Felodipine is a Calcium blocker and nitroglycerin, a nitrate vasodilating agent, were compared. Two parameters were studied in vitro on bovine aortic media. Calcium uptake and vascular tone. The Calcium uptake measurement was performed by incubating in Krebs solution small slices of the preparation in the presence of 45Ca. Studies on vascular tone were performed on deendothelialized bovine aortic rings suspended in Krebs solution. Felodipine (1nM-100microM) decreases Ca2+ uptake and relaxes the preparation while nitroglycerin's 1nM-100microM) action is also inhibiting but very weak. When the preparation is stimulated by alpha 1-adrenergic against phenylephrine 1microM, then nitroglycerin 100microM has a much stronger inhibiting effect on Call uptake and vascular tone than felodipine 100microM. These results are reversed when the preparation is stimulated by KC165.4mM. Then felodipine 100nM exerts a strong inhibiting effect on Ca2+ uptake and vascular tone while nitroglycerin's 100nM inhibiting action is very weak. It is well known that in cases of endothelium disfunction the adrenergic stimulation provokes vasoconstriction and ischemia. This ischemia induces a second phase of vasoconstriction that is due to a depolarization provoked by the increased levels of extracellular K+. Felodipine is able to antagonize the consequences of such a depolarization. Thus, felodipine may be useful as an additional agent to nitroglycerin's treatment and that is the clinical message of our findings.
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Vascul Pharmacol
January 2025
Department of Clinical and Biological Sciences, University of Torino, Regione Gonzole 10, 10043 Orbassano, Italy. Electronic address:
The appropriate regulation of peripheral vascular tone is crucial for maintaining tissue perfusion. Myoendothelial junctions (MEJs), specialized connections between endothelial cells and vascular smooth muscle cells, are primarily located in peripheral resistance vessels. Therefore, these junctions, with their key membrane proteins, play a pivotal role in the physiological control of relaxation-contraction coupling in resistance arterioles, mainly mediated through endothelium-derived hyperpolarization (EDH).
View Article and Find Full Text PDFPhytomedicine
December 2024
Univ Coimbra, Coimbra Institute for Clinical and Biomedical Research (iCBR), Faculty of Medicine, Azinhaga de S. Comba, Coimbra 3000-548, Portugal; Univ Coimbra, Center for Innovative Biomedicine and Biotechnology (CIBB), Coimbra, Portugal; Clinical Academic Centre of Coimbra (CACC), Coimbra, Portugal.
Background: Pulmonary Arterial Hypertension (PAH) is characterized by pulmonary vascular remodelling, often associated with disruption of BMPR2/Smad1/5 and BMPR2/PPAR-γ signalling pathways that ultimately lead to right ventricle failure. Disruption of intercellular junctions and communication and a pro-angiogenic environment are also characteristic features of PAH. Although, current therapies improve pulmonary vascular tone, they fail to tackle other key pathological features that could prevent disease progression.
View Article and Find Full Text PDFBasic Clin Pharmacol Toxicol
February 2025
Department of Biomedicine, Aarhus University, Aarhus, Denmark.
The media-lumen diameter ratio of small arteries is increased in hypertension, diabetes and obesity. It is likely that both shear stress on the endothelial cells, transmural pressure and smooth muscle cell tone are important for the altered vascular structure. However, the precise interaction and importance of these factors are incompletely understood.
View Article and Find Full Text PDFActa Physiol (Oxf)
February 2025
Cardiovascular Health Across the Life Span, Research Institute of the McGill University Health Centre, Montreal, Quebec, Canada.
Preserving the balance of metabolic processes in endothelial cells (ECs) and vascular smooth muscle cells (VSMCs), is crucial for optimal vascular function and integrity. ECs are metabolically active and depend on aerobic glycolysis to efficiently produce energy for their essential functions, which include regulating vascular tone. Impaired EC metabolism is linked to endothelial damage, increased permeability and inflammation.
View Article and Find Full Text PDFJ Hypertens
December 2024
Institute for Fetology, The First Affiliated Hospital of Soochow University, Jiangsu.
Background: Paternal preconception alcohol exposure affects fetal development; however, it is largely unknown about the influences on offspring vasculature and mechanisms.
Methods: Offspring born form paternal rats treated with alcohol or water before pregnant was raised until 3 months of age. Vessel tone of mesenteric arteries was detected using myograph system; whole-cell calcium channel current in smooth muscle cells was tested using patch-clamp; molecule expressions were detected with real-time PCR, western blotting, and Dihydroethidium (DHE); DNA methylations were determined using targeted bisulfate sequencing assay.
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