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8 articles for “agonists”
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The Renaissance and Resilience of CB1 Reverse Agonists: From Central Liabilities to Peripheral Promise
Abstract: Building upon these foundational insights, current research has increasingly focused on refining the pharmacological profile of CB1 reverse agonists to maximize therapeutic benefit while minimizing central adverse effects. The adverse neuropsychiatric outcomes associated with first-generation agents such as Rimonabant including anxiety, depression, and suicidal ideation highlighted the critical role of central CB1 receptors in mood regulation. Consequently, drug development strategies have shifted toward peripherally restricted CB1 reverse agonists that exhibit …
Published in International Journal of Cheminformatics · Vol. 4, Issue 1, 2026 · pp. 30–35 Read article
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CB₁ Reverse Agonists: A Cheminformatic and Patent Landscape Study
Abstract: The endocannabinoid system plays a crucial role in numerous physiological functions, making cannabinoid receptor 1 (CB1) an attractive target for therapeutic development. This review provides a systematic analysis of patent filings from 2019 to 2023 that focus on small-molecule CB1 reverse agonists. It begins with an overview of the endocannabinoid system, highlighting CB1’s involvement in energy balance, pain regulation, and neuroinflammatory processes The main section of the review examines fifteen …
Published in International Journal of Cheminformatics · Vol. 3, Issue 2, 2025 · pp. 33–36 Read article
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Samelisant, an H3 Receptor Agonist as an Anti-Alzheimer Potential – A Pilot Study on Molecular Docking
Abstract: Neurodegenerative diseases have become more prevalent and about 55 million of the population are affected by dementia globally. One of the most important neurodegenerative diseases is Alzheimer’s disease which is known for its effect on memory and cognitive impairment. Alzheimer’s disease (AD) is an area of intense scientific investigation due to its high prevalence and the lack of a definitive cure. Amyloid precursor protein plays a central role in Alzheimer’s …
Published in International Journal of Brain Sciences · Vol. 3, Issue 1, 2026 · pp. 15–26 Read article
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In silico analysis of Abrus precatorius L. as a potential agonist of PPARγ : A novel approach to the treatment of diabetes
Abstract: Diabetes mellitus is a chronic disorder that is characterized by a lack of insulin secretion by the pancreas or a defect in insulin action, or both. If diabetes is not controlled, over time it can cause damage to blood vessels and nerves, leading to life-threatening complications such as, kidney damage, heart disease and vision impairment. It can also weaken the immune system, making patients more prone to infection. Although treatments …
Published in International Journal of Molecular Biotechnological Research · Vol. 3, Issue 2, 2025 Read article
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Assessment of Finerenone Safety and Efficacy in Individuals with Type 2 Diabetes and Chronic Kidney Disease
Abstract: Background: In this work, we provide strong evidence for the safety and efficacy of finerenone in people with type 2 diabetes and chronic kidney disease. Our goal is to improve patients' quality of life and general well-being through our research. Aim: Finerenone exhibited a significant decrease in the likelihood of renal and cardiovascular (CV) events in individuals with both type 2 diabetes and chronic kidney disease. This exploratory subgroup analysis …
Published in International Journal of Antibiotics · Vol. 1, Issue 2, 2024 · pp. 06–09 Read article
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Role of Gastric Receptors in Gastrointestinal Disorder
Abstract: The established and potential roles of cholecystokinin1 and cholecystokinin2 receptors in gastrointestinal and metabolic diseases are analyzed, along with findings from human studies involving agonists and antagonists. While there is considerable evidence implicating cholecystokinin1R in various diseases such as pancreatic disorders, motility disorders, tumor growth, satiety regulation, and cholecystokinin-deficient states, its specific role in these conditions remains ambiguous. Conversely, the role of cholecystokinin2R in physiological (e.g., atrophic gastritis) and pathological …
Published in International Journal of Biomedical Innovations and Engineering · Vol. 2, Issue 2, 2024 · pp. 37–49 Read article
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Molecular Dynamics and Therapeutic Architectures of Cannabinoid Receptors: A Comprehensive Review
Abstract: Expanding on these foundations, recent structural biology studies using cryo-electron microscopy have provided high-resolution insights into the conformational dynamics of CB₁ and CB₂ receptors. These findings have enabled a more precise understanding of ligand–receptor interactions, particularly how agonists, antagonists, and reverse agonists stabilize distinct receptor states. Such knowledge is critical for rational drug design, allowing researchers to selectively modulate downstream signaling pathways. For instance, CB₁ receptors primarily couple to Gi/o …
Published in International Journal of Cheminformatics · Vol. 4, Issue 1, 2026 · pp. 36–40 Read article
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The Evolution of Asthma Management: A Comprehensive Analysis of GINA 2024 Guidelines, Endotype-Driven Diagnosis, and Targeted Biologic Intervention
Abstract: Asthma remains a substantial global public health challenge, characterized by heterogeneous airway inflammation leading to variable airflow obstruction. Recent advances in personalized medicine and guideline revisions, notably the Global Initiative for Asthma (GINA) 2024 update, mandate a profound paradigm shift from reliance on short-acting beta2-agonists (SABA) to antiinflammatory reliever (AIR) strategies utilizing inhaled corticosteroid (ICS)-formoterol. This report provides an exhaustive analysis of current asthma epidemiology, molecular pathogenesis distinguishing between Type …
Published in Recent Trends in Infectious Diseases · Vol. 3, Issue 2, 2026 Read article