During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were prepared and evaluated in an attempt to also improve the cardiovascular safety profile over lead arylamide 1, which possessed ion channel activity. The resultant compounds retained excellent potency and exhibited diminished ion channel activity.
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http://dx.doi.org/10.1016/j.bmcl.2010.05.013 | DOI Listing |
Brain Res
December 2024
Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen 2100, Denmark. Electronic address:
Psychedelics show promise in treating psychiatric disorders. Therapeutic effects appear to involve activation of the 5-Hydroxytryptamine 2A receptor (5-HTR), a G protein-coupled receptor (GPCR). Several SNPs of the 5-HTR naturally occur, which are associated with differences in receptor function and altered responsiveness to treatments.
View Article and Find Full Text PDFPlant Physiol Biochem
December 2024
College of Landscape Architecture, Sichuan Agricultural University, Chengdu, Sichuan, 611130, China. Electronic address:
Moderate mowing of the shoot is an effective strategy for improving Pb-contaminated soil remediation using bermudagrass. However, the mechanisms by which mowing facilitates Pb uptake and accumulation remain insufficiently understood. Root radial transport is critical in efficient heavy metal uptake and translocation in plants and is influenced by root physiological-biochemical characteristics.
View Article and Find Full Text PDFBiomed Pharmacother
December 2024
Department of Biology, University of Naples Federico II, Naples, Italy; Biogem, Istituto di Biologia e Genetica Molecolare, Ariano Irpino, AV, Italy.
Intracellular Ca homeostasis dysregulation, through the modulation of calcium permeable ion channels and transporters, is gaining attention in cancer research as an apoptosis evasion mechanism. Recently, we highlighted a prognostic role for several calcium permeable channels. Among them, here, we focused on the plasma membrane bidirectional Na/Ca exchanger SLC8A1.
View Article and Find Full Text PDFDev Cell
December 2024
Edwin L. Steele Laboratories, Department of Radiation Oncology, Massachusetts General Hospital Cancer Center, Massachusetts General Hospital and Harvard Medical School, Boston, MA 02114, USA. Electronic address:
Lymphatic muscle cells (LMCs) within the wall of collecting lymphatic vessels exhibit tonic and autonomous phasic contractions, which drive active lymph transport to maintain tissue-fluid homeostasis and support immune surveillance. Damage to LMCs disrupts lymphatic function and is related to various diseases. Despite their importance, knowledge of the gene transcriptional signatures in LMCs and how they relate to lymphatic function in normal and disease contexts is largely missing.
View Article and Find Full Text PDFAnn Med
December 2025
Department of Anatomy, College of Medicine, King Khalid University, Abha, Saudi Arabia.
Background: Substance use disorders are multifaceted conditions influenced by both genetic and environmental factors. Serotonergic pathways are known to be involved in substance use disorder susceptibility, with genetic markers within serotonin receptor genes identified as potential risk factors.
Methods: To further explore this relationship, we conducted a study to investigate the association between several polymorphisms in five serotonin receptor genes (, , ) and substance use disorders (SUD) in Jordanian males by sequencing genotypes in 496 SUD patients and 496 healthy controls.
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