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Structural insights into substrate transport and drug inhibition of the human vesicular monoamine transporter 2 (VMAT2).
FEBS J
January 2025
Laboratory of Soft Matter Physics, Institute of Physics, Chinese Academy of Sciences, Beijing, China.
Vesicular monoamine transporter 2 (VMAT2) is a proton-monoamine antiporter that is widely expressed in central and peripheral neurons and plays a crucial role in loading monoamine neurotransmitters into secretory vesicles. Dysfunction of VMAT2 causes many neuropsychiatric disorders, such as depression and Parkinson's disease. Consequently, VMAT2 is a valid and important therapeutic target.
View Article and Find Full Text PDFPolysaccharides from Scrophularia ningpoensis Hemsl. Improve reserpine-induced depression-like behavior by inhibiting HTR2A/HTR2C mediated AKT/GSK3β/β-catenin/CBP/BDNF signaling.
Int J Biol Macromol
January 2025
College of Pharmacy, Jining Medical University, Rizhao, Shandong 276800, PR China; College of Pharmacy, Binzhou Medical University, Yantai, Shandong 264003, PR China; Shandong Collaborative Innovation Center for Diagnosis, Treatment and Behavioral Interventions of Mental Disorders, Institute of Mental Health, Jining Medical University, Jining, Shandong 272067, PR China; Jining Key Laboratory of Depression Prevention and Treatment, Jining Medical University, Jining, Shandong 272067, PR China. Electronic address:
Scrophularia ningpoensis Hemsl. is a traditional Chinese medicine used to regulate blood sugar levels, immunity, etc. We previously isolated polysaccharides from S.
View Article and Find Full Text PDFEvidence for the anxiolytic- and antidepressant-like effects of three semi-synthetic derivatives of xylopic acid in mice.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Pharmacology and Toxicology, School of Pharmacy, University of Health and Allied Sciences, Ho, Ghana.
Purpose: Major depressive disorder is one of the most common and burdensome psychiatric disorders worldwide. This study evaluated the anxiolytic- and antidepressant-like activity of three semi-synthetic derivatives of xylopic acid (XA) to identify the most promising derivative based on mechanism(s) of action, in vivo pharmacokinetics and in vitro cytotoxicity.
Methods: The anxiolytic potential and the involvement of GABAergic mechanisms were assessed in the elevated plus-maze and open field tests in mice.
Method for Testing Drugs Belonging to Substrates and Inhibitors of the Transporter Protein BCRP on CACO-2 Cells.
Dokl Biochem Biophys
January 2025
Ryazan State Medical University, Ryazan, Russian Federation.
Introduction: Breast cancer resistance protein (BCRP) is an efflux membrane transporter that controls the pharmacokinetics of a large number of drugs. Its activity may change when taking some endo- and exogenous substances, thus making it a link in drug interactions.
Aim: The aim of the study was to develop a methodology for testing drugs for belonging to BCRP substrates and inhibitors in vitro.
Characterisation of periorbital mechanical allodynia in the reserpine-induced fibromyalgia model in mice: The role of the Schwann cell TRPA1/NOX1 signalling pathway.
Free Radic Biol Med
January 2025
Graduate Program in Biological Sciences: Toxicological Biochemistry, Centre of Natural and Exact Sciences, Federal University of Santa Maria, Santa Maria, RS, Brazil.
Fibromyalgia (FM) is a complex and multifaceted condition characterized by a range of clinical symptoms, including widespread pain and a strong association with migraine headaches. Recent findings have underscored the role of oxidative stress and transient receptor potential ankyrin 1 (TRPA1) channel in migraine and FM. However, the precise mechanisms underlying the comorbidity between migraine and FM are unclear.
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