Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 91, Issue 2
Displaying 1-7 of 7 articles from this issue
  • Yu YAMAGUCHI, Yoshiko FUTAGAWA, Masaru KUNITOMO, Yoshio BANDO
    1988 Volume 91 Issue 2 Pages 61-69
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The effects of dietary linoleic acid on serum lipids, lipid peroxides and aortic cholesterol were studied in mice fed a purified diet enriched with 5% cholesterol for a period of 14 weeks. The diet was supplemented with 10% coconut oil (Group I), lard (Group II), corn oil (Group III) or linoleic acid (Group IV) to give various levels of linoleic acid. After 4 to 12 weeks, the increment of serum total cholesterol was retained in the following order: group IV>III>II>I, which was the same order as the linoleic acid content in the diet. At week 14, the levels of serum free and esterified cholesterol, HDL-cholesterol, triglycerides and phospholipids were highest in group IV and lowest in group I. The serum lipid peroxide level was higher in the order of group IV>III>II>I. The ester ratio of cholesterol, the atherogenic index and LCAT activity were not significantly different among the four groups. Gallstone formation was markedly observed with higher dietary linoleic acid intake. Aortic cholesterol levels also increased in the same order as the dietary linoleic acid level: group IV>III>II>I. There were significant positive correlations between the aortic cholesterol level and all the serum lipid levels, and also the lipid peroxide level. All these findings indicate that under hypercholesterolemic conditions, excess dietary linoleic acid can increase serum lipids and lipid peroxide levels, resulting in lipid deposition in the aorta. These metabolic alterations may adversely influence atherogenesis.
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  • Hisashi SATOH, Takao TERAI, Hajime NAKANISHI, Takaharu ONO, Fumio SHIB ...
    1988 Volume 91 Issue 2 Pages 71-80
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Tiapride is a central dopamine receptor specific antagonist, and it has a benzamide chemical structure. This drug is very useful for the treatment of dyskinesia and such abnormal behaviors as delirium and psychomotor excitation in patients with arteriosclerosis. Most of these patients are elderly and generally suffer from other diseases. Since they are apt to be treated with several drugs for such diseases, the effect of tiapride in combination with various kinds of drugs was examined in rats and mice. Tiapride significantly potentiated the catalepsy-inducing effect of haloperidol and chlorpromazine in rats and tended to potentiate the muscle relaxing effect of diazepam at the highest dose in mice. Conversely., tiapride did not enhance or diminish the hypnotic effect of bromvalerylurea, the anti-cholinergic activity of trihexyphenidyl, the diuretic effect of trichloromethiazide, or the anti-diabetic effect of glibenclamide. Our findings suggest that tiapride should be used with care in patients taking neuroleptics, but can be used freely in patients on other kinds of drugs.
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  • Masahiro MIZOTA, Yukio KATSUKI, Kiyoshi MIZUGUCHI, Shoji ENDO, Haruo M ...
    1988 Volume 91 Issue 2 Pages 81-89
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The effects of highly purified ethyl ester of eicosapentaenoic acid (EPA-E) on ellagic acid-induced thrombus formation in the stenosed femoral artery in rabbits and on the progression of laurate-induced vascular lesions in rats were examined. (1) EPA-E in single administration significantly prevented the thrombus formation induced by ellagic acid in the stenosed femoral artery of rabbits. (2) EPA-E restored the hypercoagulation activity at 5 min and 3 hr after the ellagic acid injection. Platelet aggregability induced by arachidonic acid decreased at 5 min and 3 hr after the ellagic acid injection; EPA-E had little effect on this change. EPA-E showed almost no effect on fibrinolytic activity, blood viscosity and filterability of washed red blood cells after the ellagic acid injection. (3) Moreover, EPA-E in daily administrations showed a significant preventative effect against the laurate-induced vascular lesions in rats. The efficacy of EPA-E on arterial thrombosis and vascular lesions observed in this study suggests that EPA-E is a candidate for the treatment of peripheral circulatory disturbance.
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  • Hiroyuki SONOKI, Yasumi UCHIDA, Takanobu TOMARU, Tsuneaki SUGIMOTO
    1988 Volume 91 Issue 2 Pages 91-96
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Effects of 3, 4-diaminopyridine (DAP), which decreases the membrane K conductance, on the contractions of guinea-pig tracheal smooth muscle induced by histamine and prostaglandin D2 (PGD2) were investigated. Pretreatments with 5 ×10-4 and 10-3M DAP increased the exitability of histamine-induced contraction. The increment of the excitability by DAP was not suppressed by tetrodotoxin (TTX), but by nifedipine (Nif). Pretreatment with 10-3M DAP did not affect the contraction induced by PGD2. The results suggest that DAP increases the excitability of histamine-induced contraction by activating the voltage-dependent Ca channels and that PGD2 contracts tracheal smooth muscle through a mechanism different from that of histamine.
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  • Miwa MISAWA, Saizo YANAURA, Tomokazu HOSOKAWA, Hiroyuki MIZUNO, Kazuhi ...
    1988 Volume 91 Issue 2 Pages 97-103
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The effects of flutropium bromide (Ba598Br), a new antiasthma drug possessing the quarternary ammonium structure of atropine derivatives, on mediator release from mast cells and on actions of leukotriene (LT) D4 and serotonin were investigated. Flutropium bromide (3 and 10 mg/kg, i.v.) showed an inhibitory action on the 48 hr homologous PCA in guinea pigs. Atropine showed no inhibitory effect. Flutropium bromide also inhibited the release of histamine from isolated rat mast cells stimulated by antigen, although the inhibitory action was weaker than that of disodium cromoglycate. Atropine also had no inhibitory action in this case. Flutropium bromide and atropine showed no antagonistic action against LTD4-induced contraction of isolated tracheal smooth muscle of guinea pigs. Inhalation of flutropium bromide (0.3%) also showed no antagonistic action against serotonin-induced bronchoconstriction in dogs. From the above results, it is indicated that flutropium bromide has a weak mast cell stabilizing action, but no antagonistic action against LTD4 and serotonin.
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  • Kiyoshi SAITOH, Tatsuo MANABE, Osamu IRINO
    1988 Volume 91 Issue 2 Pages 105-109
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The mode for the manifestation of the inhibitory effect of ifenprodil tartrate on platelet aggregation in vivo and ex vivo was studied in mice and men, respectively. The ifenprodil level in plasma reached the maximum in 20 min after oral administration of 30 mg ifenprodil tartrate/kg in mice, and it decreased over a 3 hr period after the administration. On the other hand, the maximal inhibitory effect was observed 60 min after the administration. Thus ifenprodil tartrate manifested its inhibitory effect on platelet aggregation only after the maximum plasma concentration of ifenprodil was reached. The same phenomenon was observed with the inhibitory effects of ifenprodil tartrate on platelet aggregation ex vivo in man. To clarify the reason for the delay in the manifestation of the inhibitory effects of ifenprodil, the ifenprodil contents in mouse platelets after the oral administration of the drug was measured. The pattern of change in the ifenprodil contents in platelets was found to resemble closely the pattern of the change in its inhibitory effects, suggesting that the manifestation of the inhibitory effects on platelet aggregation by oral administration of ifenprodil tartrate was directly related to the ifenprodil contents in platelets rather than the ifenprodil level in plasma.
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  • Hisashi KURIBARA, Sakutaro TADOKORO
    1988 Volume 91 Issue 2 Pages 111-119
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Behavioral effects of buflomedil, 4-(1-pyrrolidinyl)-1-(2, 4, 6-trimethoxyphenyl)-1-butanone hydrochloride, a vasoactive drug, were investigated by means of ambulatory activity and the discrete lever-press and shuttle avoidance responses in mice. Single administration of buflomedil (1, 3, 10, 30 and 100 mg/kg, p.o.) produced no marked change in the ambulatory activity and the discrete lever-press avoidance response. However, the ambulation-increasing effect of methamphetamine (2 mg/kg, s.c.) was suppressed by 30 mg/kg of buflomedil. The avoidance-suppressing effect of chlorpromazine (1 mg/kg, s.c.) was enhanced by 3 ?? 100 mg/kg of buflomedil, but the avoidance-suppressing effect of physostigmine (0.2 mg/kg, s.c.) was not modified by the same doses of buflomedil. On the other hand, the acquisition of the discrete shuttle avoidance response was not affected markedly by buflomedil (3, 10 and 30 mg/kg, p.o.) when the drug was administered immediately before the start of training. The present results suggest that buflomedil shows a central suppressing effect, probably through catecholaminergic neuronal systems, and that the effect is detectable only by the combined administration with typical psychoactive drugs.
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