Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 70, Issue 4
Displaying 1-5 of 5 articles from this issue
  • Yasuo ISHII, Yasuhiko FURUTA, Takeshi TANAKA, Masako MINOWA
    1974 Volume 70 Issue 4 Pages 507-514
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    The inhibitory action of amylopectin sulfate (APS) on gastrointestinal proteases and experimental peptic ulcer was investigated with the following results : 1) APS inhibited pepsin, trypsin and chymotrypsin in vitro. Pepsin inhibition enhanced with the increasing concentration of APS and the maximum inhibition reached 100 %. On the other hand, the maximum inhibition of trypsin and chymotrypsin by APS was 60-70 %. 2) In a toluidine blue method at pH 3.0 and a 1 : 5 ratio of APS to protein, the affinity of APS for hemoglobin was strongest and the order of the affinity for other proteins was trypsin, chymotrypsin and pepsin. 3) In an experiment of cross electrophoresis of APS with protein, APS reacted with substrates and pepsin at pH 1.8 and reacted with enzymes alone at pH 7.8. 4) From the above results, the anti-pepsin action of APS may be due to a combination of APS and both substrate and pepsin, while anti-trypsin and anti-chymotrypsin actions of APS may be due to the combination of APS with enzymes. 5) APS strongly protected against ulceration and pepsin activity of gastric juice in pylorus ligated rats but did not prevent erosions in the glandular portion of the stomach induced by pyloric ligation and cold stress in spite of potent inhibition of pepsin activity.
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  • Shoji TSUTSUMI, Yasuhiro USUI, Yoshihito MATSUMOTO
    1974 Volume 70 Issue 4 Pages 515-522
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    When milk containing or cereal containing diets with a large dose of As2O3 (650 ppm/day) were administered to rats, the influence of these different diets on a lowering of the activity of succinic acid dehydrogenase induced by As2O3 was examined in the liver, brain and kidneys. The results were that an inhibition of this enzyme activity induced by As2O3 was stronger in those rats on the cereal diet than those on the milk diet regarding the liver and brain. In the kidneys, however, the inhibition was low and of the same grade in the both groups. As inhibition of this enzyme activity did not parallel the amount of As2O3 in each organ, it appears to be specific.
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  • Hideji MORISHITA, Tatsuo FURUKAWA
    1974 Volume 70 Issue 4 Pages 523-530
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    The present study is concerned with general characteristics of strips of dog femoral artery as pharmacological test objects and with the responses of such strips to drugs. The spirally cut strips of dog femoral artery possessed a small amount of spontaneous tone and never exhibited rhythmic contractions. When strips were first attached to a lever under 4 g tension, they underwent a gradual elongation and increased in sensitivity to stimulating drugs over a period of about 1.5 to 3 hr. Once maximal sensitivity had been attained, the response to stimulating drugs usually remained constant for 7 hr. When effects of adrenergic drugs, such as noradrenaline, isoprenaline, dopamine, tyramine and ephedrine were tested, Krebs-bicarbonate solution containing NaHS03 was used in order to inhibit oxidation of amines in the solution. All drugs except isoprenaline produced contractions which were inhibited completely by phenoxybenzamine. Isoprenaline showed biphasic effects, i.e., relaxation in low concentration and contraction in high concentration. The former relaxation was inhibited by propranolol and the latter contraction by phenoxybenzamine, but acetylcholine, at any concentration, caused relaxation which was blocked by atropine. As strips of dog femoral artery respond to drugs in a manner similar to in vivo experiments, femoral arterial strips of dogs make for good pharmacological test objects.
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  • Shigenori WATANABE, Hiromu KAWASAKI, Hiroyoshi NISHI, Showa UEKI
    1974 Volume 70 Issue 4 Pages 531-542
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Electroencephalographic effects of ID-690 were investigated in unanesthetized, unrestrained rabbits with chronic electrode implants, and compared with those of diazepam. ID-690, in a does of 0.05 ?? 0.2 mg/kg i.v., revealed a drowsy pattern in spontaneous EEG, i.e. high voltage slow waves and spindle bursts increased in the neocortex and amygdaloid complex, while the hippocampal theta rhythm was desynchronized. In addition, low voltage fast waves appeared particularly in cortical EEG. This is charasteristic of benzodiazepines. The EEG arousal response to auditory stimulation was markedly depressed by ID-690. The arousal response to electric stimulation of the posterior hypothalamus was more strongly inhibited by ID-690 than that to mesencephalic reticular stimulation. The EEG effects of diazepam were qualitatively similar but less potent than those of ID-690. ID-690 and diazepam showed no effect on the photic driving response elicited by flash light in the visual cortex. The recruiting response was slightly enhanced by ID-690 and diazepam. ID-690 was much more potent than diazepam in depressing hippocampal and amygdaloid afterdischarges.
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  • Hajime FUJIMURA, Kaito TSURUMI, Yasuzo HIRAMATSU, Koichiro GO, Kazumas ...
    1974 Volume 70 Issue 4 Pages 543-569
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    The anti-inflammatory, analgesic and antipyretic properties of ketoprofen, 2-(3-benzoylphenyl)-propionic acid, were assessed by a battery of standard tests. Ketoprofen inhibited the increased vascular permeability and the acute edema induced by various phlogistic stimulations and ultraviolet erythema. The inhibitory activities were about 10 times as potent as those of phenylbutazone and the same as those of indomethacin. This agent was slightly more potent than indomethacin in inhibiting sustained paw edema induced by mustard. It was also potent in reducing granuloma formation and adjuvant arthritis without affecting the weight of the adrenals and thymus, but slightly less so than indomethacin. Ketoprofen inhibited carrageenin induced paw edema in both adrenalectomized and normal rats. It is therefore suggested that the anti-inflammatory action of ketoprofen is a direct one at inflamed sites and not one via a corticoid intermediary. On the other hand, the drug was acutely ulcerogenic in fasting rats. The activity was also the same as that of indomethacin and paralleled the anti-inflammatory activity of the latter. Utilizing the writhing and modified Haffner test in mice for analgesic appraisal, ketoprofen showed the same activity as indomethacin. When the Randall-Selittos' analgesic method was utilized in rats, a significant rise in pain threshold was obtained only at the inflamed foot and the activity was more potent than that of indomethacin. Ketoprofen showed a more potent antipyretic action than indomethacin in febrile rabbits. From the above results, ketoprofen may be classified as a potent nonsteroid anti-inflammatory agent with analgesic and antipyretic actions.
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