STING agonists show robust anti-tumor activities and may represent an attractive approach for targeting the STING pathway.
Warren J. Leonard is recognized for pioneering work in X-linked severe combined immunodeficiency and cloning the IL-2 receptor alpha chain. His findings led to a deeper understanding of cytokine signaling and immune dysregulation.
Scientists from Tokyo University of Science discovered that an opioid compound called KNT-127 can help mask fear memory, reducing anxiety in individuals with PTSD. The study suggests that combining KNT-127 with cognitive behavioral therapy may enhance treatment efficacy for anxiety disorders.
A study published in PLOS Medicine found that co-prescribing benzodiazepines with opioid agonist treatment increases the risk of overdose death by three-fold. Doctors should avoid this practice, especially for patients who have recently left treatment or continue to use opioid drugs.
Guidelines recommend universal screening for opioid use and offering opioid agonist therapy, counselling, and mental health supports. Ongoing support in the postpartum period is crucial for women with opioid use disorders at increased risk of fatal overdose.
The new national guideline provides evidence-based treatment options for people with severe opioid use disorder, including injectable opioid agonist treatment with prescription heroin and hydromorphone. The guideline aims to reduce overdose deaths by supporting health care providers in delivering life-saving treatments.
A synthetic compound based on a brain hormone has shown surprising benefits in treating lung and other cancers in mice, but its effect on human cells was the opposite. The compound, MR409, is one of several GHRH analogs that spur healthy tissue growth and may alleviate concerns about stimulating cancer cell growth.
A new approach for treating liver cirrhosis has been found with aleglitazar, which reduces inflammation and portal hypertension in rats with cirrhosis. Aleglitazar suppresses inflammation, vasoconstriction, angiogenesis, and tumor necrosis factor overproduction in cirrhotic rats.
A network meta-analysis found that SGLT-2 inhibitors and GLP-1 agonists improved survival rates compared to DPP-4 inhibitors in patients with type 2 diabetes. The study analyzed data from 236 clinical trials involving 176,310 participants.
Phase 2 studies of tropifexor and seladelpar demonstrate potent anti-cholestatic and anti-inflammatory activity without increasing pruritus. Tropifexor and seladelpar are being explored as potential treatments for patients with primary biliary cholangitis, a progressive liver disease.
The new Canadian guideline recommends opioid agonist treatment with buprenorphine-naloxone as the preferred first-line treatment to reduce risk of overdose and death. It also identifies common practices that should be avoided, such as withdrawal management alone without transition to long-term treatment.
A study found that Medicaid coverage for methadone maintenance therapy increases planned use of opioid agonists among pregnant women with opioid use disorder. The rate of planned OAT use was about 61% in states with Medicaid coverage compared to 28% in states without coverage.
Researchers identified beta-2 adrenergic receptor agonists as compounds that can suppress alpha-synuclein gene expression, reducing the genetic risk factor for Parkinson's disease. The findings suggest that widely used beta-2AR agonists should be rigorously tested in PD patients.
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 have found a new pathway in the liver that opens the door to treat non-alcoholic fatty liver disease. The pathway involves activating a protein called TRPV4, which releases nitric oxide and blocks an enzyme contributing to the disease.
Researchers developed a 'biased' KOR agonist that suppresses pain and itch while avoiding common side effects like sedation and dysphoria. This breakthrough offers a promising new way to treat pain and intractable itch without the potential for abuse.
A study published in JAMA found that liraglutide did not improve post-hospitalization clinical stability in patients with advanced heart failure. The drug was tested in a randomized controlled trial involving 154 patients, but showed no significant effect on primary end points such as death and rehospitalizations.
A recent study examined opioid agonist therapy (OAT) use among Medicare Part D beneficiaries. The analysis found that only approximately 81,000 patients received buprenorphine-naloxone therapy, despite an estimated 300,000 patients struggling with opioid use disorder and over 200,000 requiring hospitalization for opioid-related issues.
A Mayo Clinic study reveals a drug combination of TLR agonists and cyclophosphamide to effectively treat advanced and metastatic cancers in mice. The treatment promotes the destruction of cancer cells and activates immune responses without toxicity.
Temple researchers are investigating novel compounds that activate cannabinoid receptor type 2 (CB2) to prevent HIV-associated neurocognitive disorder (HAND). The study aims to test the safety and effectiveness of these compounds in cell models and mice with HIV infection.
Researchers have discovered a new class of drugs that specifically induce apoptosis in B cell malignancies, such as leukemia and lymphoma. The drugs target the STING protein, which plays a critical role in regulating the immune system, and have been shown to be effective in treating chronic lymphocytic leukemia and multiple myeloma.
Researchers tested a low-dose dopamine-1 receptor agonist for treating cognitive and negative symptoms of schizophrenia, but found no significant improvements. The study suggests that higher doses of the medication may be more effective in counteracting these symptoms.
Researchers at Drexel University found that mothers who took B2AR agonist drugs during pregnancy were 30% more likely to have children diagnosed with autism spectrum disorder. The study suggests that these medications may influence a newborn's neurodevelopment, highlighting the need for further research on potential risks.
A new TSRI study defines an unexpected mechanism at work in an anti-autoimmune drug candidate, ozanimod. The researchers found that S1PR1 agonists directly target immune cells to slow the overproduction of proteins known to cause autoimmune disease.
Researchers have developed a new way to enhance the effectiveness of antigen-based vaccines by mimicking the natural arrangement of multiple TLR agonists. This triply-linked activator more effectively triggers an immune response than mixing individual components, paving the way for improved vaccine design.
A new study reveals that GLP-1 agonists may activate glucagon receptors, potentially promoting high blood sugar levels in patients with diabetes. The researchers emphasize the need for a more comprehensive understanding of how these drugs interact with receptors in different parts of the body.
Researchers found that GLP-1 receptor activation decreases anticipatory food reward, reducing cravings, and increases feeling of food reward during consumption, reducing overeating. The study suggests a potential therapeutic target for substance abuse disorders, offering new insights into the mechanisms of obesity.
The ELIXA study found no increased risk of cardiovascular death, heart attack, stroke, or heart failure in patients with type 2 diabetes taking lixisenatide. Lixisenatide also showed a modest benefit for weight control and no increase in hypoglycemia or pancreatic injury risk.
Local physician Jeffrey H. Samet recommends retiring the term opioid substitution therapy due to its unintended adverse consequences, suggesting the use of opioid agonist treatment instead. This change in terminology could have broad and substantial impact on patient care for opioid use disorders.
Researchers discover cannabinoid CB2 agonist AM1710 suppresses chemotherapy-induced pain in mice without tolerance or withdrawal symptoms. The therapeutic effect of AM1710 is preserved even after repeated dosing and blocking CB1 receptors produces no signs of withdrawal.
Researchers observed a crucial protective role for farnesoid-X receptor in cholestatic liver injury, with oral FXR-agonist INT-747 normalizing dysfunctional intestinal FXR-signaling and changing in intestinal permeability, inflammation, and bacterial translocation. The study suggests potential new therapeutic avenues for liver disease.
A patient who suffered a traumatic brain injury unexpectedly recovered full consciousness after receiving midazolam, a mild depressant drug. The administration of this medication resulted in the first reported case of an 'awakening' from a minimally-conscious state using this therapy.
Researchers suggest that peroxisome proliferator-activated receptor (PPAR) agonists may be effective in treating alcohol dependence. The study found that PPARα or PPARγ agonists, such as fenofibrate, reduced alcohol intake and preference in mice, indicating potential for repurposing these drugs for human treatment.
Researchers found no evidence of asymptomatic myocardial dysfunction or deterioration of systolic function in patients taking pramipexole and ropinirole. This suggests that non-ergot derived dopamine agonists may be safe for the heart, contradicting previous concerns about an increased risk of heart failure.
A study found that maintenance opioid agonist therapy with methadone or buprenorphine reduced the incidence of hepatitis C virus (HCV) infection in young injection-drug users. The treatment strategy is crucial for preventing the spread of HCV among this high-risk group.
A study published in JAMA Internal Medicine found that maintenance opioid agonist therapy with methadone or buprenorphine reduces the incidence of hepatitis C virus (HCV) infection among young injection-drug users. The treatment was associated with a lower risk of HCV transmission, highlighting its potential as a prevention strategy.
A study found associations between dopamine receptor agonist drugs and serious impulse control disorders, including pathological gambling and hypersexuality. The medications were prescribed for Parkinson disease and restless leg syndrome, but the reports showed mostly male patients, median age of 55, primarily in the US.
A systematic review and meta-analysis found that combining basal insulin with a GLP-1 agonist resulted in improved blood sugar control, similar rates of hypoglycaemia, and greater weight loss compared to other anti-diabetic treatments. This combination therapy showed a 92% greater likelihood of achieving target blood sugar control.
A new observational study investigates the prevalence of paradoxical bronchoconstriction after using β2 agonists in smokers and ex-smokers with Chronic Obstructive Pulmonary Disease (COPD). The study reveals that African-American patients are twice as likely to experience a paradoxical response, leading to worse respiratory outcomes.
Phase III study results show obeticholic acid produces meaningful biochemical improvements, including reduced ALP and bilirubin levels. The treatment also demonstrates significant clinical benefits, such as improved liver function parameters and a lower risk of liver transplantation and death.
Researchers found that rare gene variants significantly increased the risk of hospital admission for severe asthma episodes and urgent outpatient visits among patients treated with long-acting beta agonists. Non-Hispanic whites with these variants were more than twice as likely to experience uncontrolled symptoms during LABA therapy.
Researchers have found that a selective GABA inverse agonist can potentiate learning and memory performances in mice with Down's syndrome, reversing learning impairments. The drug also restored normal levels of gene expression in disregulated pathways, suggesting its therapeutic potential.
The newly reported technique can greatly speed the process of discovering therapeutic antibodies with desired biological effects. The team discovered an antibody that potently mimics thrombopoietin, a hormone essential for blood clotting.
The data presented at the AUA Annual Meeting shows that degarelix lowers the risk of cardiovascular events or death when compared to luteinising hormone-releasing agonists. Analysis of disease control-related outcomes from six comparative randomised clinical trials also supports this finding.
A new study suggests that hormone acting drugs combined with uterine artery embolization can effectively treat large uterine fibroids without the need for surgery. The treatment has been shown to reduce complications and shrink fibroids by an average of 36%.
A Cochrane Systematic Review revises conclusions on two fertility treatments, finding GnRH antagonists comparable to agonists in live birth rates while reducing ovarian hyperstimulation syndrome risks. This shift justifies the use of GnRH antagonists over agonists.
Scientists have solved the three-dimensional structure of a key biological receptor, enabling chemists to design molecules for experimental drugs. This finding has the potential to expedite drug discovery in various areas, including arthritis, respiratory disorders, and wound healing.
Researchers from Scripps Research Institute determine a new structure of the human A2A adenosine receptor, bound to a full agonist, revealing a super stabilizing agonist. This finding has important implications for drug design, particularly for treating diseases such as Parkinson's and COPD.
Research suggests that stimulating alpha-7 nicotinic receptors could enhance cortical function and improve symptoms of schizophrenia. Two studies found that low doses of AZD0328 and DMXB-A produced significant improvements in spatial working memory tasks, suggesting a potential therapeutic approach for cognitive impairments.
Scientists from Scripps Research Institute have identified a novel synthetic activator of RORα and RORγ nuclear receptors, which play key roles in human metabolism and immune function. This discovery could lead to new therapeutic approaches for diseases such as diabetes and osteoporosis.
Researchers found that compounds targeting PPARγ can improve insulin sensitivity without promoting fat cell growth, offering a new target for anti-diabetic treatments. The study suggests a unified framework for understanding the relationship between fat cell dysfunction and anti-diabetic therapies.
A Scripps Research study has found that the endocannabinoid system, which regulates memory and emotional reactions, can also dampen the effects of alcohol. The research suggests a potential target for developing drugs to treat alcohol addiction.
A dual FXR and TGR5 agonist decreases liver damage and modulates hepatic inflammation and fibrosis in a mouse model of PSC. FXR and TGR5 agonists regulate bile acids, glucose, lipids and inflammation.
The Scripps Research Institute has been awarded $1.2 million to develop high-throughput screening tests that will help identify potential small molecule therapies for breast cancer and cardiovascular disease. The project aims to modulate the activity of the LRH-1 receptor, which plays a crucial role in hormone-driven breast cancer.
A new study published in the Journal of the National Cancer Institute found that treatment with gonadotropin-releasing hormone agonists increases the risk of incident diabetes among men of all ages diagnosed with local or regional prostate cancer. The study also found an increased risk of cardiovascular disease, including coronary hear...
Researchers link beta 2 adrenergic agonists to increased autism risk in children of mothers treated for asthma and pre-term labor. Long-term neurophysiologic and behavioral impairment is also a concern with prolonged exposure to these drugs during pregnancy.