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Volume 75, Issue 8
Displaying 1-7 of 7 articles from this issue
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Yuichiro ARAI, Kumeji TAKEUCHI, Kenji YAMADA, Hiroshi KOGO, Yoshio AIZ ...1979 Volume 75 Issue 8 Pages 765-769
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSCarrageenin was injected into the knee joint cavity of rats, and influence of anti-inflammatory drugs on prostaglandin (PG) release in vitro from inflamed synovial membrane was studied. Release of PGE and F from inflamed synovial membrane was increased. Aspirin suppressed PGE and F release from non-inflamed and inflamed synovial membrane in vivo and in vitro, but suppression of PGF release was more intense. Hydrocortisone suppressed release of PGE and F from inflamed synovial membrane in vivo, and did not influence PG release in vitro. Release of PGE and F from non-inflamed synovial membrane was not influenced by hydrocortisone in vivo and in vitro. PGE content in inflamed synovial membrane was increased markedly, and PGE and F content in inflamed and non-inflamed synovial membrane was decreased markedly by aspirin in vivo. Content of PGE and F in non-inflamed and inflamed synovial membrane showed a tendency to decrease with hydrocortisone administration in vivo, but such was not significant.View full abstractDownload PDF (5963K) -
Kaito TSURUMI, Kimio YASUDA, Eiji MAKI, Hajime FUJIMURA1979 Volume 75 Issue 8 Pages 771-776
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffects of autonomic, anti-histaminic, anti-5HT drugs, papaverine and morphine on cathartic activity of spasmogens such as pilocarpine, 5-HT and prostaglandin E2 (PGE2) were tested by giving these drugs to mice subcutaneously. Mice used were male dd strain weighing 20±2 g and the cathartic effect was evaluated by the all or none method. The cathartic effect by pilocarpine was inhibited markedly by anti-cholinergic drugs such as atropine and diphenhydramine, but not by hexamethonium and methysergide. Therefore, the action of pilocarpine was found to be direct on the acetylcholine receptors. The cathartic effect by 5-HT was inhibited significantly by hexamethonium and methysergide. Atropine inhibited the cathartic effect of 5-HT, but the inhibitory activity was lower by about one hundredth than that on pilocarpine-induced diarrhea. It is suggested that 5-HT has dual sites of actions and there are less cholinergic and specific serotonergic actions. The cathartic effect by PGE2 was inhibited by anticholinergic, anti-5HT and ganglion blocking agents. PGE2 appears to possess the same mode of action as both pilocarpine and 5-HT. Papaverine inhibited little the cathartic effect of all three spasmogens, while morphine had a potent and nonspecific inhibitory effect on the cathartic action of all three spasmogens.View full abstractDownload PDF (7794K) -
Yutaka SAKAI1979 Volume 75 Issue 8 Pages 777-787
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe potencies of four benzodiazepine minor tranquilizers in depressing respiratory function were investigated in rats and cats anesthetized with pentobarbital. The effect of the drug on respiration was studied in the rat, and the effect on the phrenic nerve activity which reflects the activity of an inspiratory centre was investigated in the cat vagotomized bilaterally at the level of the neck. The change of blood pressure, heart rate and pCO2 in expiration were also recorded simultaneously in experiments witn the cat, an infra-red CO2 gas analyzer (Model LB-1, Beckman) was used to measure the pCO2. Respiration in the rat was decreased by the oral administration of diazepam 10, 20 mg/kg or chlordiazepoxide 20, 40 mg/kg. Although the pre-administration level of ventilation was not decreased by oxazolam or cloxazolam, both 20, 40 mg/kg, p.o., the level after administration was slightly lower than that after the administration of CMC alone. Diazepam, given intravenously either as a CMC-suspension or as the preparation Cercine®, in the dose of 0.5 mg/kg, suppressed both the number of the burst discharges and the magnitude of the integrated signal of the discharge of the phrenic nerve of the cat. Chlordiazepoxide 1 mg/kg, i.v. also slightly decreased the magnitude of the integrated signal. Oxazolam 1 mg/kg, i.v. had little effect on the phrenic activity. Cloxazolam 1 mg/kg, i.v., on the other hand, tended to increase the magnitude of the integrated signal but only immediately after the administration. It is suggested that the potencies which depress the respiratory function vary for each minor tranquilizer, namely the depressive actions of oxazolam and cloxazolam are weaker than those of diazepam and chlordiazepoxide.View full abstractDownload PDF (13533K) -
Katsushi YAMADA, Shuuzo HATTORI, Tatsuya HAKODA, Michiyo MIYAZAKI, Tam ...1979 Volume 75 Issue 8 Pages 789-798
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSTo establish a reliable laboratory assay for quantitating topical anti-inflammatory efficacy, the method of Tonelli et al was modified by employing felt fixed forceps, felt and sharp punch in Wistar rats. Croton oil, applied topically to the rat ear, elicited an acute phlogistic response which was maximal 6 hr after the application. The phlogistic response elicited by a single topical application of croton oil (1, 2, 5 and 10%) was increased in a dose-dependent manner, and croton oil, 5%, induced 63.2% increase of ear weight and was the optimal concentration for the experiment. Using this procedure, the antiphlogistic potencies of two corticoids were assayed under conditions of a blind test. ED50 of betamethasone valerate and diflucortolone valerate was 0.26 mg/ml and 0.0097 mg/ml, respectively, in Wistar rats, and 0.86 mg/ml and 0.016 mg/ml in Sprague Dawley rats, suggesting that diflucortolone valerate has an antiphlogistic potency of 27-56 relative to that seen with betamethasone valerate with minor differences in the strain of the rat. Our method should prove to be a useful assay for rapidly quantitating antiphlogistic activities of topically applied corticoids.View full abstractDownload PDF (12211K) -
Yukio MIZUSHIMA, Michio ISHIKAWA1979 Volume 75 Issue 8 Pages 799-804
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSBetamethasone 17, 21-dipropionate (BDP) does not have glycogenic activity and antagonizes cortisol in glycogenesis in fetal rat liver explants. In an attempt to elucidate whether BDP commonly has an antagonistic effect on the glucocorticoid responsive system in fetal rat liver, effects on activities of glycogen synthase and tyrosine aminotransferase were examined. Cortisol increased both total and α activities of glycogen synthase at concentrations above 3×10-8M. BDP, unlike cortisol, did not increase total synthase activity at 10-6M and antagonized cortisol (10-6M), but like cortisol, it did increase synthase α activity. Both cortisol and BDP increased tyrosine aminotransferase activity at concentrations above 10-8M. BDP did not always act as an antagonist in the glucocorticoid responsive systems in fetal rat liver.View full abstractDownload PDF (8005K) -
Effects due to the difference in strain, sex and drug administration time on physical dependence development and characteristics of withdrawal signs in CNS-affecting drug dependent ratsKohji YOSHIMURA, Ken-ichi YAMAMOTO1979 Volume 75 Issue 8 Pages 805-828
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSWe studied the influence of differences in strain, sex and drug administration time on physical dependence of morphine and phenobarbital in rats and also whether or not pole climbing avoidance is useful as an indicator of physical dependence. We then compared the behavioral characteristics seen with morphine-dependence with those of other CNS-affecting drugs. Withdrawal signs involving weight loss in morphine and phenobarbital groups were different in JCL-Wistar, SLC-Wistar, JCL-Sprague Dawley and HOS-Donryu strain rats. Withdrawal signs in males were generally more marked than in females. Withdrawal signs due to the difference of drug administration time were different with the sex and/or kinds of drugs. After administration of morphine-type and barbiturate-type drugs, withdrawal signs of sedation and weight loss, also excitability together with weight loss appeared 24 and 40 hours later, respectively. These signs were generally greatly increased by antagonist-induced withdrawal. Abrupt withdrawal of methamphetamine and cocaine caused no withdrawal signs. Rectal temperature was unchanged on abrupt withdrawal in the case of each drug, though temperatures did decrease with morphine-type drugs, and increased with phenobarbital and chlordiazepoxide groups, on antagonist-induced withdrawal. Inhibition of the avoidance was mild with the abrupt withdrawal of morphine, codeine, phenobarbital, chlordiazepoxide and cocaine, but was marked on antagonist-induced withdrawal of morphine and codeine.View full abstractDownload PDF (30003K) -
Keiichi TABATA, Hiroshi OHTSUKI, Susumu OKABE1979 Volume 75 Issue 8 Pages 829-836
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSA single oral administration of CH-800 induced a dose-dependent irritation of the stomach and intestine. As determined from the UD50 value (the dose inducing ulceration by 50%), the potency of gastric irritation was as follows; indomethacin>diclofenac Na>ibuprofen>aspirin>CH-800>phenylbutazone. Repeated administrations of CH-800 for 5 days induced a gastric irritation when given in doses from 3 to 100 mg/kg, however, the response was not dose-related. In contrast, the irritation of intestinal mucosa seen with CH-800 administration was dose-related. The degree of gastric or intestinal irritation seen with dosing of other drugs was as follows; indomethacin>diclofenac Na>ibuprofen>aspirin>phenylbutazone or indomethacin>CH-800=diclofenac Na>ibuprofen>phenylbutazone, respectively. CH-800 given for 5 days significantly delayed the healing of active ulcers and the healed ulcers showed a tendency toward re-ulceration. However, the irritating activity of phenylbutazone, diclofenac Na and ibuprofen was more potent than that of CH-800. Thus, CH-800 appears to have a rather weak irritative activity on the gastrointestinal tract of rats without ulceration, in contrast to other commonly clinically prescribed drugs.View full abstractDownload PDF (9572K)
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