The development of new μ-opioid receptor (MOR) antagonists has been stimulated by the opioid overdose crisis. Our earlier in silico investigations on ligand-MOR receptor interactions indicated that the ligand cis-equatorial conformation of the amine and phenol is the most likely orientation observed within the MOR receptor. Here, we synthesized and characterized AT-99 [3-(1,3-dimethyl-cis-5-(methyl(phenethyl)amino)cyclohexyl)phenol] as a new in vivo and in vitro MOR antagonist.
View Article and Find Full Text PDFWe present a novel method for the fabrication of ultra-uniform metasurfaces through the direct electrostatic self-assembly of positively charged gold nanoparticles (AuNPs) on chemically unmodified glass. The method was successfully applied to two types of ultra-uniform AuNPs like nanospheres and nanocubes differing in shape, size, and cationic surfactant ligands, proving the versatility of the proposed methods. Unlike previous studies, we found that the AuNP clustering was due to improper drying of the metasurfaces after the deposition and not to instability of the colloids.
View Article and Find Full Text PDFGastric cancer (GC) is a highly aggressive disease often complicated by resistance to chemotherapy agents like paclitaxel (PTX), which targets microtubules to induce apoptosis. Resistance arises through complex molecular mechanisms, including the overexpression of pro-angiogenic factors (VEGFA, ANG-2), activation of survival pathways (PDGFRβ, PPARγ), and epithelial-mesenchymal transition (EMT) driven by proteins such as VIM, E-CAD, N-CAD, and FLOT-1. The extracellular matrix (ECM), regulated by COL1A1 and influenced by PPARγ, acts as a physical barrier to drug penetration.
View Article and Find Full Text PDFPurpose Of Review: This narrative review comprehensively analyzes VLEKT as an advanced nutritional strategy for obesity management. The focus is on the beneficial effects on key disease organs, such as adipose tissue and liver, as well as the modulation of intestinal permeability and its fundamental role in influencing the gut microbiota and inflammatory pathways.
Recent Findings: The impact of VLEKT on obesity-related comorbidities, including metabolic syndrome, cardiovascular disease, endocrine disorders, metabolic dysfunction-associated steatotic liver disease (MASLD), neurological disorders, and kidney alterations, is also investigated.
25I-NBOMe (4-Iodo-2,5-dimethoxy-N-(2-methoxybenzyl) phenethylamine) is a synthetic psychedelic compound abused for its ambiguous legal state as a counterfeit lysergic acid diethylamide (LSD). 25I-NBOMe acts as a selective agonist of 5HT receptors leading to hallucinations, intoxications, and fatalities. Here, we assessed the rewarding properties of 25I-NBOMe and its behavioral and neurotoxic acute effects on the central nervous system of C57BL/6J mice.
View Article and Find Full Text PDF: Horseradish ( L.) roots-largely used in traditional medicine for their multiple therapeutic effects-are a rich source of health-promoting phytochemicals. However, their efficacy can be compromised by low chemical stability and poor bioavailability.
View Article and Find Full Text PDFBackground: The recently published New Italian version of the Wilkins Rate of Reading Test (standard Italian WRRT) was designed to measure reading speed in repeated-measures designs in research and/or clinical examinations. The test features 15 equivalent 10-line passages made up of unrelated words, adhering to the principles established by the Wilkins Rate of Reading Test in English (original WRRT).
Aim: To develop a short Italian version of the WRRT (SI-WRRT), and to determine the equivalence across the new, shorter passages of text.
Am J Transplant
May 2025
Int J Mol Sci
September 2024
Evidence suggests that angiotensin-converting enzyme inhibitors (ACEIs) may increase metabolic rate by promoting thermogenesis, potentially through enhanced fat oxidation and improved insulin. More research is, however, needed to understand this intricate process. In this study, we used 22 lines from the Genetic Reference Panel to assess the metabolic rate of virgin female and male flies that were either fed a standard medium or received lisinopril for one week or five weeks.
View Article and Find Full Text PDFThe use of synthetic cannabinoid receptor agonists (SCRAs) represents a public health concern. Besides abuse liability and cognitive impairments, SCRAs consumption is associated with serious medical consequences in humans, including cardiotoxicity. The precise mechanisms underlying cardiac or other toxicities induced by SCRAs are not well understood.
View Article and Find Full Text PDFLung cancer presents significant therapeutic challenges, motivating the exploration of novel treatment strategies. Programmed cell death (PCD) mechanisms, encompassing apoptosis, autophagy, and programmed necrosis, are pivotal in lung cancer pathogenesis and the treatment response. Dysregulation of these pathways contributes to tumor progression and therapy resistance.
View Article and Find Full Text PDFObjective: Bariatric surgery induces a significant loss of both fat mass (FM) and fat-free mass (FFM). The proteoglycan receptor syndecan-4 (SDC4) plays a crucial role in adipose tissue and skeletal muscle functions. Thus, this study was performed (i) to assess plasma SDC4 levels after both Sleeve Gastrectomy (SG) and Roux-en-Y Gastric Bypass (RYGB) surgeries, and (ii) to explore potential associations with changes in body composition variables.
View Article and Find Full Text PDFBackground: The proliferation of novel psychoactive substances (NPS) in the drug market raises concerns about uncertainty on their pharmacological profile and the health hazard linked to their use. Within the category of synthetic stimulant NPS, the phenethylamine 2-Cl-4,5-methylenedioxymethamphetamine (2-Cl-4,5-MDMA) has been linked to severe intoxication requiring hospitalization. Thereby, the characterization of its pharmacological profile is urgently warranted.
View Article and Find Full Text PDFThe intestine is essential for the modulation of nutrient absorption and the removal of waste. Gut pathologies, such as cancer, inflammatory bowel diseases (IBD), irritable bowel syndrome (IBS), and celiac disease, which extensively impact gut functions, are thus critical for human health. Targeted drug delivery is essential to tackle these diseases, improve therapy efficacy, and minimize side effects.
View Article and Find Full Text PDFA timely detection of visual hemifield deficits (VHFDs; hemianopias or quadrantanopias) is critical for both the diagnosis and treatment of stroke patients. The present study determined the sensitivity and specificity of four qualitative visual field tests, including face description, confrontation tests (finger wiggle), and kinetic boundary perimetry, to screen large and dense VHFDs in right-brain-damaged (RBD) stroke patients. Previously, the accuracy of qualitative visual field tests was examined in unselected samples of patients with heterogeneous aetiology, in which stroke patients represented a very small fraction.
View Article and Find Full Text PDFThe use of synthetic cannabinoid receptor agonists (SCRAs) poses major psychiatric risks. We previously showed that repeated exposure to the prototypical SCRA JWH-018 induces alterations in dopamine (DA) transmission, abnormalities in the emotional state, and glial cell activation in the mesocorticolimbic DA circuits of rats. Despite growing evidence suggesting the relationship between substance use disorders (SUD) and neuroinflammation, little is known about the impact of SCRAs on the neuroimmune system.
View Article and Find Full Text PDFMech Ageing Dev
April 2024
The recently identified syndrome known as Long COVID (LC) is characterized by a constellation of debilitating conditions that impair both physical and cognitive functions, thus reducing the quality of life and increasing the risk of developing the most common age-related diseases. These conditions are linked to the presence of symptoms of autonomic dysfunction, in association with low cortisol levels, suggestive of reduced hypothalamic-pituitary-adrenal (HPA) axis activity, and with increased pro-inflammatory condition. Alterations of dopamine and serotonin neurotransmitter levels were also recently observed in LC.
View Article and Find Full Text PDFBackground: Severe acquired brain injury (sABI) encompasses a range of neurological impairments. Visual dysfunction, particularly homonymous visual field defects (HVFDs) and homonymous hemianopia (HH), commonly afflicts sABI survivors, affecting their cognitive and motor rehabilitation. This study presents the FunctionaL Assessment Scale of Hemianopia (FLASH), developed to analyze the most common postural behaviors exhibited by sABI patients with hemianopia during activities of daily living.
View Article and Find Full Text PDFDiabetol Metab Syndr
August 2023
Diabetol Metab Syndr
July 2023
Background: Syndecan-4 (SDC4) is a member of the heparan sulfate proteoglycan family of cell-surface receptors. We and others previously reported that variation in the SDC4 gene was associated with several components of the metabolic syndrome, including intra-abdominal fat, fasting glucose and triglyceride levels, and hypertension, in human cohorts. Additionally, we demonstrated that high fat diet (HFD)-induced obese female mice with a Sdc4 genetic deletion had higher visceral adiposity and a worse metabolic profile than control mice.
View Article and Find Full Text PDFThe increasing misuse of novel synthetic opioids (NSOs) represents a serious public health concern. In this regard, U-47700 (trans-3,4-dichloro-N-[2-(dimethylamino)cyclohexyl]-N-methylbenzamide) and related "U-compounds" emerged on recreational drug markets as synthetic substitutes for illicit heroin and constituents of counterfeit pain medications. While the pharmacology of U-compounds has been investigated using in vitro and in vivo methods, there is still a lack of understanding about the details of ligand-receptor interactions at the molecular level.
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