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Advanced pharmacological and pharmacokinetic evaluation of 1,3 dimethylpurine-2,6-dione derivative (GR-14) with prominent mood-modulating activity in rats.
Pharmacol Rep
December 2024
Department of Clinical Pharmacy, Faculty of Pharmacy, Medical College, Jagiellonian University, Medyczna 9, Kraków, 30-688, Poland.
Background: Research on new candidates for antidepressant/anxiolytic drugs from the long-chain arylpiperazines (LCAPs) group containing a 1,3-dimethylpurine-2,6-dione as a terminal amide fragment fits into the modern exploration trend. This study aimed to examine, for the first time in male Wistar rats, pharmacodynamic (antidepressant- and anxiolytic-like) and pharmacokinetic properties of 7-(5-(4-(3-chlorophenyl)piperazin-1-yl)pentyl)-1,3-dimethyl-3,7-dihydro-1 H-purine-2,6-dione hydrochloride (GR-14).
Methods: Antidepressant- and anxiolytic-like activities have been assessed in the forced swim test (FST) and Vogel conflict drinking test, respectively.
Discovery of New 3-(Benzo[]Thiophen-2-yl)Pyrrolidine-2,5-Dione Derivatives as Potent Antiseizure and Antinociceptive Agents-In Vitro and In Vivo Evaluation.
Pharmaceuticals (Basel)
November 2024
Department of Medicinal Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.
: To address the unmet clinical needs in the treatment of epilepsy and pain, the continued development of more effective and safer anticonvulsants and analgesics is still necessary. Therefore, herein we report synthesis and antiseizure/antinociceptive evaluation of a focused series of 3-(benzo[b]thiophen-2-yl)pyrrolidine-2,5-dione derivatives. : The anticonvulsant properties were investigated in acute models of seizures, namely the maximal electroshock (MES), the 6 Hz (32 mA), and subcutaneous pentylenetetrazole (PTZ) seizure models, whereas analgesic activity was tested in the model of a tonic pain/formalin test and oxaliplatin-induced neuropathic pain (in CD-1-mice, i.
View Article and Find Full Text PDFConstruction of a pumpless gravity-driven vascularized Skin-on-a-Chip for the study of hepatocytotoxicity in percutaneous exposure to exogenous chemicals.
Biomed Microdevices
September 2024
Department of Health Toxicology, College of Naval Medicine, Naval Medical University, Shanghai, 200433, China.
Article Synopsis
- Existing Skin-on-a-Chip (SoC) technology faces limitations due to complex structures and the need for multiple devices, hindering the assessment of harmful chemicals that impact liver health after skin contact.
- A new gravity-driven SoC was developed, featuring three layers of cell chambers (human skin, blood vessel cells, and liver cells) that allows for effective study of liver toxicity from exogenous chemicals, with validation through specific parameters.
- This SoC accurately mimics the way chemicals are absorbed through the skin, processed in the bloodstream, and affect the liver, offering a potential substitute for animal testing in evaluating the safety of skin-penetrating chemicals.
Isobavachin induces autophagy-mediated cytotoxicity in AML12 cells via AMPK and PI3K/Akt/mTOR pathways.
Toxicol In Vitro
October 2024
Center of Drug Safety Evaluation, Tianjin University of Traditional Chinese Medicine, Tianjin, China; National Key Laboratory of Chinese Medicine Modernization, Tianjin University of Traditional Chinese Medicine, Tianjin, China; State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China. Electronic address:
Article Synopsis
- Isobavachin (IBA) is a dihydroflavonoid with potential healh benefits, but its hepatotoxic effects need more research.
- The study evaluated IBA’s impact on liver cell viability, revealing it has dose-dependent toxic effects and induces autophagy in specific liver cells.
- Findings suggest that IBA inhibits key signaling proteins related to cell survival, but targeting certain pathways could help mitigate its liver toxicity, offering insights for clinical prevention and treatment.
Combination of biotransformation and metabolomics reveals tolfenpyrad-induced hepatocytotoxicity.
Sci Total Environ
November 2024
National Center of Biomedical Analysis, Beijing 100039, China. Electronic address:
Tolfenpyrad (TFP) is an extensively used pesticide that inevitably leads to human exposure to both TFP and its transformation product residues. However, the biotransformation of TFP in humans has not been elucidated, and the toxicity of TFP along with its biotransformation products remains largely unknown. In this study, the biotransformation process of TFP was investigated using human liver microsomes and human hepatic cells.
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