A new class of methylfuroxans and methylfurazans arylthio, arylsulphinyl and arylsulphonyl substituted, characterized by vasodilating and antiaggregatory properties, is described. Vasodilating activity, tested on rabbit aortic rings percontracted with 1 microM noradrenaline, is enhanced by N-oxidation of the furazan ring and is maximized by increase of the sulphur atom oxidation level. Compounds 4-methyl-3-(p-methoxyphenylsulphonyl) furoxan 6c, 3-phenyl-4-phenylsulphonylfuroxan 10, 4-phenyl-3-phenylsulphonylfuroxan 11 and 3,4-bis(phenyl-sulphonyl)furoxan 12 (EC50 values ranging between 0.055-1.07 microM), seem to be promising since they show the highest potency as well as maximal efficacy, causing complete reversal of noradrenaline induced contraction. The structure-activity relationship, observed in the platelet aggregation test, is substantially similar to that reported for the vasodilating activity, in line with the general profile of these drugs as putative NO-mimetic derivatives.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1006/phrs.1993.1123 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Heat acclimation defense against exertional heat stroke by improving the function of preoptic TRPV1 neurons.
Theranostics
January 2025
Department of Critical Care Medicine and Department of Anaesthesiology, Xijing Hospital, Fourth Military Medical University, Xi'an, Shaanxi, China, 710032.
Record-breaking heatwaves caused by greenhouse effects lead to multiple hyperthermia disorders, the most serious of which is exertional heat stroke (EHS) with the mortality reaching 60 %. Repeat exercise with heat exposure, termed heat acclimation (HA), protects against EHS by fine-tuning feedback control of body temperature (Tb), the mechanism of which is opaque. This study aimed to explore the molecular and neural circuit mechanisms of the HA training against EHS.
View Article and Find Full Text PDFRh-relaxin-2 attenuates oxidative stress and neuronal apoptosis via ERK-nNOS-NO pathway after germinal matrix hemorrhage in rats.
Fluids Barriers CNS
January 2025
Department of Neurosurgery, Institute of Brain Diseases, Nanfang Hospital of Southern Medical University, Guangzhou, 510515, China.
Oxidative stress and neuronal apoptosis could be an important factor leading to post-hemorrhagic consequences after germinal matrix hemorrhage (GMH). Previously study have indicated that relaxin 2 receptor activation initiates anti-oxidative stress and anti-apoptosis in ischemia-reperfusion injury. However, whether relaxin 2 activation can attenuate oxidative stress and neuronal apoptosis after GMH remains unknown.
View Article and Find Full Text PDFApplication of a dynamic colonic gastrointestinal digestion model to red wines: a study of flavanol metabolism by the gut microbiota and the cardioprotective activity of microbial metabolites.
Food Funct
January 2025
Instituto de Ciencias de la Vid y del Vino-ICVV (Consejo Superior de Investigaciones Científicas-CSIC, Universidad de La Rioja-UR, Gobierno de La Rioja), Finca La Grajera, Ctra. de Burgos Km. 6 (LO-20, - salida 13), 26007 Logroño, Spain.
Over the last decade, research has emphasized the role of the microbiome in regulating cardiovascular physiology and disease progression. Understanding the interplay between wine polyphenols, the gut microbiota, and cardiovascular health could provide valuable insights for uncovering novel therapeutic strategies aimed at preventing and managing cardiovascular disease. In this study, two commercial red wines were subjected to dynamic gastrointestinal digestion (GIS) to monitor the flavanol-microbiota interaction by evaluating the resulting microbial metabolites.
View Article and Find Full Text PDFReversal of inflammatory reprogramming by vasodilator agents in pulmonary hypertension.
ERJ Open Res
January 2025
Center for Pulmonary Vascular Biology and Medicine, Pittsburgh Heart, Lung and Blood Vascular Medicine Institute, Division of Cardiology, Department of Medicine, University of Pittsburgh School of Medicine and UPMC, Pittsburgh, PA, USA.
Background: Pulmonary arterial hypertension (PAH) is a deadly disease without effective non-invasive diagnostic and prognostic testing. It remains unclear whether vasodilators reverse inflammatory activation, a part of PAH pathogenesis. Single-cell profiling of inflammatory cells in blood could clarify these PAH mechanisms.
View Article and Find Full Text PDFAdrenomedullin 2 attenuates anxiety-like behaviors by increasing IGF-II in amygdala and re-establishing blood-brain barrier.
Transl Psychiatry
January 2025
Department of Neurosurgery, West China Hospital of Sichuan University, Chengdu, Sichuan, China.
Anxiety disorder, a prevalent mental health issue, is one of the leading causes of disability worldwide. Damage to the blood-brain barrier (BBB) is implicated in anxiety, but its regulatory mechanisms remain unclear. Herein, we show that adrenomedullin 2 (ADM2), a novel angiogenic growth factor, alleviates autistic and anxiety-like behaviors in mice.
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!