ChemMedChem
Dipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, Via Orabona 4, 70125, Bari, Italy.
Published: May 2022
Mounting evidence suggests that the serotonin system serves in signal transmission to regulate insulin secretion in pancreatic islets of Langerhans. Among the 5-HT receptor subtype found in pancreatic islets, serotonin receptor 1A (5-HT ) demonstrates a unique ability to inhibit β-cell insulin secretion. We report the design, synthesis, and characterization of two novel fluorescent probes for the 5-HT receptor. The compounds were prepared by conjugating the scaffold of the 5-HT receptor agonist 8-OH-DPAT with two fluorophores suitable for live-cell imaging. Compound 5a {5-(dimethylamino)-N-[5-[(8-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)amino]pentyl]naphtalen-1-sulfonammide} showed high affinity for the 5-HT receptor (K =1.8 nM). Fluoroprobe 5a was able to label the 5-HT receptor in pancreatic islet cell cultures in a selective manner, as the fluorescence emission was significantly attenuated by co-administration of the 5-HT receptor antagonist WAY-100635. Thus, fluoroprobe 5a showed useful properties to further characterize this unique receptor's role.
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http://dx.doi.org/10.1002/cmdc.202100759 | DOI Listing |
Medicina (Kaunas)
January 2025
Faculty of Medicine, Transilvania University of Brasov, 500036 Braşov, Romania.
: Endothelial dysfunction (ED) and oxidative stress play major contributions in the initiation and progression of atherosclerosis. Diabetes is a pathological state associated with endothelial damage and enhanced oxidative stress. This study evaluated endothelial dysfunction and oxidative stress in patients with severe coronary artery disease (CAD) undergoing coronary artery bypass graft (CABG) surgery, comparing those with and without type 2 diabetes mellitus (T2DM).
View Article and Find Full Text PDFBiomolecules
December 2024
Neurochemical Research Unit and Bebensee Schizophrenia Research Unit, Department of Psychiatry and Neuroscience and Mental Health Institute, University of Alberta, Edmonton, AB T6G 2G3, Canada.
Schizophrenia is a complex heterogenous disorder thought to be caused by interactions between genetic and environmental factors. The theories developed to explain the etiology of schizophrenia have focused largely on the dysfunction of neurotransmitters such as dopamine, serotonin and glutamate with their receptors, although research in the past several decades has indicated strongly that other factors are also involved and that the role of neuroglial cells in psychotic disorders including schizophrenia should be given more attention. Although glia were originally thought to be present in the brain only to support neurons in a physical, metabolic and nutritional capacity, it has become apparent that these cells have a variety of important physiological roles and that abnormalities in their function may make significant contributions to the symptoms of schizophrenia.
View Article and Find Full Text PDFBrain Res Bull
January 2025
Department of Radiology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China. Electronic address:
Background: Increasing evidence has documented cortical involvement at all stages of PD. The local vulnerabilities within certain brain regions in PD have been previously demonstrated, whereas its underlying genetic and neurochemical factors remain unclear. This study aims to investigate the spatial spectrum of cortical atrophy in Parkinson's disease (PD) and link these variances in gray matter properties and curvature respectively to putative molecular pathways and neurotransmitter factors.
View Article and Find Full Text PDFEur J Pharmacol
January 2025
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
Buspirone, a commonly prescribed medication for generalized anxiety disorder (GAD), is gaining attention for its narrow window of side effects such as lack of physical dependence, non-sedative properties as compared to other anxiolytic drugs. Its dose-specific therapeutic effects beyond anxiety highlights its clinical significance. Pharmacologically, buspirone activates serotonin-1A pre-synaptic autoreceptors and post-synaptic heteroreceptors which modulate serotonergic neurotransmission induced behavioral changes such as anxiolytic and nootropic effects.
View Article and Find Full Text PDFJ Microbiol Biotechnol
November 2024
Department of Biotechnology and Department of Integrative Food, Bioscience and Biotechnology (BK21 FOUR), Chonnam National University, Gwangju 61186, Republic of Korea.
This study investigates the modulatory effects of nicergoline, a major bioactive compound derived from ergot fungus, on the 5-hydroxytryptamine 3A (5-HT3A) receptor. Utilizing a two-electrode voltage-clamp technique, we evaluated the impact of nicergoline on the 5-HT-induced inward current (I) in 5-HT3A receptors. Our findings reveal that nicergoline inhibits I in a reversible and concentration-dependent manner.
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