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Discovery of Novel Na1.7-Selective Inhibitors with the 1-Indole-3-Propionamide Scaffold for Effective Pain Relief.
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College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
Na1.7 is considered a promising target for developing next-generation analgesic drugs, given its critical role in human pain pathologies. Although most reported inhibitors with strong in vitro activity and high selectivity share the aryl sulfonamide scaffold, they failed to demonstrate marked clinical efficacy.
View Article and Find Full Text PDFLeveraging Model-Based Simulations to Optimize Extended Dosing of Leuprolide 6-Month Intramuscular Depot Formulation.
Eur J Drug Metab Pharmacokinet
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School of Pharmacy, National Defense Medical Center, Taipei, Taiwan.
Background And Objective: A gonadotropin-releasing hormone (GnRH) agonist such as leuprolide is widely used to achieve sustained suppression of testosterone levels, which play a critical role in the treatment of prostate cancer. Recent advances in drug delivery systems have led to the development of long-acting depot formulations, such as the 6-month intramuscular (IM) leuprolide formulation, which aim to simplify dosing and improve convenience for both patients and healthcare providers. Exploring extended dosing intervals for such formulations represents a promising approach to further optimize treatment regimens, potentially balancing efficacy with patient-centered care.
View Article and Find Full Text PDFThe role of weak interactions in evaluation of inhibitory potential of Indinavir as an HIV protease inhibitor and its comparison with innovative drug candidates.
Comput Biol Med
January 2025
Department of Chemistry, Graduate University of Advanced Technology, Kerman, Iran.
Designing and employing enzyme inhibitors against viral enzymes is one of the innovative and efficient approaches to treating viral diseases. These inhibitors can disrupt the viral replication cycle by deactivating vital enzymes, thereby curbing the spread of viral infections by reducing their population. So far, inhibitors have been designed, validated, and introduced for these enzymes.
View Article and Find Full Text PDFTranexamic dosing for major joint arthroplasty in adult patients with chronic kidney disease: A pharmacokinetic study and new dosing regimen.
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View Article and Find Full Text PDFChemical Profiling, Antioxidant, and Antiproliferative Activities of Algerian Cistus creticus L. Leaf Extracts: Evidence from In vitro and In Silico Studies.
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Medicinal Chemistry Department, Theodor Bilharz Research Institute Kornaish El Nile, Warrak El-Hadar, Imbaba (P.O. 30), Giza 12411, Egypt.
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