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Beta-adrenergic receptors and the effect of beta-adrenergic blocking agent propranolol on histamine and reserpine stimulated gastric acid secretion in man: normals and duodenal ulcer cases.

The effects of the beta adrenergic stimulant drug, "Nylidrin", and the beta adrenergic blocking agent, "Propranolol", on human basal gastric acid secretion were studied in 20 healthy volunteer subjects and 10 chronic D.U. cases. Nylidrin increased gastric acid secretion and volume. All effects of nylidrin were blocked by prior administration of beta adrenergic inhibitor propranolol. Propranolol diminished both acid secretion and volume in both normal and D.U. cases. The presence of beta adrenergic receptors in the human stomach was suggested. The effects of beta adrenergic blocking agent propranolol on gastric secretion, stimulated with histamine, were studied in 10 normal subjects and 10 cases of chronic duodenal ulcer patients. Pretreatment with propranolol produced a signigicant depression of the 90 minute acid response to histamine in both volume and acidity in normals and duodenal ulcer cases. It is concluded that propranolol has an antisecretory effect, not only on basal gastric secretion but also on histamine stimulated secretion in man. Reserpine stimulated gastric acid secretion and volume in normals but showed no similar effect in D.U. cases. After pretreatment with propranolol it reduces the gastric acid secretion and volume in normals and D.U. cases.

Adult↗

[The effect of shourong compound formula on levels of dopamine and its metabolites in brain of Parkinson's disease mice induced by reserpine].

OBJECTIVE: To investigate the effect of Shourong compound formula on treating Parkinson's disease. METHOD: Parkinson's disease model mice induced by reserpine was used and by HPLC-ED the levels of Dopamine (DA) and its metabolites were determined. RESULT: Madopar could increase the levels of DA in brain of PD mice. The effect of madopar together with Sourong compound formula was better than that of madopar(P < 0.001). CONCLUSION: Shourong compound formula together with madopar has synergic effect on increase of DA level in brain and can reduce clinic dose of madopar so that side effect of madopar can be decreased.

3,4-Dihydroxyphenylacetic Acid↗

[The mechanism of the effect of reserpine on endocrine system function].

The experiments in rabbits and guinea-pigs showed that the use of reserpine, 0.1 and 0.25 mg/kg body weight a day, led to a 2-2.8-fold increase in thyroid hormones and 25-45% enhancement in cortisol in the blood. At the same time cAMP concentrations increased by 87% and almost by 5 times in the thyroid and adrenals, respectively. The pancreas exhibited a 5-fold increase in cAMP, 2.5- and 2.3-fold decrease in insulin in rabbit peripheral blood and in the activity of pancreatic aldolase and dehydrogenases, respectively. Blood levels of glucose reduced by 15-17%.

Adrenal Cortex Hormones↗

Rapid development of dopaminergic supersensitivity in reserpine-treated rats demonstrated with 14C-2-deoxyglucose autoradiography.

Dopaminergic denervation supersensitivity has been implicated in the pathogenesis of levodopa-induced dyskinesias, the most common and limiting side effect in the drug treatment of Parkinson's disease, yet the mechanisms that mediate altered drug sensitivity remain poorly understood. In animals models, one key component of denervation supersensitivity is the enhanced efficacy of selective D1 agonists to stimulate locomotion. In rats with chronic dopamine depletion induced by 6-hydroxydopamine nigral lesion, the increased ability of D1 agonists to stimulate regional cerebral glucose utilization (RCGU) in the substantia nigra pars reticulata (SNr) has provided a metabolic correlate to the heightened motor response. In this study, we used the stimulation of RCGU in the SNr as a sensitive in vivo assay of D1 agonist effect to examine the time course of development of supersensitivity in rats following acute dopamine depletion with single doses of reserpine (5.0 mg/kg, i.p.) and alpha-methyl-p-tyrosine (AMPT; 100 mg/kg, i.p.). The stimulatory effect of the D1 agonist SKF 38393 (30 mg/kg) on RCGU in the SNr was first enhanced 6 hr after reserpine/AMPT injection and was maximally enhanced at 12-24 hr (relative 2-deoxyglucose uptake increased 32-51%; P less than 0.05). The response to SKF 38393 returned to control values 5 d after reserpine/AMPT injection. The single reserpine/AMPT injections depleted striatal dopamine to 1-2% of control values from 3-48 hr postinjection, whereas D1 and D2 dopamine receptor densities were unchanged at 24 hr.(ABSTRACT TRUNCATED AT 250 WORDS)

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗

Thioridazine reduces resistance of methicillin-resistant staphylococcus aureus by inhibiting a reserpine-sensitive efflux pump.

Previous studies suggested that the phenothiazine chlorpromazine (CPZ) could reverse or reduce the antibiotic resistance of bacteria. In some areas of the world, the majority of Staphylococcus aureus isolates are now resistant to methicillin, prompting this study to see whether such resistance can be altered by phenothiazine thioridazine (TZ), an agent with equal antibacterial activity, which is free of the severe side-effects associated with chronic administration of CPZ. The results indicated that, whereas methicillin-sensitive strains of Staphylococcus aureus (MSSA) were not rendered more susceptible to oxacillin, resistance to oxacillin by highly-resistant strains (MRSA) could be significantly reduced by sub-inhibitory concentrations of TZ. Reserpine, an inhibitor of efflux pumps, was also shown to reduce the resistance of MRSA strains to oxacillin in a concentration-dependent manner. The phenothiazines have been shown, by others, to inhibit the efflux pumps of bacteria and the mechanism by which MRSA are rendered more susceptible to oxacillin in the presence of TZ is believed to be due to a similar efflux pump.

Anti-Bacterial Agents↗

Effect of reserpine and calcium antagonists on doxorubicin storage in various organs of young and senescent rats.

Reserpine pre-treatment causes a considerable decrease in typical red-orange doxorubicin fluorescence of the organs examined (kidney, large intestine, spleen) and a similar picture is observed after calcium antagonists administration. This effect is far more evident in the spleen and large intestine than in the kidney; moreover, it seems more marked in young rats compared with aged ones. An inhibitory action of these drugs on the anthracycline transport carrier through the cell membrane is hypothesized.

Aging↗

Doxorubicin storage in myocardial tissue of reserpine- and nicardipine-pretreated rats.

While reserpine and nicardipine pretreatment induced a more or less marked decrease in typical red-orange doxorubicin fluorescence in certain rat tissues, such as spleen, kidney and large intestine, the myocardial tissue (right atrium and left ventriculum) did not show any significant variations in nuclear doxorubicin storage. This different behaviour of cardiac tissue may be related to the well-known doxorubicin cardiotoxicity.

Animals↗

[Plasma ACTH, STH and other hormone levels in various groups under chlormethiazole, haloperidol or reserpine load in alchohol delirium, alcoholic hallucinations, and chronic alcoholism].

Studies of 135 men with safely diagnosed alcohol delirium mostly revealed increased ACTH blood values when sober and increased T4 values in about 1/3 of these patients. There is a correlation between the psychiatric clinical picture of the alcohol delirium and the ACTH content of the plasma. Under load with chloromethiazole, halperidole or with reserpine, there is a significant drop in the increased ACTH and T4 values. In an acute alcoholic hallucinosis (n=16) similar endocrinological changes as in most cases of safely diagnosed alcohol delirium were observed. In a chronic alcoholic hallucinosis (n=11) and in chronic alcoholics (n=31) the endocrinological values were similar to those of patients after alcohol delirium.

17-Hydroxycorticosteroids↗

[Severe ischemia of the hand. Treatment with regional intravenous sympathicolysis with reserpine].

Treatment of severe hand ischemia a associated to progressive systemic sclerosis and other disorders is controversial. We studied prospectively 45 patients, 41 female and 4 males, over an 11 year period. Age ranged from 16 to 73 years, mean 46. Underlying disease was systemic sclerosis in 30, CREST in 8, overlapping syndrome in 4, systemic lupus in 1 and non rheumatic vasculitis in 2 patients. Treatment consisted of intravenous injection of reserpine, 1 mg, at a superficial arm vein after controlled local circulatory block for 15 min. Regional anesthesia was required in 38 patients. Adequate follow up was obtained in 32 females and 2 males, receiving a mean of 3.1 therapy sessions (range 1 to 13). Morphologic improvement from 3.09 +/- 0.16 to 1.57 +/- 0.13 and functional improvement from 3.6 +/- 0.12 to 1.75 +/- 0.14 (5 grade scoring system), was observed (p < 0.001). These results correlate with adequate rehabilitation confirmed clinically.

Adolescent↗

The influence of central chemical sympathectomy and reserpine on peripheral effects of noradrenaline and cyclic AMP dibutyrate injected into the cerebral ventricles.

Chemical sympathectomy of the central nervous system by injection of 6-hydroxy-dopamine (2 X 250 mug) or 6-hydroxydopa (90 mug) intensified some of the peripheral effects of noradrenaline and cyclic AMP dibutyrate injected into the cerebral ventricles. Reserpine (5 mg/kg) injected intraperitoneally weakened the peripheral reactions to noradrenaline injected intraventricularly. The results of the experiments indicate that peripheral reactions to intraventricularly injected noradrenaline depend on changes in the content of endogenous narodrenaline in the brain and on the mechanisms leading to these changes.

Animals↗

[Fluorimetric determination of the concentration of histamine and serotonin in the mast cells of ordinary and germ-free rats following administration of reserpine and cyclic adenosine-3',5'-monophosphate].

The microspectrometric method was applied to the determination of the content of histamine (a test with orthophthalic aldehyde) and serotonin (Falk's test) in the mast cells of the mesentery of common and germfree rats. Reserpine (10 mg/kg of body weight, intramuscularly) failed to alter histamine content, whereas serotonin content fell by 50%. Administration of cyclic AMP (3.5 mg/kg of body weight, intraperitoneally) led to the increase in serotonin content by 80%, and histamine--by 280--320%.

Animals↗

Combination of a thiazide, a vasodilator and reserpine compared with methyldopa plus hydrochlorothiazide in the treatment of hypertension in Zimbabwe.

Brinerdin (Sandoz), a combination of a diuretic (clopamide 5 mg), a vasodilator (dihydro-ergocristine 0.5 mg) and reserpine (0.1 mg) (CDR) was compared with methyldopa (MD) plus hydrochlorothiazide (HCT) for antihypertensive effect, adverse reactions, compliance and patient preference in an open cross-over trial. Eighteen patients completed both arms of the trial and 5 patients who completed the CDR arm were withdrawn while on the MD arm because of adverse effects in 4 and poor control in 1. On HCT 50 mg daily the mean baseline systolic blood pressure was 163.9 +/- 16.3 mmHg and the diastolic blood pressure was 105.9 +/- 6.7 mmHg. On CDR these were reduced to systolic blood pressure 140.3 +/- 15.1 mmHg and diastolic blood pressure 87.8 +/- 9.3 mmHg. On MD + HCT the systolic blood pressure was reduced to 138.5 +/- 16.9 mmHg and the diastolic blood pressure to 88.9 +/- 10.3 mmHg. The differences between the two treatment periods in systolic blood pressure (1.8 mmHg; 95% confidence interval (CI) - 4.1 + 7.7 mmHg) and diastolic blood pressure (1.1 mmHg; 95% CI - 4.6 + 2.4 mmHg) were not significant with P values of 0.6 and 0.7 respectively. Compliance was 98.2% for CDR and 94.7% for MD + HCT (P = 0.02). Unusual sleepiness occurred more frequently in the MD arm (P less than 0.01). Thirteen patients chose to continue on CDR, 2 on MD + HCT and 3 had no preference (P = 0.005). CDR is similar in antihypertensive effect to MD + HCT but is better tolerated with fewer withdrawals, fewer adverse effects, better compliance and has more patients electing to continue taking it.

Adult↗

Comparative study of beta andreoceptor antagonists on the isolated atria of control and of the reserpine treated rabbits.

The effect of four adrenoceptor antagonists, chosen because of reported differences in their selectivities, were compared using the positive chronotropic response to isoprenaline on isolated rabbit atria. Oxprenolol was the most potent antagonist of the isoprenaline induced cardiac arrhythmias. Alprenolol, practolol and propranolol also blocked the positive chronotropic responses to isoprenaline effectively. All the antagonists lowered the resting heart rate. The effects of all four selected antagonists on heart rate probably result from cardiac beta adrenoceptor blockade. Atria isolated from reserpine treated rabbits, showed a reduced percentage of increase in the heart rate in response to addition of isoprenaline. This decreased response has been related in some cases to direct myocardial inhibition.

Adrenergic beta-Antagonists↗

[Action of toxins isolated from scorpion and sea anemone venoms on ileum isolated from reserpine-treated guinea pigs].

We have shown that the ileum isolated from a reserpinized guinea Pig does respond to toxin II obtained from Scorpion venom but does not react to Anemonia sulcata toxin. We conclude that if Acetylcholine is the neurotransmitter inducing pharmacological activity of Scorpion toxin it is serotonin which triggers activity of Anemonia sulcata toxin in ileum of a normal guinea Pig.

Animals↗

[Simultaneous determination of 6 components contained in compound reserpine tablets by Kalman filtering spectrophotometry].

Kalman filtering spectrophotometry was investigated to assay the contents of vitamin B1, vitamin B6, chlordiazepoxide, dihydralazine sulfate, promethazine hydrochloride and hydrochlorothiazide in compound reserpine tablets consisting of 10 components. Absorption proportionality constant for each component was obtained by the application of non-negative least square method. The average recoveries for each were 97-103% with CV% less than or equal to 6.9 except vitamin B1 (n = 11).

Chlordiazepoxide↗