6 results on '"G. Zapata"'
Search Results
2. Antihypertensive Effect of New Agonist of Adenosine Receptor in Spontaneously Hypertensive Rats.
- Author
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de Souza Rocha B, Silva JSD, Pedreira JGB, Montagnoli TL, Barreiro EJ, and Zapata-Sudo G
- Subjects
- Rats, Animals, Male, Rats, Inbred SHR, Rats, Wistar, Blood Pressure, Potassium Channels, Antihypertensive Agents pharmacology, Antihypertensive Agents therapeutic use, Hypertension drug therapy
- Abstract
Background: Systemic arterial hypertension is a risk factor for cardiac, renal, and metabolic dysfunction. The search for new strategies to prevent and treat cardiovascular diseases led to the synthesis of new N-acylhydrazones to produce antihypertensive effect. Adenosine receptors are an alternative target to reduce blood pressure because of their vasodilatory action and antioxidant properties, which may reduce oxidative stress characteristic of systemic arterial hypertension., Objective: To evaluate the antihypertensive profile of novel selenium-containing compounds designed to improve their interaction with adenosine receptors., Methods: Vascular reactivity was evaluated by recording the isometric tension of pre-contracted thoracic aorta of male Wistar rats after exposure to increasing concentrations of each derivative (0.1 to 100 μM). To investigate the antihypertensive effect in spontaneously hypertensive rats, systolic, diastolic, and mean arterial pressure and heart rate were determined after intravenous administration of 10 and 30 μmol/kg of the selected compound LASSBio-2062., Results: Compounds named LASSBio-2062, LASSBio-2063, LASSBio-2075, LASSBio-2076, LASSBio-2084, LASSBio-430, LASSBio-2092, and LASSBio-2093 promoted vasodilation with mean effective concentrations of 15.5 ± 6.5; 14.6 ± 2.9; 18.7 ± 9.6; 6.7 ± 4.1; > 100; 6.0 ± 3.6; 37.8 ± 11.8; and 15.9 ± 5.7 μM, respectively. LASSBio-2062 (30 μmol/kg) reduced mean arterial pressure in spontaneously hypertensive rats from 124.6 ± 8.6 to 72.0 ± 12.3 mmHg (p < 0.05). Activation of adenosine receptor subtype A3 and potassium channels seem to be involved in the antihypertensive effect of LASSBio-2062., Conclusions: The new agonist of adenosine receptor and activator of potassium channels is a potential therapeutic agent to treat systemic arterial hypertension.
- Published
- 2024
- Full Text
- View/download PDF
3. Riociguat: An Alternative to Treat Pulmonary Hypertension.
- Author
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Zapata-Sudo G
- Subjects
- Chronic Disease, Humans, Pyrazoles therapeutic use, Pyrimidines therapeutic use, Hypertension, Pulmonary drug therapy
- Published
- 2022
- Full Text
- View/download PDF
4. Crossroads between Estrogen Loss, Obesity, and Heart Failure with Preserved Ejection Fraction.
- Author
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Alencar AKN, Wang H, Oliveira GMM, Sun X, Zapata-Sudo G, and Groban L
- Subjects
- Estrogens, Female, Humans, Male, Obesity, Abdominal complications, Stroke Volume, Ventricular Function, Left, Heart Failure etiology, Ventricular Dysfunction, Left etiology
- Abstract
The prevalence of obesity and heart failure with preserved ejection fraction (HFpEF) increases significantly in postmenopausal women. Although obesity is a risk factor for left ventricular diastolic dysfunction (LVDD), the mechanisms that link the cessation of ovarian hormone production, and particularly estrogens, to the development of obesity, LVDD, and HFpEF in aging females are unclear. Clinical, and epidemiologic studies show that postmenopausal women with abdominal obesity (defined by waist circumference) are at greater risk for developing HFpEF than men or women without abdominal obesity. The study presents a review of clinical data that support a mechanistic link between estrogen loss plus obesity and left ventricular remodeling with LVDD. It also seeks to discuss potential cell and molecular mechanisms for estrogen-mediated protection against adverse adipocyte cell types, tissue depots, function, and metabolism that may contribute to LVDD and HFpEF.
- Published
- 2021
- Full Text
- View/download PDF
5. Inhibition of L-type calcium current by tramadol and enantiomers in cardiac myocytes from rats.
- Author
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Medei E, Raimundo JM, Nascimento JH, Trachez MM, Sudo RT, and Zapata-Sudo G
- Subjects
- Analysis of Variance, Animals, Depression, Chemical, Male, Models, Animal, Patch-Clamp Techniques, Rats, Rats, Wistar, Tramadol analogs & derivatives, Analgesics, Opioid pharmacology, Calcium Channels, L-Type drug effects, Myocardial Contraction drug effects, Myocytes, Cardiac drug effects, Papillary Muscles drug effects, Tramadol pharmacology
- Abstract
Background: Tramadol is a centrally acting analgesic, whose mechanism of action involves opioid-receptor activation. Previously, we have shown that tramadol and its enantiomers had a negative inotropic effect on the papillary muscle in which the (+)-enantiomer is more potent than (-)- and (±)-tramadol., Objective: In this study, we investigated the effects of tramadol and its enantiomers on L-type calcium current (ICa-L)., Methods: The experiments were carried out in isolated Wistar rat ventricular myocytes by using the whole cell patch clamp technique., Results: Tramadol (200 µM) reduced the peak amplitude of ICa-L at potentials from 0 to +50 mV. At 0 mV, I(Ca-L) was reduced by 33.7 ± 7.2%. (+)- and (-)-tramadol (200 µM) produced a similar inhibition of ICa-L, in which the peak amplitude was reduced by 64.4 ± 2.8% and 68.9 ± 5.8%, respectively at 0 mV (p > 0.05). Tramadol, (+)- and (-)-tramadol shifted the steady-state inactivation of ICa-L to more negative membrane potentials. Also, tramadol and (+)-tramadol markedly shifted the time-dependent recovery curve of I(Ca-L) to the right and slowed down the recovery of I(Ca-L) from inactivation. The time constant was increased from 175.6 ± 18.6 to 305.0 ± 32.9 ms (p < 0.01) for tramadol and from 248.1 ± 28.1 ms to 359.0 ± 23.8 ms (p < 0.05) for (+)-tramadol. The agonist of µ-opioid receptor DAMGO had no effect on the I(Ca-L)., Conclusion: The inhibition of ICa-L induced by tramadol and its enantiomers was unrelated to the activation of opioid receptors and could explain, at least in part, their negative cardiac inotropic effect.
- Published
- 2011
- Full Text
- View/download PDF
6. Anesthetic profile of a non-lipid propofol nanoemulsion.
- Author
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Sudo RT, Bonfá L, Trachez MM, Debom R, Rizzi MD, and Zapata-Sudo G
- Subjects
- Anesthetics, Intravenous toxicity, Animals, Emulsions, Male, Mice, Nanostructures, Propofol toxicity, Rats, Rats, Wistar, Anesthetics, Intravenous pharmacology, Propofol pharmacology
- Abstract
Background and Objectives: The clinical use of a lipid propofol formulation causes pain during injection, allergic reactions, and bacterial growth. Propofol has been reformulated in different non-lipid presentations to reduce the incidence of adverse effects, but those changes can modify its pharmacokinetics and pharmacodynamics. In the present study, we investigate the pharmacology and toxicology of lipid propofol (CLP) and the non-lipid nanoemulsion (NLP)., Methods: Conventional lipid formulation of propofol and NLP were infused in the jugular veins of rats and blood pressure (BP), heart rate (HR), and respiratory rate (RR) were measured. Both formulations (1%) were infused (40 μL.min⁻¹) over 1 hour. Hypnotic and anesthetic doses as well as recoveries were determined. The pain induced by the CLP and NLP vehicles was compared by counting the number of abdominal contortions ("writhing test") after the intraperitoneal (i.p.) injection in mice. Acetic acid (0.6%) was used as positive control., Results: Hypnotic and anesthetic doses of 1% CLP (6.0 ± 1.3 and 17.8 ± 2.6 mg.kg⁻¹, respectively) and 1% NLP (5.4 ± 1.0 and 16.0 ± 1.4 mg.kg⁻¹, respectively) were not significantly different. Recovery from hypnosis and anesthesia was faster with NLP than with CLP. Changes in HR, BP, and RR caused by NLP were not significantly different from those caused by CLP. Acetic acid and the vehicle of CLP caused 46.0 ± 2.0 and 12.5 ± 0.6 abdominal contortions 20 min after i.p. injection, respectively. The absence of abdominal contractions was observed with the vehicle of NLP. Abdominal inflammatory response was not observed after the i.p. injection of both propofol vehicles., Conclusions: Non-lipid formulation of propofol can be a better alternative to CPL for intravenous anesthesia with fewer adverse effects., (Copyright © 2010 Elsevier Editora Ltda. All rights reserved.)
- Published
- 2010
- Full Text
- View/download PDF
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