Substituted 1,4-benzoxazines bearing an amino side chain at the 2-position were prepared and were found to have a moderate activity on intracellular calcium. Of the compounds studied it was found that those which possess a homoveratrylamino moiety exhibited superior potency. The chain length and the nature of the amine (4-fluorophenylpiperazine, 4-fluorobenzhydryloxyethylamine, N-substituted homoveratrylamine) is discussed. The 4-benzyl-3, 4-dihydro-2-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-2H-1, 4-benzoxazine (3c) is the most potent derivative of the series with a ratio of IC50 values against PE (phenylephrine) and K+ of 2.1. Under these test conditions a ratio near 1 indicates potential intracellular calcium activity while a ratio greater than 100 an action on extracellular calcium influx.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm970795t | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Impact of Oxidative Stress and Neuroinflammation on Sarco/Endoplasmic Reticulum Ca-ATPase 2b Downregulation and Endoplasmic Reticulum Stress in Temporal Lobe Epilepsy.
ACS Pharmacol Transl Sci
January 2025
Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER)-Guwahati, Changsari, Kamrup, Assam 781101, India.
Epilepsy is one of the most common neurological disorders. Calcium dysregulation and neuroinflammation are essential and common mechanisms in epileptogenesis. Sarco/endoplasmic reticulum (ER) Ca-ATPase 2b (SERCA2b), a crucial calcium regulatory pump, plays pathological roles in various calcium dysregulation-related diseases.
View Article and Find Full Text PDFRegulation of MAP2, GFAP, and calcium in the CA3 Region Following Kainic Acid Exposure to organotypic hippocampal slice culture.
F1000Res
January 2025
Faculty of Teaching and Education Sciences, Islamic University of Malang, Malang, East Java, Indonesia.
Background: Neurodegeneration due to neurotoxicity is one of the phenomena in temporal lobe epilepsy. Experimentally, hippocampal excitotoxicity process can occur due to kainic acid exposure, especially in the CA3 area. Neuronal death, astrocyte reactivity and increased calcium also occur in hippocampal excitotoxicity, but few studies have investigated immediate effect after kainic acid exposure.
View Article and Find Full Text PDFThe involvements of intracellular basal calcium and membrane potential in para-phenylenediamine-impaired sperm function.
Transl Androl Urol
December 2024
Center for Reproductive Medicine, Affiliated Hospital of Nantong University, Nantong, China.
Background: Para-phenylenediamine (PPD) is a crystalline solid that belongs to the aromatic amine group, widely used in the manufacturing of various dyes. PPD exhibits toxic effects on female hormone stability, ovarian function, and embryo development. Although studies have shown that PPD exposure can damage oocyte quality in female mice, research on its effects on male reproductive capability, particularly on human sperm quality and function, is limited.
View Article and Find Full Text PDFRecombinant Klotho administration after myocardial infarction reduces ischaemic injury and arrhythmias by blocking intracellular calcium mishandling and CaMKII activation.
J Pathol
January 2025
Cardiorenal Translational Laboratory, Imas12 Research Institute, Hospital Universitario 12 de Octubre, Madrid, Spain.
Ischaemic heart disease (IHD) remains a major cause of death and morbidity. Klotho is a well-known anti-ageing factor with relevant cardioprotective actions, at least when renal dysfunction is present, but its actions are much less known when renal function is preserved. This study investigated Klotho as a biomarker and potential novel treatment of IHD-associated complications after myocardial infarction (MI) under preserved renal function.
View Article and Find Full Text PDFWidespread occurrence and relevance of phosphate storage in foraminifera.
Nature
January 2025
SUGAR, X-star, Japan Agency for Marine-Earth Science and Technology (JAMSTEC), Yokosuka, Japan.
Foraminifera are ubiquitous marine protists that intracellularly accumulate phosphate, an important macronutrient in marine ecosystems and in fertilizer potentially leaked into the ocean. Intracellular phosphate concentrations can be 100-1,000 times higher than in the surrounding water. Here we show that phosphate storage in foraminifera is widespread, from tidal flats to the deep sea.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!