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Design of ()-3-(5-Thienyl)carboxamido-2-aminopropanoic Acid Derivatives as Novel NMDA Receptor Glycine Site Agonists: Variation in Molecular Geometry to Improve Potency and Augment GluN2 Subunit-Specific Activity.
J Med Chem
January 2025
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, DK-2100, Denmark.
NMDA receptor ligands have therapeutic potential in neurological and psychiatric disorders. We designed ()-3-(5-thienyl)carboxamido-2-aminopropanoic acid derivatives with nanomolar agonist potencies at NMDA receptor subtypes (GluN12/A-D). These compounds are superagonists at GluN1/2C compared to glycine and partial to full agonists at GluN1/2A and GluN1/2D but display functional antagonism at GluN1/2B due to low agonist efficacy.
View Article and Find Full Text PDFA complete sojourn on nanotechnological advancements and nanocarrier applications in psoriasis management.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Pharmaceutics, ISF College of Pharmacy, GT Road, Moga, 142001, Punjab, India.
Psoriasis, a chronic autoimmune and non-communicable skin disease, affects 2-3% of the global population, creating a significant financial burden on healthcare systems worldwide. Treatment approaches are categorized based on disease severity, with first-line therapy focusing on topical treatments and second-line therapy encompassing phototherapy, systemic therapy, and biological therapy. Transdermal drug delivery methods present a promising alternative by enhancing drug absorption through the skin, potentially improving therapeutic outcomes while minimizing systemic adverse effects.
View Article and Find Full Text PDFIntegration of Asymmetric Multi-Path Hollow Structure and Multiple Heterogeneous Interfaces in FeO@C@NiO Nanoprisms Enabling Ultra-Low and Broadband Absorption.
Small
January 2025
Key Laboratory of Aerospace Materials and Performance (Ministry of Education) School of Materials Science and Engineering, Beihang University, No.37 Xueyuan Road, Beijing, 100191, P. R. China.
A reasonable construction of hollow structures to obtain high-performance absorbers is widely studied, but it is still a challenge to select suitable materials to improve the low-frequency attenuation performance. Here, the FeO@C@NiO nanoprisms with unique tip shapes, asymmetric multi-path hollow cavity, and core-shell heteroepitaxy structure are designed and synthesized based on anisotropy and intrinsic physical characteristics. Impressively, by changing the load of NiO, the composites achieve strong absorption, broadband, low-frequency absorption: the reflection loss of -55.
View Article and Find Full Text PDFThe Pharmacokinetic Changes in Cystic Fibrosis Patients Population: Narrative Review.
Medicines (Basel)
December 2024
Pharmacy School, West Coast University, Los Angeles, CA 90004, USA.
Cystic fibrosis (CF) is a rare genetic disorder commonly affecting multiple organs such as the lungs, pancreas, liver, kidney, and intestine. Our search focuses on the pathophysiological changes that affect the drugs' absorption, distribution, metabolism, and excretion (ADME). This review aims to identify the ADME data that compares the pharmacokinetics (PK) of different drugs in CF and healthy subjects.
View Article and Find Full Text PDFAnalytical sensitivity factors from distributions of time of flight of photons for near-infrared spectroscopy studies in multilayered turbid media.
J Biomed Opt
January 2025
CIFICEN (UNCPBA - CICPBA - CONICET), Tandil, Argentina.
Significance: In the last years, time-resolved near-infrared spectroscopy (TD-NIRS) has gained increasing interest as a tool for studying tissue spectroscopy with commercial devices. Although it provides much more information than its continuous wave counterpart, accurate models interpreting the measured raw data in real time are still lacking.
Aim: We introduce an analytical model that can be integrated and used in TD-NIRS data processing software and toolkits in real time.
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