Two different potency tests were evaluated, consisting in one-dilution used to determine 50% lethal dose (LD50) and four--dilution used to calculate 50% effective dose (ED50), respectively. Our experience has led to propose the four-dilution test for routine lot releasing.
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ACS Pharmacol Transl Sci
January 2025
Department of Medicinal Chemistry and Institute for Translational Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Opioid agonist ligands bind opioid receptors and stimulate downstream signaling cascades for various biological processes including pain and reward. Historically, before cloning the receptors, muscle contraction assays using isolated organ tissues were used followed by radiolabel ligand binding assays on native tissues. Upon cloning of the opioid G protein-coupled receptors (GPCRs), cell assays using transfected opioid receptor DNA plasmids became the standard practice including S-GTPγS functional and cAMP based assays.
View Article and Find Full Text PDFChem Biodivers
January 2025
univ oeb, snv, ali menjli, 25000, constantine, ALGERIA.
This study investigates the pharmaceutical potential both in vitro and in silico of ethanolic propolis extract from three Algerian regions namely TAH (Tahir-Jijel), ATH (Oued Athmania-Mila) and OZ (Oued Zhor-skikda). Twenty-three compounds were identified via HPLC‒DAD, with key constituents including caffeic acid, cynarin, chrysin, naringin, and hesperetin. Moreover, Antioxidant and anti-Alzheimer activities were assessed by multiple assays.
View Article and Find Full Text PDFBr J Pharmacol
January 2025
Department of Physiology and Pharmacology, School of Medicine, Tel Aviv University, Tel Aviv, Israel.
Background And Purpose: The antiepileptic drug ethosuximide (ETX) suppresses epileptiform activity in a mouse model of GNB1 syndrome, caused by mutations in Gβ protein, likely through the inhibition of G-protein gated K (GIRK) channels. Here, we investigated the mechanism of ETX inhibition (block) of different GIRKs.
Experimental Approach: We studied ETX inhibition of GIRK channels expressed in Xenopus oocytes with or without their physiological activator, the G protein subunit dimer Gβγ.
Arch Oral Biol
January 2025
Pharmaceutical Sciences and Technology Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand; Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand; Center of Excellent in Natural Products and Nanoparticles (NP2), Chulalongkorn University, Bangkok, Thailand.
Objective: Asiaticoside has the capacity to induce osteogenic differentiation of human periodontal ligament cells (hPDLCs) through Wnt (Wingless-related integration site) signaling. A modified chemical structure (by removing glycoside side chain), referred to as asiatic acid methyl ester (AA1), has been constructed and evaluated for its capacity to induce osteogenic differentiation.
Design: hPDLCs viability was determined by MTT assay.
J Agric Food Chem
January 2025
State Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, Central China Normal University, Wuhan 430079, PR China.
4-Hydroxyphenylpyruvate dioxygenase (HPPD) is a crucial herbicide target in current research, playing an important role in the comprehensive management of resistant weeds. However, the limited crop selectivity and less effectiveness against grass weeds of many existing HPPD inhibitors, limit their further application. To address these issues, a series of novel HPPD inhibitors with fused ring structures were designed and synthesized by introducing an electron-rich indazolone ring and combining it with the classical triketone pharmacophore structure.
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