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Volume 87 (1986)
- Issue 6 Pages 609-
- Issue 5 Pages 507-
- Issue 4 Pages 351-
- Issue 3 Pages 253-
- Issue 2 Pages 99-
- Issue 1 Pages 1-
Volume 87, Issue 2
Displaying 1-12 of 12 articles from this issue
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Noritaka YOSHIKAWA, Yoshiyuki SEYAMA, Saburo YAMASHITA, Michinori AKAS ...1986 Volume 87 Issue 2 Pages 99-104
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSWe observed that cepharanthine might exert its anti-allergic action by stimulating the secretion of corticosterone. The present experiments were carried out to investigate stimulation of the pituitary-adrenocortical system by cepharanthine. Administration of cepharanthine to rats produced increases in plasma and adrenal corticosterone levels. Administration of cepharanthine to propranolol pretreated rats also produced increases in plasma and adrenal corticosterone levels and plasma ACTH level. The elevation of corticosterone level induced by cepharanthine was considered to be the specific effect of cepharanthine. Cepharanthine did not increase plasma corticosterone level in rats in the state of dexamethasone suppression of the pituitary-adrenocortical system, in which the level was lowered. Administration of cepharanthine to Bordetella pertussis vaccine induced β-adrenergic blocked rats also produced increases in plasma and adrenal corticosterone levels. The production and release of corticosterone from an adrenal cell suspension were not influenced by cepharanthine in vitro. These results suggest that cepharanthine stimulates the pituitary-adrenotropic function.View full abstractDownload PDF (4305K) -
Eiko ONISHI, Toshio YAMADA, Kazuo YAMADA, Hajime INOUE, Yoshiyuki SEYA ...1986 Volume 87 Issue 2 Pages 105-112
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSIt is generally accepted that Diabetes mellitus is caused by the endocrinological functional disturbance of the pancreas, decreasing available insulin for carbohydrate metabolisms. Diabetes mellitus is not necessarily related to hypoinsulinemia, and some senile subjects show diabetic symptoms although the insulin levels in thier blood are within the normal range. Therefore, in order to examine the cause of Diabetes mellitus, the glucose tolerance test is usually given as a routine laboratory method to monitor the pancreatic endocrine functions. The pattern of decreasing glucose level in blood will tell us what is the cause of the disease. In testing the effects of anti-diabetic drugs, experimental diabetic conditions have been prepared by various methods, and recently streptozotocin (STZ) and cyproheptadine (CPH) have been successfully used to induce diabetic conditions of various degrees. In the present study, degree of disturbance of the pancreatic functions by STZ and CPH were compared, and in addition, disturbance of organs other than the pancreas was also examined biochemically. When a high dose of STZ was given, irreversible disfunction of glucose level normalizing and insulin secreting abilities was observed. Serum GOT, GPT, lysosomal enzyme activities and lysosomal enzyme activity in the liver and pancreas decreased in high dose STZ administrated rats. Low dose STZ disturbed the pancreatic endocrine function less than that in high dose STZ, and the blood glucose level normalizing function was reversibly disturbed. Insulin secretion decreased, and normalized on discontinuation of low dose STZ administration. Low dose STZ also disturbed organs other than the pancreas as in high dose STZ. On the other hand, CPH only disturbed the endocrine function of the pancreas, and blood level increased only on glucose loading; and the magnitude of increase of the blood glucose level on loading was more with CPH than with low dose STZ. Thus, CPH showed less pancreatic disturbance, but amplifies the glucose loading effect more, and the pancreatic disturbance is reversible. Such experimental results suggest that CPH administration would cause a mild and reversible diabetic condition, and since the disturbance is limited to the pancreas, the proposed experimental conditions might be of use for testing mild anti-diabetic drugs such as herbal, medicines.View full abstractDownload PDF (5608K) -
Katsuhiko NAKATA, Kazuo NISHIMURA, Toyokazu TAKADA, Hideyasu YAMAUCHI, ...1986 Volume 87 Issue 2 Pages 113-121
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSSA446 [(2R, 4R)-2-(o-hydroxyphenyl)-3-(3-mercaptopropionyl)-4-thiazolidinecarboxylic acid] (30 mg/kg/day), an orally active angiotensin-converting enzyme inhibitor, lowered significantly indirect systolic blood pressure (SBP) of 2-kidney, 1-clip renal hypertensive rats (RHR) by consecutive oral administration over a 14 week period. Daily oral dosing of hydralazine (2 mg/kg/day) for 14 weeks had little or no effect on SBP, but potentiated the antihypertensive effect of SA446. One to two weeks after discontinuation of the drugs, SBP in SA446 and the combination groups returned to the control level. Survival rates were 64%, 30% in the control and hydralazine group, respectively, but no death was observed in the SA446 group and the combination group throughout the administration period. Twenty-four hour urine volume and water intake tended to increase in the hydralazine group through the administration period, but increased apparently in the SA446 group and the combination group after discontinuation of the drugs. Daily oral dosing of SA446 (45 mg/kg/day) for over 16 weeks completely prevented the development of hypertension in spontaneously hypertensive rats (SHR). Daily oral dosing of hydralazine (2 mg/kg/day) similarly prevented the development. The combined effect with SA446 and hydralazine on the development was also observed. SBP in the SA446 group and the combination group increased gradually after discontinuation of the drugs, but were maintained at a low level as compared with the control group 3 weeks after discontinuation, while hydralazine gave a rapid return. No influences were observed in 24 hr-urine volume and water intake during and after the administration period in SHR. These results demonstrate that long-term treatment with SA446 could maintain the antihypertensive effect in RHR and prevent the development of hypertension in SHR and that the combined effect with SA446 and hydralazine was also observed on the antihypertensive effects.View full abstractDownload PDF (6560K) -
Koji TAKEUCHI, Osamu FURUKAWA, Hironori TANAKA, Hideyuki NISHIWAKI, Su ...1986 Volume 87 Issue 2 Pages 123-133
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSWe studied the effects of elcatonin (eel calcitonin), on various gastric and duodenal lesions, gastric acid and duodenal alkaline secretion, and gastric motility in rats. Elcatonin at 1 ?? 30 unit/kg, given subcutaneously, dose-dependently inhibited the development of HCl-aspirin-, HCl-ethanol-, water-immersion stress- and indomethacin-induced gastric lesions. This agent also significantly prevented the formation of duodenal lesions induced by indomethacin plus histamine at 30 unit/kg, although it showed only a tendency of inhibition against mepirizole-induced duodenal lesions. 16, 16-Dimethyl prostaglandin E2 (3 ?? 30 μg/kg), given orally as a reference drug, showed a potent inhibition against all types of lesions tested herein at the dose of 3 μg/kg or greater. Elcatonin dose-dependently inhibited gastric secretion (volume, acid and pepsin output) in pylorus-ligated rats and gastric motility in conscious rats, but had no effect on duodenal alkaline secretion in anesthetized rats. On the other hand, 16, 16-dimethyl prostaglandin E2 at 10 μg/kg, given intraduodenally, significantly inhibited gastric secretion and motility, but stimulated duodenal alkaline secretion. We conclude that elcatonin markedly protects the gastrointestinal mucosa from injury induced by stress or various irritants. These effects might be in part accounted for by the antisecretory and antimotility activities of this peptide, although some other unknown mechanisms may be involved in the mucosal protection afforded by elcatonin.View full abstractDownload PDF (7864K) -
Daisuke HOURI1986 Volume 87 Issue 2 Pages 135-142
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSA mirror-covered staircase was erected to study screening methods, and several basic experiments were carried out using it. The staircase consisted of 5 steps each measuring 15 cm long by 20 cm wide by 6 cm high, fabricated in a wooden device measuring 95 cm by 20 cm by 30 cm high. The inner surfaces were all mirrored, including steps, floors and walls. At the foot of the stairs, a rat weighing about 200 g was placed quietly with the back toward the stairs. The frequencies of rearing and climbing on the stairs were recorded for the subsequent 3 and 10 min. The recordings were also performed using 2 rats placed simultaneously and in a non-mirrored device of the same structure. When mirrored, the frequencies of rearing and climbing were much higher, and the average duration lasted also longer than when non-mirrored. To compare the results among the following 3 qualifications: i) a rat in the mirrored device, ii) 2 rats in the mirrored device, and iii) 2 rats in the non-mirrored device, the highest frequency of rearing for the first 3 min was observed in i). Effects of nitrazepam, phenobarbital and morphine were compared between mirrored and non-mirrored qualifications. No significant differences between them were observed in the drug-induced changes in the behaviors. Although the mirrored staircase test as a screening method was almost identical to the non-mirrored test, it was superior in the point of continuation of augmented frequencies. As a fact arousing interest, the subject received more potent stimulation from its self image exposed on the mirrors than the image of another individual of the same species (within the same device).View full abstractDownload PDF (5465K) -
Akihiro TOBE, Mitsuo EGAWA, Noriko HASHIMOTO, Rie NAGAI, Kouko ISHIKAW ...1986 Volume 87 Issue 2 Pages 143-159
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSGeneral pharmacological action of 4-(o-Benzylphenoxy)-N-methylbutylamine hydrochloride (bifemelane hydrochloride, MCI-2016) was examined with regard to the effects mainly on the central nervous system. MCI-2016, at 30 ?? 100 mg/kg, p.o., only showed a weak sleep prolongation effect (mice), anti-convulsant action (mice) and a moderate facilitation of exploratory behavior, but produced no remarkable behavioral changes. Above the doses of 200 to 300 mg/kg, p.o., MCI-2016 produced a decrease in muscle or body tone, mydriasis and a slight decrease of locomotor activity. The drug, however, showed little influence on exploratory behavior, conditioned avoidance response and normal body temperature (rats). Normal body temperature in rabbits was also little affected by MCI-2016. Effects on EEG was characterized by moderate activation of spontaneous EEG and potentiation of arousal response by stimulation of the midbrain reticular formation (1.5 ?? 5 mg/kg, i.v.). The drug, however, did not significantly change the sleep-wakefulness cycle and REM-sleep in rats. MCI-2016 also showed little influence on spinal reflex potentials and neuromuscular junction at high doses (10 mg/kg, i.v.). These results may indicate that MCI-2016 has slight influence on overall behavioral and motor changes. Effects of MCI-2016 on acetic acid-induced writhing, carrageenin edema and corneal reflex were also examined. MCI-2016 showed moderate analgesic and anti-inflammatory actions at 50 100 mg/kg, p.o., and also showed local anesthetic action. The duration of local anesthetic action was relatively long but the drug produced no local damage.View full abstractDownload PDF (11549K) -
Yoshikuni TAMAO, Hiroto HARA, Kohei UMEZU, Jindo ITO, Akiko DOI, Atsuk ...1986 Volume 87 Issue 2 Pages 161-167
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSMCI-2016 showed little influence on coagulation (APTT) and fibrinolysis (plasma clot lysis activated by urokinase) at doses (concentrations) as high as 300 mg/kg, p.o. or 8.6×10-4 M. Hemolytic action of MCI-2016 was only observed at the concentrations above 2 mM. The drug also showed no influence on blood glucose level (30 ?? 300 mg/kg, p.o.). Effects of MCI-2016 on hemorheological properties were studied either in vitro or ex vivo. Above the doses (concentrations) of 100 mg/kg, p.o. and 10 μM, MCI-2016 suppressed the mechanical hemolysis and accelerated the membrane filtration rate. These effects of MCI-2016 were superior to those of cinepazide, Ca-hopantenate, meclofenoxate and pentoxyfylline. MCI-2016 also inhibited platelet aggregation induced by collagen with the IC 50 of 35 to 60 μM (rabbit and human platelets). Secondary aggregations of ADP and epinephrine were also inhibited by MCI-2016. As for reference drugs, bencyclane showed inhibitory patterns similar to MCI-2016. Other drugs examined exhibited little effect. In summary, it may be suggested that MCI-2016 exhibits beneficial influences in the clinical fields of cerebrovascular diseases.View full abstractDownload PDF (5239K) -
Shigefumi TAKEDA, Shunichi MAEMURA, Kazuhiko SUDO, Yoshio KASE, Ichiro ...1986 Volume 87 Issue 2 Pages 169-187
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSEffects of oral administration of gomisin A, one of the components isolated from Schizandra fruits, on liver injuries induced by CCl4, d-galactosamine and dl-ethionine and on liver microsomal drug-metabolizing enzyme activities were investigated. Gomisin A suppressed the increase of serum transaminase activities and the appearances of histological changes such as degeneration and necrosis of hepatocyte, inflammatory cell infiltration and fatty deposition in each type of liver injury. The repeated administration of gomisin A (30 or 100 mg/kg, p.o., daily for 4 days) induced an apparent increase of liver weight in liver-injuried and normal rats. Gomisin A decreased serum triglyceride and lipid contents of the liver in biochemical studies. Increases of microsomal cytochrome b5 and P-450, elevations of NADPH cytochrome C reductase, aminopyrine N-demethylase and 7-ethoxycoumarin O-deethylase activities and decrease of 3, 4-benzo(a)pyrene hydroxylase activity per cytochrome P-450 were observed after the administration of gomisin A. In addition, gomisin A was found to enhance the in corporation of 14C-phenylalanine into liver protein and to shorten the hexobarbital-induced sleeping time. These changes caused by gomisin A were similar to those by phenobarbital. However, gomisin A is distinctly different from phenobarbital in the finding that phenobarbital lessened the survival ratio of CCl4-intoxicated mice, but gomisin A did not. Our observation suggest that gomisin A shows an antihepatotoxic action by oral application and also has hypolipidemic (mainly triglyceridemic) and liver protein synthesis-facilitating actions and that the enlargement of the liver seen with gomisin A is the adaptive hypertrophy which is due to the induction of drug-metabolizing enzymes.View full abstractDownload PDF (16894K) -
Yoshimi SHIRAKURA1986 Volume 87 Issue 2 Pages 189-197
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSAn increase in urinary flow has been observed in rats during cataleptic response to haloperidol. The present experiment was carried out to study the mechanism of haloperidol-induced diuresis. Wistar-Imamichi adult female rats were injected i.p. with haloperidol in a dose of 0.1, 1 or 10 mg/kg, and the time course of changes in urine volume was observed. The dose-dependent diuretic effect of 1 or 10 mg/kg haloperidol was significant from 4 hr afterward, and the haloperidol-induced diuresis was prevented by pretreatment with phenoxybenzamine, prazosin or yohimbine. Chlorpromazine but not spiperone and pimozide induced a significant increase in urine volume, though the effect of chlorpromazine was less marked as compared with that of haloperidol. Clonidine in a dose of 0.125 ?? 1.0 mg/kg enhanced urine flow markedly from 30 min, and the same α-adrenergic blockers were also effective in blocking the diuretic effect of clonidine. Urinary osmolarity in 1 mg/kg haloperidol and 0.125 mg/kg clonidine-treated rats decreased significantly, whereas only clonidine stimulated urinary Na and K excretion. Plasma osmolarity and negative free water clearance did not change in both haloperidol and clonidine-treated rats. The present results suggest that the haloperidol-induced diuretic effect could be due to the central α-adrenoceptor blocking action of haloperidol.View full abstractDownload PDF (7133K) -
Ikunobu MURAMATSU, Motohatsu FUJIWARA1986 Volume 87 Issue 2 Pages 199-207
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSVasorelaxing effects of nicorandil, a new antianginal drug, were examined in isolated rat thoracic aorta and compared with those of nitroglycerin and Ca antagonists (verapamil and diltiazem). Nicorandil at concentrations over 10-7 M produced a potent relaxation in norepinephrine-contracted aortic strips, and the EC50 was 2.2×10-6 M. The relaxing pattern varied between the different concentrations of nicorandil. At 10-5 M, the response was transient; after the peak relaxation, the tension gradually returned to the precontracted level. Rhythmic contraction occurred during the recovery. At a higher concentration (10-4 M), the relaxation lasted for more than 30 min. In the aortic strips which had been treated with Ca antagonists beforehand, nicorandil at all concentrations tested produced a long lasting relaxation, and the rhythmic contraction did not appear during exposure to nicorandil. Pharmacological analyzing experiments revealed that nicorandil at concentrations lower than 10-5 M inhibits intracellular Ca release and the receptor-operated Ca channel, but that at higher concentrations the voltage-dependent Ca channel is also inhibited. Nitroglycerin produced a transient relaxation by mechanisms similar to those proposed at low concentration of nicorandil. Ca antagonists selectively inhibited the voltage-dependent Ca channel. From these results, it is suggested that nicorandil has both the pharmacological profiles of nitroglycerin and Ca antagonists.View full abstractDownload PDF (6066K) -
Effects on gross-behavior in rats and monkeys and on DRL response, CER, and CAR in ratsMichio YAMAMURA, Kayoko MAEDA, Hiroyuki NAKAGAWA, Ryuichi ISHIDA1986 Volume 87 Issue 2 Pages 209-221
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSWhether nicergoline has psychotropic-like pharmacological properties was examined through the gross-behavioral and operant behavioral observations in rats and monkeys. In gross-behavioral observations, slight decrement of spontaneous motor activity, lying on the abdomen and relaxation of abdominal tone were observed in rats when nicergoline was administered intravenously (1 mg/kg or more) and intraperitoneally (4 mg/kg or more). However, when it was administered orally, slight decrement of spontaneous motor activity was observed only at large doses of 32 and 128 mg/kg. In monkeys, nicergoline produced decrement of spontaneous motor activity, palpebral ptosis, and lacrimation when administered intraperitoneally at doses of 1 mg/kg or more. Under a differential reinforcement of low rate (DRL) schedule for food reinforcement in rats, nicergoline depressed the response at 4 mg/kg, i.p., or 128 mg/kg, orally. In conditioned emotional response (CER), nicergoline had no effect on the responses during both the alarm and safe periods at doses of 0.25, 1, and 4 mg/kg, i.p., or 8, 32, and 128 mg/kg, p.o. In Sidman continuous avoidance response (CAR), nicergoline (0.25, 1, and 4 mg/kg, i.p., or 8, 32, and 128 mg/kg, p.o.) slightly depressed the response and increased the total shock. These results were compared with those of chlorpromazine, chlordiazepoxide, pentobarbital, and methamphetamine and the following conclusion was drawn: Inhibitory effects of nicergoline on gross and operant behaviors seem to be non-specific, and its behavioral pharmacological properties are qualitatively different from those of anti-psychotics, anti-anxietics, hypnotics, and stimulants.View full abstractDownload PDF (9834K) -
Influence on respiratory and cardiovascular systems, renal function, autonomic nervous system, isolated smooth muscle and digestive organsAkihiro NARIMATSU, Ken-ichiro NAKAO, Hidenobu IKOMA, Mitsuo EGAWA, Yos ...1986 Volume 87 Issue 2 Pages 223-251
Published: 1986
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSMCI-2016 at 3 mg/kg, i.v., caused slight changes in systemic blood pressure (SBP), heart rate (HR), respiratory rate (RR) and ECG but at 10 mg/kg, i.v., it caused a significant increase in RR, decrease in SBP, increase or decrease in HR and a moderate change in ECG. Biphasic changes in SBP, HR and blood flow were sometimes observed after high doses. MCI-2016 also decreased SBP at 30 mg/kg, i.p., in SHR. MCI-2016 (50 mg/kg, p.o./day) showed little influence on SBP, HR and ECG in conscious beagle dogs. In isolated hearts, MCI-2016 decreased HR and contractility at the concentrations above 10-5 g/ml, and 30 μg, i.a. MCI-2016 prolonged the AVCT at 10 mg/kg, i.v. MCI-2016 (i.v. or i.a.) moderately increased cerebral and femoral artery blood flows. MCI-2016 did not change CMRO2, but decreased MVO2. Coronary and renal artery flows were moderately increased by 10 mg/kg, i.v., of MCI-2016. Renal function was suppressed after 10 mg/kg, i.v., or 300 mg/kg, p.o., of MCI-2016. MCI-2016 potentiated the action of NE (increase in SBP, contractions of nictitating membrane and vas deferens), but showed little anti-cholinergic action. In contrast, MCI-2016 moderately increased gastrointestinal motility and salivatory response. As for the influence on isolated smooth muscles, MCI-2016 antagonized the contraction of blood vessels by high K+ at 10-6 g/ml, or more, and it depressed the contractions by ACh, 5-HT, histamine and BaCl2 and also depressed spontaneous movements of uterus and ileum at 10-5 M or more, in a nonspecific manner. MCI-2016 had no influence on liver damage and bile secretion, but inhibited stress ulcer and gastric acid secretion on the one hand, and caused gastric damage (125 mg/kg p.o., or more) on the other hand.View full abstractDownload PDF (1428K)
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