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Biomedical subjects

E Echevarria

Publications and source records attributed to E Echevarria.

At least 19 recordsLinked to original sources

Diabetic cardiomyopathy: electromechanical cellular alterations.

Diabetic patients show a higher incidence of cardiac arrhythmias, including ventricular fibrillation and sudden death. However, although diabetic cardiomyopathy is a frequent and important complication of diabetes mellitus, its physiological basis is not completely known. The electrocardiogram of diabetic patients shows several alterations from normal patterns, most of them related to the QT interval and T wave. Recently, different alterations in cardiac ionic currents have been described in myocytes isolated from diabetic hearts, mainly a reduction in potassium repolarizing currents. Three different mechanisms could be involved in these alterations. First, direct metabolic alterations of the cardiac myocyte, such as impaired activity of protein kinases and phosphatases, intracellular pH regulation, intracellular calcium handling, and others. Second, impaired support of extra cardiac factors regulating cardiac activity, such as sympathetic regulation of heart rate and contractility. Thus, diabetic autonomic neuropathy leads to diminished noradrenaline release in cardiac ventricle in response to standing, exercise or cold stress. Besides, diabetic cardiomyopathy reduces cardiac myocyte response to acute noradrenaline exposure and finally, impairs support of different trophic factors responsible for the regulation of ionic channel expression. Thus, basal noradrenaline release in the ventricles, necessary to maintain adequate potassium channel expression, is reduced by sympathetic neuropathy. Moreover, the levels of insulin and other trophic factors required for the maintenance of adequate ionic channel expression are also altered in diabetic patients. Therefore, different physiopathological mechanisms are involved in diabetic cardiomyopathy. Thus, further research is needed in order to prevent the development of this long-term complication, and to improve the pharmacological management of diabetic patients.

Calcium↗

Spironolactone and captopril attenuates isoproterenol-induced cardiac remodelling in rats.

The role of renin-angiotensin-aldosterone system in cardiac remodelling was studied in isoproterenol-induced cardiac hypertrophy in rats. The effects of captopril and spironolactone were compared. Isoproterenol treatment increased ventricular to body weight ratio (4.6 vs 3.7) and collagen area (22.6 vs 8.2%), and reduced systolic (89.93 vs 107.5 mm Hg) and diastolic (59.6 vs 70.8 mm Hg) pressure. In these animals, captopril decreased systolic (67.4 mm Hg) and diastolic pressure (31.9 mm Hg), whereas spironolactone regressed systolic pressure to control values (101.2 mm Hg). Captopril and spironolactone prevented cardiac hypertrophy (4.01 and 3.95). However, only spironolactone prevented myocardial fibrosis (11.3%).

Angiotensin-Converting Enzyme Inhibitors↗

Toluene alters mu-opioid receptor expression in the rat brainstem.

Toluene is an ototoxic organic solvent widely used in industry and could be a cause of sleep apnea. Acute toluene administration in rats induces an increase in the number of neural cells immunostained for mu-opioid receptors in several brainstem nuclei, such as the inferior colliculus, dorsal and lateral periaqueductal gray and dorsal raphe, without changes in the superior colliculus and the interpeduncular and lateral reticular nuclei. These data suggest that mu-opioid receptors could be involved in toluene-induced neurotoxic effects on the physiological regulation of breathing during sleep, and auditive function.

Animals↗

Toluene alters brainstem enkephalinergic system in rats.

Acute exposure to high doses of toluene can generate respiratory depression. However, neurotoxic mechanism of its action in the brainstem is not completely clear. In this work, acute, but not subchronic, exposure of rats to toluene increased leu-enkephalin immunostaining in several myelencephalic nuclei implicated in cardiorespiratory control. Due to the physiological role of enkephalins in the central regulation of breathing, it is suggested that the enkephalinergic system could play a role in neurotoxic respiratory depression induced by high dose acute toluene exposure.

Animals↗

Effects of acute lidocaine administration on the rat prosencephalic enkephalinergic system.

Lidocaine is a local anesthetic widely used in therapeutics and as antiarrhythmic agent. However, information concerning possible alterations in the enkephalinergic system after acute treatment with this substance is not complete. This being the case, we focused on analyzing enkephalin immunostaining in several regions of the rat brain after lidocaine administration. We could not find significative changes in rat prosencephalon. These data might suggest that the enkephalinergic system is not altered by lidocaine.

Anesthetics, Local↗

Effects of imipramine administration on mu-opioid receptor immunostaining in the rat forebrain.

Imipramine hydrochloride (CAS 113-52-0) is a widely used antidepressant and can interact with opioid receptors. However, complete information concerning possible regional alterations in mu-opioid receptor expression in the rat forebrain after chronic treatment with this substance is still lacking. This being the case, analysis of mu-opioid receptor immunostaining in several regions of the rat brain after imipramine administration in vivo was made, and an increase in the density of cells expressing mu-opioid receptors in the caudatus-putamen, the dentate gyrus and the frontal, parietal and piriform cortices after chronic imipramine treatment, with respect to controls, was found. These data suggest that mu-opioid receptor expression in the rat forebrain is altered by in vivo chronic imipramine treatment.

Animals↗

Effects of chronic treatment with two selective 5-HT2 antagonists on sleep in the rat.

The effect of chronic administration of 2(2-dimethylaminoethylthio)-3-phenylquinoline (ICI-169,369) and 2(2-dimethylamino-2-methylpropylthio)-3-phenylquinoline (ICI-170,809), two selective 5-HT2 antagonists, on sleep was studied in rats. As previously shown, the acute effect of ICI-170,809 was to increase latency to rapid eye movement sleep (REMS), decrease the number of REM periods (REMPs), suppress the cumulative amount of REMS over 12 h, and increase the duration of REMPs in the first 6 h, while having no effect on non-REM sleep (NREMS). Administration of ICI-169,369 had similar effects except no change was seen in the duration of REMPs and cumulative REMS was suppressed for 24 h. When given 2 x daily for 5 days, tolerance to the REMS suppressant effects developed in both drugs. After discontinuation of treatment, a REMS rebound occurred after ICI-170,809, but not ICI-169,369. No significant effect on NREMS was seen after administration of ICI-170,809, whereas ICI-169,369 lowered 24-h cumulative NREMS on the fifth day of administration.

Animals↗

Aspartate-aminopeptidase activity during the estrous cycle and the pregnancy in rat brain and pituitary gland.

The present report describes the activity of aspartate aminopeptidase, in 9 brain areas and in the pituitary gland, during the estrous cycle and several stages of pregnancy of the rat. The quantitation of the enzyme activity was performed by measuring the rate of hydrolysis of the chromogenic substrate Asp-beta-naphthylamide. Aspartate aminopeptidase activity, in the pituitary gland and in several limbic areas, was found to be greater in cyclic than in pregnant rats. However the enzyme activity did not change significantly during either the estrous cycle and pregnancy.

Aminopeptidases↗

PD117302, a selective non-peptide opioid kappa agonist, protects against NMDA and maximal electroshock convulsions in rats.

The pharmacological profile of PD117302 was studied in three rat models of experimental seizures. It was determined that PD117302 is a potent and efficacious anticonvulsant against NMDA (ED50 = 0.27 mg/kg, i.v.) and MES (ED50 = 16.3 mg/kg, s.c.), but not flurothyl, convulsions. Its anticonvulsant profile was dose- and time-dependent, stereospecific and sensitive to naloxone and the selective kappa opioid antagonist nor-binaltorphimine. Given these findings, we suggest that PD117302 acts via the kappa receptor to modulate seizure protection. Furthermore, in view of its marked ability to block NMDA excitotoxicity (including lethality) it seems possible that this drug, or related compounds, may have potential therapeutic utility as a neuroprotective agent.

Animals↗

Serum and brain aminopeptidase activities in cyclic rats.

Research into the functional role of brain peptides is performed, in part, by studying peptidase enzymes which might be involved in the processing or inactivation of the brain peptides. Aminopeptidase activity has been proposed as a candidate for the regulation of the degradation of these peptides. In this paper, acid (Asp-) and basic (Arg-) aminopeptidase activities were studied in several brain regions and in the serum during the estrous cycle of the rat. Asp-aminopeptidase activity did not significantly change at any point. However, a marked rise was found in Arg-aminopeptidase activity in all the brain areas studied and the serum during the proestrus. It is suggested that this activity plays a role in the hormonal changes that take place during the cycle, possibly in regulating the activity of several neuroactive peptides.

Aminopeptidases↗

Suppressant effects of selective 5-HT2 antagonists on rapid eye movement sleep in rats.

The effects of the novel, highly selective serotonin-2 (5-HT2) antagonists, ICI 169,369 and ICI 170,809, on 24 h EEG sleep-wake activity were studied in the rat. Both compounds caused a dose-related increase in the latency to rapid eye movement sleep (REMS) and significantly suppressed cumulative REMS time up to 12 h postinjection. In contrast, neither drug disrupted slow-wave sleep continuity in as much as the latency to non-REMS (NREMS) and cumulative NREMS time were unchanged. However, at the highest dose tested (20 mg/kg) ICI 170,809 did produce a significant increase in total NREMS time during the second half of the sleep-awake cycle. These results demonstrate effects of selective 5-HT2 antagonists on sleep in rats which appear to be specific for REMS behavior, suggesting that the priming influence of serotonin on REMS may involve 5-HT2 receptor subtypes. The relationship between the REMS suppressant actions of these compounds and their consideration as therapeutic agents in depression is discussed.

Animals↗

Selective kappa antagonist properties of nor-binaltorphimine in the rat MES seizure model.

The opioid antagonist properties of nor-binaltorphimine (nor-BNI; 17,17'-Bis(cyclopropylmethyl)-6,6',7,7'-tetradehydro-4,5:4', 5'-diepoxy-6,6'-(imino) [7,7'-bimorphinan]-3,3',14,14'-tetrol) were evaluated in vivo in the rat maximal electroshock (MES) seizure model. Following s.c. or i.c.v. pretreatment, nor-BNI selectively antagonized the anticonvulsant effects of the kappa opioid U50, 488, significantly increasing its ED50 by 2.3 and 4.5 fold, respectively. In contrast, pretreatment with nor-BNI (s.c. or i.c.v.) failed to antagonize the anticonvulsant effects of the selective mu opioid, DAMGO. At the doses and injection routes used, nor-BNI itself had no apparent effect on overt behavior or MES-induced convulsions. These data support the earlier suggestion that the anticonvulsant effects of U50,488 are mediated by kappa opioid receptors and confirm 1) the selectivity of nor-BNI as a kappa antagonist and 2) its applicability as a pharmacological tool in the differentiation of multiple opioid receptors.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗

Pre- and postnatal aminopeptidase activities in the rat brain.

Research concerning the functional role of brain peptides is performed, in part, by studying peptidase enzymes which might be involved in brain peptide processing or inactivation. Aminopeptidase (AP) activity has been proposed as a candidate regulator of the degradation of these peptides. In this paper, changes in Lys- and Leu-aminopeptidase activities in rat brain hemispheres, cerebellum and medulla were examined in 20 day fetuses and one day postnatal subjects. Aminopeptidase activities were studied by measuring the rate of hydrolysis of the artificial substrates Lys- and Leu-2-naphthylamides (fluorimetrically detected in triplicate). Both enzyme activities increase from the last fetal stage up to the first day of birth in all the brain areas examined except for the case of Leu-AP activity in the medulla. It is suggested that these activities play a part in the neurochemical changes that take place during rat brain maturation, possibly by regulating the activity of several neuroactive peptides.

Aminopeptidases↗

Anticonvulsant effects of mu (DAGO) and delta (DPDPE) enkephalins in rats.

The effects of highly selective mu and delta opioid peptide agonists were determined in two rat models of experimentally-induced convulsions, the flurothyl threshold test and the maximal electroshock test. Intracerebroventricular injections of the mu selective enkephalin DAGO (0.3-2.2 nmol) resulted in a dose-related protection in both seizure models. Pretreatment with a low dose of naloxone (29 nmol) or the irreversible mu antagonist beta-FNA (21 nmol), but not the delta opioid antagonist ICI 154,129 (50 nmol), antagonized the anticonvulsant actions of DAGO. Intracerebroventricular injections of the delta selective enkephalin DPDPE (70-140 nmol) also resulted in seizure protection. These effects were selectively antagonized by the delta antagonist ICI 174,864 (2.8 nmol), but not by pretreatment with beta-FNA. Thus, using agonists and antagonists highly selective for mu and delta opioid receptors, anticonvulsant actions of enkephalin have been described against chemically- and electrically-induced convulsions in rats.

Animals↗