Medicinal Chemistry Insights in Neuronal Nitric Oxide Synthase Inhibitors Containing Nitrogen Heterocyclic Compounds: A Mini Review.

Many scientific reports over the last two decades have focused on the discovery and development of novel nNOS inhibitors. The structural identity of isoforms, bioavailability, pharmacokinetic, and safety profile issues remain major obstacles in the discovery of more potent and selective nNOS inhibitors. This review aims to provide an in-depth overview of the molecular interaction patterns between nNOS active site and inhibitors containing structurally diverse nitrogen heterocyclic compounds and highlight the structural properties needed to develop selective nNOS inhibitors.

Extract Loaded Gel: Formulation, and Evaluation of Anti-Inflammatory Properties.

The objective of the study was to develop a novel topical gel by mixing ethanolic extract, thermosensitive poloxamer 407, and carbomer 940 and evaluating its stability and rheological behavior. The irritation potential of the gel was evaluated in accordance with the Organization for Economic Cooperation and Development Guidelines 404. The potential anti-inflammatory effects of the developed gel were evaluated in rats using the carrageenan-induced paw edema test.

Prolonged intermittent theta burst stimulation restores the balance between A2AR- and A1R-mediated adenosine signaling in the 6-hydroxidopamine model of Parkinson's disease.

JOURNAL/nrgr/04.03/01300535-202507000-00027/figure1/v/2024-09-09T124005Z/r/image-tiff An imbalance in adenosine-mediated signaling, particularly the increased A2AR-mediated signaling, plays a role in the pathogenesis of Parkinson's disease. Existing therapeutic approaches fail to alter disease progression, demonstrating the need for novel approaches in PD.

Newly Developed Semi-Solid Formulations Containing Extract: Characterization, Assessment of Stability, Safety, and Anti-Inflammatory Activity.

has been traditionally used as an anti-inflammatory agent; nevertheless, a comprehensive evaluation of its efficacy and safety and comparison with standard drugs are lacking. Taking into consideration concerns with current therapies, like efficacy limitations, side effects, and resistance, we aimed to develop a natural gel and cream based on extract and explore their anti-inflammatory potential. After the chemical analysis of the extract confirmed the presence of coumarin, -coumaric acid, gallic acid, and quercetin, formulations were prepared and subjected to physical and chemical stability evaluations over 6 months.

Impaired olfactory performance and anxiety-like behavior in a rat model of multiple sclerosis are associated with enhanced adenosine signaling in the olfactory bulb via AR, AR, and AR.

The present study shows that animals with experimental autoimmune encephalomyelitis (EAE) exhibit olfactory dysfunction and impaired general cognitive abilities, as well as anxiety-like behavior. Olfactory dysfunction occurs on average at 2 dpi, well before the onset of the first motor signs of EAE (8-10 dpi). After the initial olfactory dysfunction, the EAE animals show a fluctuation in olfactory performance that resembles the relapsing-remitting course of human MS.