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[Indicators of mental and physical work capacity during reserpine treatment of patients with arterial hypertension working under neuro-emotional stress].

The article deals with reserpine influence on mental and physical working capacity, psychic state and professionally relevant functions of memory and concentration in 36 male patients of 50 +/- 2.0 years of age suffering from arterial hypertension and engaged in professions characterized with extreme neuro-emotional stress conditions ( enterprise managers). It was shown that reserpine induced a stable and significant hypotensive effect, improved the physiological indices and physical working capacity, but hampered the mental and cognitive function activity, concentration and short-term memory. Reserpine cannot be recommended for drug therapy in out-patient departments in the treatment of the patient professionally engaged in stable emotional stress conditions.

Adult↗

[Effect of reserpine on both CL seizures and cAMP levels in seizure mice brain].

Reserpine injection (1 mg/kg i.p.) could not only significantly reduce cAMP levels in both cerebral cortex and hippocampus in naive WC1 mice, but also potentiate the degree of seizures elicited by CL. Reserpine injection could significantly shorten CL-seizures latency and decrease its threshold, too. Reserpine pretreatment could also diminish CL seizure-induced accumulation of cAMP. These results indicated the cAMP level elevated by seizure activity was associated with monoamine neurotransmitter activity, and the seizure-induced accumulation of cAMP might take part in the process which eliminated the spread of seizure discharges and speeded up the termination of seizures.

Animals↗

Investigation of exercise stress by antihypertensive treatment with a combination containing beta-blocker/diuretic or reserpine.

The effects of a beta-blocker/diuretic combination and a reserpine-containing combination on exercise hypertension were compared in 20 patients suffering from mild hypertension with a diastolic pressure between 90 and 105 mmHg and a positive exercise test. This double-blind, randomized, within-patient, cross-over study involved two four-week phases, each preceded by a two-week wash-out period. The effect on the double product (tension-time index) and the physical working capacity at a heart rate of 170 bpm (PWC170) was also measured. The advantage of the preparation containing the beta-receptor blocker was apparent in both phases as physical work load increased. The PWC170 was twofold greater in the beta-receptor blocker group than in the reserpine group. The tension-time index was lowered in the normal range in both phases by the beta-blocker combination. The reserpine-containing preparation in the second phase did not further enhance the improvement produced by the beta-blocker in the first phase. These results suggest that it is worth questioning the traditional antihypertensive treatment in elderly patients, in whom mild hypertension is common, in order to better protect them from cardiovascular complications.

Adrenergic beta-Antagonists↗

Thin layer densitometry in the quantitative assay of drugs. Note V--Assay of reserpine and chlorthalidone in the presence of the potential impurities of their solid pharmaceutical forms.

Densitometric detection of compounds separated by thin layer was applied to the assay of a mixture of reserpine and chlorthalidone and their possible impurities. The method of analysis gave satisfactory results in the quality control of pharmaceutical preparations. Good results were obtained in urine tests for the detection of chlorthalidone, reserpine and methylreserpate. The times for the development of fluorescence in reserpine and methylreserpate directly in the chromatographic plate, are also described.

Chlorthalidone↗

[The effect of estradiol and reserpine on cortisol formation in sexually immature rats].

The studies were carried out on immature female rats. The animals were divided into 4 groups: 1) treated with saline, 2) treated with reserpine, 3) treated with estradiol and 4) treated with estradiol and reserpine. Administration of drugs were made on 35, 36 and 37 day after delivery. There was statistically significant difference between the control group, treated with saline, and the group of rats, treated with estradiol. This is a new original fact for the presence of estrogen receptors in adrenal cells. Significant difference was found between the groups, treated with reserpine, and those, treated with saline and estradiol. The presented new data support the concept on the role of the adrenergic system in inhibiting hypothalamo-hypophysial-adrenal axis.

Aging↗

Essential fatty acid deficient rats in the study of cystic fibrosis: an X-ray microanalytical and ultrastructural study in chronically reserpinized rats.

Essential fatty acid (EFA) deficiency has been proposed as a major pathogenic mechanism for cystic fibrosis (CF) and EFA-deficient animals have been proposed as an animal model for CF. In the present study, the elemental composition and ultrastructure of the acinar cells of the submandibular and parotid gland of the pancreas of EFA-deficient rats were investigated by X-ray microanalysis and electron microscopy. The effects of EFA-deficiency were compared to changes in these exocrine glands in chronically reserpine-treated rats, an established animal model for CF. EFA-deficiency did not cause any significant changes in the elemental composition of the acinar cells of the submandibular or parotid gland, or of the pancreas. The changes in elemental composition induced by reserpine treatment were only slightly modified by EFA-deficiency, mainly towards normalization. EFA-deficiency resulted in the presence of abnormal, electron translucent, zymogen granules in the parotid gland and in a reduction of the number of zymogen granules in pancreatic acinar cells. Since EFA-deficiency in rats only causes minor changes in structure and elemental composition of salivary glands and pancreas, and does not potentiate the effect of chronic reserpine treatment on these tissues, it is concluded that EFA-deficiency is likely to be of minor importance in the exocrine gland disturbances in CF.

Animals↗

Effects of reserpine on activities and amounts of tyrosine hydroxylase and dopamine-beta-hydroxylase in catecholamine neuronal systems in rat brain.

Reserpine (10 mg/kp i.p.) increased the activities of the enzymes tyrosine hydroxylase (TH) and dopamine-beta-hydroxylase, but not dopa decarboxylase, 2- to 3-fold in the nucleus locus ceruleus of rat brain. The TH response was dose-dependent, reached a maximum by 48 hours and recovered by 3 weeks. The increased activities of TH and dopamine-beta-hydroylase were shown by immunotitration with specific antibodies to each enzyme to be due entirely to increased accumulation of specific enzyme protein. At a time when the reserpine-elicited accumulation of TH was increased 300% in the locus ceruleus, activity of the enzyme only increased 20% in hypothalamus and not at all in substantia nigra or caudate nucleus. Reserpine increased the accumulation of TH, primarily in the cell bodies and to a far less degree in the terminals of neurons of locus ceruleus but not in dopaminergic neurons of the nigrostriatal system. The time course of enzyme accumulation parallels that of depletion of monoamines in brain.

Animals↗

Differential serotonin2 receptor recovery in mature and senescent rat brain after irreversible receptor modification: effect of chronic reserpine treatment.

We report here the differential time course of recovery of [3H]ketanserin-labeled serotonin2 (5-HT2) receptors in frontal cortex of mature (4 months old) and senescent (28 months old) male Fischer 344 rats. We provide evidence that the irreversible modification of 5-HT2 serotonin receptors by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline occurs at the ligand binding site and that this treatment does not appear to affect the interaction of these receptors with their guanine nucleotide regulatory protein. Senescent rats exhibited significantly reduced (-20%) maximum receptor density levels of 5-HT2 receptors compared with their mature counterparts. The time course of recovery of [3H] ketanserin binding to 5-HT2 receptors after irreversible receptor modification by a single peripheral injection of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline was significantly slower in senescent rats. The slower recovery was a function of decreases in both the receptor production rate and the degradation rate constant in senescent rats compared with mature rats. Interestingly, chronic reserpine treatment resulted in a significant decrease in control maximum receptor density values in both mature (-17%) and senescent (-18%) rats. Although the receptor production rate and receptor degradation rate constants in both mature and senescent reserpinized rats were slightly decreased, there was no significant change in the overall rates of receptor recovery when compared with their respective age-matched nonreserpinized counterparts. These data indicate that both the steady state levels and "turnover" of 5-HT2 receptors are decreased in senescence and that these receptors can be down-regulated by chronic reserpine treatment.

Adrenergic alpha-Antagonists↗

Ultrastructural alterations of the egg chambers of Galleria mellonella L. (Lepidoptera) developing after reserpine administration.

In the egg chambers of the wax moth Galleria mellonella L., developing after application of reserpine, a multilayered epithelium was observed through all the developmental stages. This epithelium consisted of "light" cells loaded with intracellular organelles. No "dark" cells, characteristic of the control material, were observed. All cells of the egg chambers of reserpine-treated insects were characterized mostly by an abundance of microtubules, strong vacuolation of cytoplasm, and dilation of intercellular and perinuclear spaces. Moreover, changes, such as malformation of nuclei and nucleoli, appearance of large glycogen deposits, occurrence of widened cisternae and canaliculi of rough endoplasmic reticulum (RER) connected with lipid droplets, and appearance of nonhomogeneous protein yolk spheres, were noted in the oocyte. The observed disturbances in the ultrastructure of the developing ovary are discussed in the aspect of a direct action of reserpine through the insect neurohormonal system, and of a possible indirect one by an impairment of calcium homeostasis.

Animals↗

Effects of short-term reserpine treatment on generalized and focal dystonic-dyskinetic syndromes.

We report that low dose reserpine treatment (0.25 mg/day for 7 days) improves the dystonic-dyskinetic disability score in patients affected by idiopathic dystonias, iatrogenic dystonic-dyskinetic syndromes and Sydenham's chorea. The results support the idea that the particular antidopaminergic activity exerted by reserpine or other dopamine-depleting agents may produce good therapeutical efficacy, although reserpine can precipitate Parkinsonism and induce dopamine-receptor supersensitivity.

Adolescent↗

Differential recovery in measures of exploration/locomotion after a single dosage of reserpine in the rat.

Different aspects of exploration/locomotion were studied in rats injected with reserpine (4 mg/kg i.p.) once and in vehicle injected yoked controls. Fifteen different parameters were measured on 7 sessions - on the 1st, 3rd, 5th, 7th, 11th, 15th and 21st postinjectiorn day. The difference scores (the value obtained from the control animal minus the corresponding value from the yoked reserpinized animal) were subjected to nonparametric analysis of variance across sessions. Of the 15 parameters only 6 revealed significant differences between sessions. Furthermore, for those six parameters which exhibited significant differences between sessions the recovery patterns revealed by differences between sessions were dissimilar. It is concluded that what is usually referred to as exploratianflocomotion must be considered apparatus- and procedure-specific and that the measures obtained in different studies should only be compared when identical procedures have been employed. In addition to the measures of exploration/locomotion the rats were subjected to a parallel series of active avoidance sessions in a shuttle-box. Comparing the reserpinized rats impaired active-avoidance aquisiticm to the recovery patterns in the exploratiodlocomotion tests, it can be tentatively concluded that the lack of recovery in the active-avoidance test is not solely due to impaired motoric abilities.

Animals↗

[Action of nonachlazine on the creatine phosphokinase and acid phosphatase activity and on the lysosomal membrane stability of the ischemic myocardium in rats after preliminary reserpinization].

Experiments on the ischemic myocardial tissue of the rat in vitro showed that despite the fact that reserpine-induced depletion of the tissue catecholamine storage failed to affect the stability of lysosomal membranes, a combination of reserpine pretreatment of the animals with subsequent administration of nonachlazine at the low dose yielded stabilization of lysosomal membranes to a greater extent than administration of nonachlazine alone. The effects of nonachlazine (0.25 mg/kg) on the activity of creatine phosphokinase and total activity of acid phosphatase with and without reserpine pretreatment were similar.

Acid Phosphatase↗

Reserpine toxicosis in a horse.

A single injection of reserpine in an adult horse was believed to induce toxicosis for several days. Clinical signs included erratic, colic-like behavior followed by depression, bradycardia, miosis, ptosis, and paraphimosis. Diarrhea was not observed and may have been due to the effect of xylazine given with the reserpine. The horse was supported with IV fluids and intensive nursing care. Gradual improvement was noted 72 hours after the horse received the drug. Qualitative analysis via high-performance liquid chromatography was positive for reserpine. Methamphetamine is the recommended antidote but was not used in this case.

Animals↗

Effect of histalog, insulin and reserpine on gastric emptying and secretion in man.

Four different groups of subjects were given Histalog, insulin or reserpine or acted as controls. Changes were noted in gastric emptying, acid, chloride, parietal and non-parietal secretions and neutral chloride. Gastric emptying and secretion were measured by the Hunt and Spurrell test meal as modified by us for drug testing.Histalog stimulated gastric secretion but not emptying. Insulin stimulated both secretion and emptying. Reserpine stimulated secretion but it stimulated emptying only in one-half of the subjects.After Histalog and reserpine the rise in hydrogen and chloride secretion was equal, so the neutral chloride did not increase. After insulin the rise of chloride was proportionately greater than the rise of hydrogen, so that neutral chloride was increased.

Gastric Acidity Determination↗

[Studies on the mechanism of action of clonidine after pretreatment with reserpine (author's transl)].

The effects of 3.7--30 micrograms 2-(2,6-dichlorophenolamino)-2-imidazoline hydrochloride (clonidine)/kg i.v. on the arterial blood pressure and the central nervous activities of the sympathetic and the phrenic nerves were studied in 33 anaesthetized, relaxed and artificially respirated cats. In part of the experiments the animals were pretreated with reserpine at a dosage of 2X0.3 mg/kg. In normal animals clonidine caused a fall in blood pressure, a reduction of nicotinic pressure effect and an inhibition of sympathetic activity. In pretreated animals the antinicotinic as well as the sympathetic inhibitory actions of clonidine were significantly increased at a dosage of 30 micrograms/kg. The single application of reserpine caused no changes of these two parameters. As a result clonidine probably caused a stimulation of central nervous postsynaptic alpha-adrenoceptors and after the pretreatment with reserpine in addition to this an inhibition of the release of epinephrine.

Animals↗

[Impairment of renal cortical blood flow autoregulation induced by reserpine, guanethidine or propranolol (author's transl)].

Local blood flow was measured in renal cortex (at 1 mm below cortical surface) by means of the hydrogen clearance method in urethanized rats. Recording of blood pressure from femoral artery was performed. The blood flow autoregulation was studied by plotting renal cortical vascular resistance (R.C.V.R.) as a function of arterial pressure in all the experimental conditions. R.C.V.R. was calculated as arterial pressure/blood flow ratio. In control animals R.C.V.R. was linearly correlated to arterial pressure; this implies the existence of autoregulation in the studied zone. In animals pretreated with guanethidine or propranolol, and in animals injected with propranolol immediately before the experiment, the increase of arterial pressure was not followed by an increase in R.C.V.R.; this implies that autoregulation was absent. In animals pretreated with reserpine the increase of arterial pressure was not followed by a significant increase in R.C.V.R., although a tendency to increase was detected. It is suggested that the impairment of autoregulation induced by guanethidine, propranolol or reserpine may be due to an inhibition of renin release. The results obtained with guanethidine and reserpine may be partially attributable to a decrease in adrenergic activity on the vascular smooth muscle of the studied zone, although other mechanisms cannot be discarded.

Animals↗

[Changes in the dopamine content in the brain of Periplaneta americana L. after application of structural analogs of dopamine and reserpine].

Changes in the content of dopamine (DA) in the CNS of the Cockroach (Periplaneta americana L.) after application of L-DOPA, p-chlorophenylalanine (p-CPA), alpha-methyltyrosine (MT), 6-hydroxydopamine (6-OHDA) and reserpine have been investigated by fluorimetric measures. The content of DA is increased by p-CPA, and decreased by MT and 6-OHDA. Reserpine exhibits a decreasing effect in high concentration only (30 micrograms/g body weight). Probably, the high compatibility of reserpine is caused by a special alkaloidesterase (a hypothetical "reserpinase").

Animals↗

influence of Mg++ and reserpine on the reactivity of rat seminal vesicle to 5-hydroxytryptamine.

The effects of varying the concentration of Mg++ in the incubation medium on the contractile responses of rat isolated seminal vesicle to 5-hydroxytryptamine (5-HT) were investigated in the absence and presence of EDTA. Preparations incubated in Mg++-free and Mg++ excess media showed supersensitivity and subsensitivity to 5-HT respectively. In the presence of EDTA alterations in the sensitivity to 5-HT produced by varying the concentrations of Mg++ were comparatively less. Preparations obtained from reserpinized animals showed subsensitivity in normal and Mg++ excess media and supersensitivity in Mg++-free medium. In the presence of EDTA, reserpinized preparations showed slight supersensitivity in normal Mg++ medium, marked supersensitivity in Mg++-free medium and lesser subsensitivity in Mg++ excess medium. Probably EDTA by more effectively removing Mg++ from the membrane binding sites by chelation makes the membrane permeable to Ca++ leading to supersensitivity to 5-HT (observed only in the presence of EDTA). These results suggest that the failure of reserpine to induce supersensitivity to 5-HT in rat seminal vesicle may be due to an enhanced antagonism of Mg++ on Ca++ movements in this preparation due to the poor capacity of rat tissue to retain Ca++ (Krishnamurty and Grollman, 1976).

Animals↗