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Volume 83 (1984)
- Issue 6 Pages 479-
- Issue 5 Pages 373-
- Issue 4 Pages 269-
- Issue 3 Pages 193-
- Issue 2 Pages 93-
- Issue 1 Pages 1-
Volume 83, Issue 4
Displaying 1-11 of 11 articles from this issue
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Shiroh KISHIOKA, Yoshiyuki IGUCHI, Masanobu OZAKI, Hiroyuki YAMAMOTO1984 Volume 83 Issue 4 Pages 269-280
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe nucleus reticularis gigantocellularis (NRGC), including the nucleus reticularis paragigantocellularis (NRPG), of male Sprague Dawley rats was destructed bilaterally by DC 0.5 mA for 40 sec (D-rats). Morphine analgesia estimated by the tail pinch method in 4 and 10 days morphine treated sham operated rats (S-rats), of which the test doses were 40 and 80 mg/kg, respectively, was equal to or smaller than the analgesia by 5 mg/kg in non-treated S-rats. Morphine analgesia at 5 mg/kg in non-treated D-rats was weaker than that in S-rats. Morphine analgesia in 4 and 10 days morphine treated D-rats, of which the test doses were 40 and 80 mg/kg, respectively, was stronger than the analgesia by 5 mg/kg but weaker than that by 20 mg/kg in non-treated D-rats. These results indicate development of morphine tolerance in S and D-rats. Reverse of diurnal variation in body weight and disappearance of diurnal variation in body temperature and in plasma corticosterone concentration (Pcs) were observed similarly in Sand D-rats during morphine treatment. Body weight loss, increase in Pcs and plasma ACTH concentration, and increase in adrenal weight were elicited by morphine withdrawal in both morphine treated S and D-rats. These signs during morphine treatment and after morphine abstinence indicate the development of morphine dependence in D-rats. These results suggest that the NRGC participates in development of morphine analgesia, but does not participate in development of morphine tolerance and dependence.View full abstractDownload PDF (6481K) -
Keigo NISHINO, Mitsuo OHASHI, Saburo HARA, Sae SUZUKI, Tsutomu IRIKURA1984 Volume 83 Issue 4 Pages 281-289
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe effects of 3-isobutyryl-2-isopropylpyrazolo (1, 5-a) pyridine (KC-404), a new anti-allergic agent with a unique mode of action, on bronchial anaphylactic reactions were investigated in guinea pigs and rats. The inhibitory effects of orally administered KC-404 on systemic anaphylactic reaction caused by intravenous antigen and on anaphylactic bronchoconstriction caused by inhaled antigen in guinea pigs actively sensitized with egg albumin were observed at doses of 100 mg/kg and 10 mg/kg, respectively. When these animals were pretreated with diphenhydramine and atropine before antigen challenge, the inhibitory effects of KC-404 were markedly enhanced; doses as low as 0.25 to 0.5 mg/kg p.o. were effective in this situation. In guinea pigs similarly sensitized as above, KC-404 injected i.v. after the maximum development of antigen-induced constriction of airways resulted in a rapid dilatation. KC-404 was about 100 times as potent as aminophylline in this respect. KC-404 inhibited passive anaphylactic bronchoconstriction in rats mediated by an IgE antibody at an oral dose of 2.5 mg/kg. The inhibitory effect of KC-404 (10 mg/kg) persisted for at least 6 hr. These results indicate that KC-404 is orally effective in inhibiting anaphylactic bronchoconstrictions mediated by IgE as well as IgG antibodies. Furthermore, KC-404 is suggested to be able to control the SRS-A-induced component of bronchospasm.View full abstractDownload PDF (4622K) -
Keigo NISHINO, Saburo HARA, Tsutomu IRIKURA1984 Volume 83 Issue 4 Pages 291-299
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe effects of 3-isobutyryl-2-isopropylpyrazolo [1, 5-a] pyridine (KC-404), a new anti-allergic agent, on type I to IV allergic reactions were investigated. KC-404 administered orally inhibited heterologous and homologous passive cutaneous anaphylaxis (PCA) reactions in guinea pigs and homologous PCA in rats; the minimum effective doses were 50, 12.5 and 3 mg/kg, respectively. However, the inhibition of PCAs by KC-404 was incomplete so that only 50 to 60% inhibitions were obtainable even at the highest doses used. KC-404 had no effect on increased vascular permeability by chemical mediators other than SRS-A and hardly affected antigen-induced degranulation of the sensitized mesenteric mast cells in vitro. These results suggest that KC-404 exerts its effect conceivably through inhibition of the SRS-A-mediated component of PCA. KC-404 had no effect on type II allergic reaction as estimated by its failure to inhibit reversed cutaneous anaphylaxis in rats and the Forssman systemic reaction in guinea pigs. Also, no influence on complement activity was observed in vitro and in vivo. KC-404 (100 ?? 200 mg/kg, p.o.) produced a marked inhibition of passive and active Arthus reactions in guinea pigs and rabbits, respectively. The tuberculin reaction in guinea pigs was not affected by KC-404. These results suggest that KC-404 inhibits PCAs mediated by IgE as well as IgG antibodies probably through a unique mechanism of action. KC-404 was shown to be effective also on type III allergic reaction.View full abstractDownload PDF (4439K) -
Kazuyoshi HORISAKA, Sonoko MASUDA1984 Volume 83 Issue 4 Pages 301-307
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSTwo drugs, trifluoropentoxypicolinic acid (TFP) and 5-butoxypicolinic acid, which are composed of a picolinic acid skeleton and an alkoxyl group, were studied to determine characteristics of their antihypertensive effect. The study was carried out using normotensive rats and experimental hypertensive rats (DOCA type hypertensive, one-kidney type hypertensive and spontaneous hypertensive), and effects of these drugs were compared with those of fusaric acid (5-butylpicolinic acid), which is known as a hypotensive agent inhibiting dopamine β-hydroxylase. The hypotensive effect of the drugs (10, 30 and 100mg/kg, p.o.) on normotensive rats was weaker than on hypertensive rats. TFP showed a dosedependent hypotensive effect which was not influenced by reserpine pretreatment. Though TFP showed the same inhibitory effect on serum dopamine β-hydroxylase as fusaric acid, it had only approximately 0.5 times the inhibitory activity. However, TFP had a hypotensive effect which was 1.4 times stronger than that of fusaric acid. According to pharmacokinetic analysis based on the determination of blood drug concentration, the transfer rate of fusaric acid from the digestive tract to the blood was much higher than TFP by 1.6×104 times. Moreover, fusaric acid had a 4.5 times greater disappearance rate than TFP. From the above results, first of all, it is supposed that the antihypertensive effect of TFP is related to inhibition of dopamine β-hydroxylase. In addition, it is suggested that prolonged presence of unchanged TFP in the blood increases its immediate depressive effect on the cardiovascular system, thereby causing a strong hypotensive effect.View full abstractDownload PDF (3735K) -
Yukio ICHINOSE, Ayako KAGA, Eiichi MATSUI, Yoshio UTSUGI, Hideo TSUYUK ...1984 Volume 83 Issue 4 Pages 309-315
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSRandomized male litter S.D. rats (weight: about 60 g, I group: 10 rats) were used. By using Crisco (hydrogenated cotton seed oil) within the limits of 10 ?? 60%, the intake of the 30% group was high and a good incidence rate of obesity (about 100%) was obtained in the 6 month experiment. In the 30% group, increases of wet weight in perirenal retroperitoneal and subcutaneous fat depots, increases of the number and diameter of fat cells (perirenal retroperitoneal fat depot), elevations of liver fat % and serum insulin level, and a fall of liver phosphoenolpyruvate carboxykinase activity were observed in the 3 month experiment.View full abstractDownload PDF (4712K) -
Yasuo ABE, Haruo SEKIGUCHI, Kiyoyuki TSURU, Tsutomu IRIKURA1984 Volume 83 Issue 4 Pages 317-324
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSEffects of 3, 4, 5-trimethoxy-N-(3-piperidyl) benzamide (KU-54), an antiulcer drug, on the tissue respiration of the gastric mucosa and the liver were studied in rats. Oral KU-54 at 100 mg/kg twice daily for 5 days (though it was given only once on the 5 th day) caused an increase in oxygen consumption of the gastric mucosa in rats, but did not affect that of the liver. Thus the principal active site of KU-54 on tissue respiration was found to be the gastric mucosa. Oral KU-54 at 100 mg/kg once daily for 11 days significantly accelerated the oxygen consumption of marginal gastric mucosa of acetic acid ulcer in rats. The effect of oral gefarnate at 200 mg/kg was about half that of KU-54 at 100 mg/kg, but it was not significant. In addition. oral KU-54 at 100 mg/kg twice daily for 5 days (though it was given only once on the 5th day) significantly inhibited the decrease of oxygen consumption of the gastric mucosa in hemorrhagic shocked rats. The effect of oral gefarnate at 100 mg/kg was not like that at KU-54 at 100 mg/kg in conscious rats. When KU-54 was added in the incubation medium with small gastric mucosal fragments of rats, the increase of oxygen consumption of the gastric mucosa did not occur. Oral KU-54 at 100 mg/kg significantly accelerated a glycogen consumptive stimulation of the gastric mucosa of the corpus in ischemic rats, but the respiration of the antral mucosa was not accelerated under anaerobic incubating conditions. Oral gefarnate at 200 mg/kg accelerated an anaerobic glycolysis of the eastric antral mucosa in rats.View full abstractDownload PDF (3881K) -
Kiyoko KAJI, Yoshiyuki SEYAMA, Saburo YAMASHITA1984 Volume 83 Issue 4 Pages 325-329
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSActive fractions that possess the hypocholesterolemic effect of iodine egg yolk lipid fraction have been investigated with male Wistar strain rats fed on a cholesterol-rich diet. Iodine egg yolk lipid was extracted by Folch's (chloroform: methanol) method and was refractionated into a neutral lipid (IEYNL) fraction and a polar lipid (IEY-PL) fraction. The iodine content in each fraction was determined. The animals were kept on the cholesterol-rich diet for 5 days, and then they were fed the fractions in addition to the above diet for 10 more days. The hypocholesterolemic effect was seen most significantly with the IEY-NL fraction. The serum total cholesterol level in rats receiving this fraction was 70% as compared with that of the Ch group (fed on the cholesterol diet). However, the liver total cholesterol level was not affected or rather increased by the IEY-NL fraction. Another fraction (IEY-PL) showed no such effect. Iodine content in the IEY-NL fraction was quite low (0.2ppm) compared with the other fractions. The daily dose in terms of iodine in the IEY-NL fraction was only the amount equivalent to 1/50 of the reported daily requirement for the rat. The IEY-NL fraction induced the hypocholesterolemic effect, though it contained only a trace of iodine.View full abstractDownload PDF (2673K) -
Kodo OKADA, Toshiro MOCHIZUKI, Yoshinori SHINOHARA, Saiko TAKAHASHI, K ...1984 Volume 83 Issue 4 Pages 331-343
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe hypolipidemic properties of KCD-232(4-(4'-chlorobenzyloxy) benzyl nicotinate), a new compound, were studied in rats fed a basal diet and mice fed a high-cholesterol diet with the following results: 1) KCD-232 reduced serum cholesterol (CH), triglyceride (TG) and phospholipid (PL) levels in a dose-dependent manner (20-160 mg/kg/day) in rats fasted for 16 hr. 2) KCD-232 significantly reduced (LDL+VLDL)-CH and decreased the (LDL+VLDL)-CH/HDL-CH ratio designated as the “atherogenic index” unlike clofibrate which was used as a reference. 3) KCD-232 slightly increased relative liver weight, but not in the dose-dependent manner of clofibrate. 4) KCD-232 also inhibited the elevation of serum CH level in mice fed a high-cholesterol diet in a dose-dependent manner, and this inhibitory effect was more pronounced than those of clofibrate and nicotinic acid (NA). 5) Liver CH and fatty acid (FA) synthesis from [1-14C] acetate were inhibited both in vitro and in vivo in rats orally administered KCD-232. Clofibrate also decreased CH synthesis, whereas it increased FA synthesis. NA had no effect on either synthesis. 6) After oral administration of [4-14C] cholesterol to rats that were cannulated into the thoracic-duct lymph, KCD-232 markedly depressed the appearance of "C-cholesterol in lymph. 7) KCD-232 induced no proliferation of hepatic peroxisomes in rats, unlike clofibrate. The detailed hypolipidemic mechanism of KCD-232 is not yet clear, but as shown, it decreased CH synthesis in the liver, exogenous CH absorption from the intestine and FA synthesis in the liver. These results suggest that the serum lipid-lowering profiles of KCD-232 differ from those of clofibrate and NA.View full abstractDownload PDF (7252K) -
Fusao AMANUMA, Shigeru OKUYAMA, Syuzo ORIKASA, Sanae HASHIMOTO, Chieko ...1984 Volume 83 Issue 4 Pages 345-354
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe analgesic and antipyretic effects of oxaprozin were investigated in comparison with those of indomethacin, ibuprofen, phenylbutazone and aspirin. On the various writhing tests in mice, the analgesic effect of oxaprozin was about 2 to 9 times more potent than those of ibuprofen, phenylbutazone and aspirin. On the other hand, the analgesic and antipyretic effects of oxaprozin in rats were roughly equivalent to those of aspirin, but less effective than those of the other drugs tested. On the urate synovitis test in dogs, only oxaprozin showed a prophylactic effect. Therefore, The effect of oxaprozin in mice and dogs was more potent than ibuprofen, phenylbutazone and aspirin. The metabolic rate of oxaprozin in rats is 3.5 and 7.2 times more rapid than in mice and dogs, respectively, and its blood level in rats is low. Moreover, the biological half-life of oxaprozin is 39 to 43 hr and 49 to 69 hr in dogs and humans, respectively. From these results, it is suggested that oxaprozin is more potent than ibuprofen, phenylbutazone and aspirin, and in clinical use, it is a long acting anti-inflammatory drug.View full abstractDownload PDF (4770K) -
Hiroyuki MIBU, Junichi HASEGAWA, Masayuki NIWA, Masakatsu NOZAKI, Kait ...1984 Volume 83 Issue 4 Pages 355-362
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe active oxygen produced from stimulated phagocytic cells emitts luminol-dependent chemiluminescence (CL) upon reaction with luminol. So the active oxygen was measured by using the CL and the results of this were compared with those by the LDH-NADH method. Moreover, effects of nonsteroidal antiinflammatory drugs (NSAID) on the generation of active oxygen were studied by both methods. Rat peritoneal and pleural exudated cells (PEEC and PLEC) emitted strong CL on incubation with zymosan, but that from rat whole blood cells was very weak. The effects of superoxide dismutase, catalase, NaN3 and L-ascorbic acid on the generation of active oxygen from rat phagocytic cells were different between CL and LDH-NADH methods. These discrepancies seem to be due to the different kinds of active oxygen that can be measured by both methods. Except for BW-755C, most of the NSAID had only a slight inhibitory effect on the generation of active oxygen measured by both methods, and the ex vivo effect was the same as that observed in vitro. It may be considered that NSAID decrease the phagocytic function of cells by non-specifically stabilizing the biological membrane and inhibit slightly the generation of active oxygen from phagocytes. On the other hand, the CL method could be performed not only in PEEC and PLEC, but also in whole blood cells. From these results, it was suggested that CL measurement can be used as a simple and valuable method for the detection of all types of active oxygen including superoxide anion radical and its metabolites and for testing cellular functions and drug actions on them.View full abstractDownload PDF (4066K) -
Masaru MINAMI, Hiroko TOGASHI, Machiko SANO, Iwao SAITO, Akira NOMURA, ...1984 Volume 83 Issue 4 Pages 363-371
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSA chronobiological study of behavioral changes in Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke prone spontaneously hypertensive rats (SHRSP) was undertaken. Attention was focused on changes in ambulatory activity and drinking behavior using an Ambulo-Drinkometer, the effects of centrally acting antihypertensive drugs, and the relationship between behavioral changes and humoral factors. (1) The experiment was performed during a light-dark alternation cycle. Approximately 10 days were required for rats to acclimate to new cages. (2) Using power spectral analysis, a 24 hr periodicity was dominant in both sexes of WKY and SHRSP. A 120 hr periodicity was demonstrated in female SHRSP. This long periodicity may have been due to a female sexual rhythm. (3) Ambulatory activity of WKY and SHRSP tended to decrease with age. (4) After abrupt cessation of clonidine administration, an ambulatory ultradian rhythm was demonstrated. Guanfacine treated SHR showed less change in ambulatory ultradian rhythm than clonidine treated SHR. (5) Using a Drinkometer with attached metabolic cages, drinking counts, urinary volumes, urinary aldosterone and catecholamine excretion rates were higher during the dark phase than during the light phase. It was demonstrated that analysis of rhythmicities and measurement of behavioral amplitude are both needed in the study of behavioral pharmacology.View full abstractDownload PDF (4447K)
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