Nitroglycerine in doses of 0.4-1.0 mg/kg decreased the heart rate in rats, which was associated with inhibition of adrenergic influences realized via beta-adrenoceptors. The negative chronotropic effect of sodium nitroprusside in a dose of 1 mg/kg was more significant compared to that of nitroglycerine (by 2-3 times). It was associated with inhibition of adrenergic and stimulation of cholinergic influences mediated via beta-adrenoceptors and muscarinic cholinergic receptors, respectively. During blockade of beta-adrenoceptors and muscarinic cholinergic receptors, sodium nitroprusside increased the time of atrioventricular conduction. These data indicate that function of myocytes in the heart conduction system of rats depends on the PQ interval.
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http://dx.doi.org/10.1007/s10517-005-0397-9 | DOI Listing |
J Comput Chem
January 2025
Departamento de Fisicoquímica, Facultad de Química, Universidad Nacional Autónoma de México, Coyoacán, CDMX, Mexico.
The G protein-coupled receptor (GPCR) pharmacology accounts for a significant field in research, clinical studies, and therapeutics. Computer-aided drug discovery is an evolving suite of techniques and methodologies that facilitate accelerated progress in drug discovery and repositioning. However, the structure-activity relationships of molecules targeting GPCRs are highly challenging in many cases since slight structural modifications can lead to drastic changes in biological functionality.
View Article and Find Full Text PDFRev Cardiovasc Med
December 2024
Liver Unit, University of Calgary Cumming School of Medicine, Calgary, AB T2N 4N1, Canada.
Am J Physiol Heart Circ Physiol
February 2025
Department of Basic Medical Sciences, University of Arizona College of Medicine, Phoenix, Arizona, United States.
Autonomic dysfunction is associated with cardiovascular and neurological diseases, including hypertension, heart failure, anxiety, and stress-related disorders. Prior studies demonstrated that late gestation exposure to dexamethasone (DEX) resulted in female-biased increases in stress-responsive mean arterial pressure (MAP) and heart rate (HR), suggesting a role for glucocorticoid-mediated programming of autonomic dysfunction. The present study investigated the influence of sympathetic (SYM) or parasympathetic (PS) blockade on cardiovascular function in male and female rat offspring of mothers injected with DEX in utero [ (GD) -].
View Article and Find Full Text PDFbioRxiv
December 2024
Istanbul Medipol University, School of Engineering and Natural Sciences, Department of Biomedical Engineering, 34810, Istanbul, Turkey.
G protein-coupled receptor (GPCR) signaling is terminated by arrestin binding to a phosphorylated receptor. Binding propensity has been shown to be modulated by stabilizing the pre-activated state of arrestin through point mutations or C-tail truncation. Here, we hypothesize that pre-activated rotated states can be stabilized by small molecules, and this can promote binding to phosphorylation-deficient receptors, which underly a variety of human disorders.
View Article and Find Full Text PDFFront Med (Lausanne)
December 2024
Division of Cardiovascular Sciences, School of Medical Sciences, University of Manchester, Manchester, United Kingdom.
Background: The sinoatrial node (SN) generates the heart rate (HR). Its spontaneous activity is regulated by a complex interplay between the modulation by the autonomic nervous system (ANS) and intrinsic factors including ion channels in SN cells. However, the systemic and intrinsic regulatory mechanisms are still poorly understood.
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