Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 49, Issue 2
Displaying 1-13 of 13 articles from this issue
  • (Report 1)
    Jun SATO
    1953 Volume 49 Issue 2 Pages 41-48,en9
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    Since Prof. Hara has reported in 1923 that cerium possesed an anticoagulant action, it has been widely recognized that, when rare-earth metals (used in a narrow sense of the term) was given intravenously, it exerted an anticoagulant action for certain period. This time, the author has made a study on the nature of this action on rabbits on the basis of Wohlisch's enzyme theory using the chlorides of La, Ce, Pr and Nd, and found that it was due to the decrease of prothrombin and thrombin contents in blood, which had no relation to the amount of calcium, anti-thrombin and fibrinogen. It possessed also an antagonistic action against the organ preparations of hemostatics and vitamin K which were without any connection with calcium. It had no synergistic action on Heparin, but on Dicumarol. From these facts it can be concluded that the nature of this action resembles to that of Dicumarol.
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  • (Report 2)
    Jun SATO
    1953 Volume 49 Issue 2 Pages 49-54,en9
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    The amount of the chlorides of La, Ce, Pr and Nd required for the moderate anticoagulant action on rabbits was 20 mg/kg. In each experiment with a single injection there was no change noticeable as to the action on the whole body and/or on the heart and liver functions, while the transitory decrease of blood pressure was often observed. The repeated admidistration of the same dose over three days caused, however, the liver disorder and finally killed the rabbit. The histological investigations revealed the intense damages concentrated around Vena centralis media with hemorrhages and the necrosis as well as the fatty infiltrations near the Glisson's capsula, which coincided with that in the case of Dicumarol. From the results of Report 1 and 2 it appears that the rare-earth metal salts are of value clinically as to the prophylaxis and theraby for the embolism and thrombosis, but there is some different points from Dicumarol, in which the former acts immediately after its administration and its action disappears within a shorter time than the latter.
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  • Nobuhide FUJITAKE
    1953 Volume 49 Issue 2 Pages 55-68,en9
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    In previous report M. Kobayashi has shown that the double-peaked time-temperature curve induced by the single injection of typhoid vaccine had been changed into a single-peaked one after repeated injections of the same pyrogen (see this Folia vol. 47, Breviaria nos. 10 and 11, 1951). The analogous facts were also proved in the case of the other pyrogens, e. g., starch, distilled water contaminated with air-born bacteria, coli vaccine and yeast extract, when applied the reduced amount of their injection. doses and also when injected repeatedly these pyrogens after heating, filtering and centrifuging. Such deformations of the fever curves are thought as concerned with the tolerance acquired by the animal against each pyrogen.
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  • Mikio KUNISHI
    1953 Volume 49 Issue 2 Pages 69-75,en10
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    When the distilled water containing the culture-media centrifuges of Escherichia coli communis or Eberthella typhosa, was perfused through the liver excised from a rabbit which had acquired tolerance by the daily intravenous injection of the same pyrogen for 10 days, ther occurred the early induced single-peaked time-temperature curve when tested with another intact rabbit which has received the perfusate injection, while in the case of the same perfusion experiment through the liver of the normal rabbit the delayed single-peaked curve was induced by the coli culture-media and the double-peaked one by the Eberthellan culture-media. It is suggested that there exists two kinds of factor in each pyrogen, the one provoking the early induced single-peaked curve and the other the delayed single-peaked, and the latter f actor would be easily destroyed and/or converted readily into the former factor during the perfusion through the liver. Again, vitamin C was found effective in converting the fever curve, into the early started single-peaked form.
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  • Yoshitaka HASHIMOTO
    1953 Volume 49 Issue 2 Pages 76-83,en10
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    In order to make the mechanism of santonin action clear the author has carried out the experiments. Result : (1) Santonin has little effect on Ascaris suillus kept in Bunge's solution. It makes never the survival time of ascaris shorter than that of the intact one. (2) Calomel, phenolphthalein and bitter salt has also little effect on ascaris. But, if given with santonin, they shorten slightly the survival time and inhibit its movement. (3) Santonin from Artemisia monogyna, when given with hydrogen sulfide, shows the paralytic action on ascaris, which is due to the : change of optical rotatory activity induced thereby.Even in this case the survival time is not shortened. (4) The solution, in which santonin and hydrogen sulfide are mixed together, exerts a remarkable more toxic action on ascaris than in the case of hydrogen sulfide alone. The analogous facts are obtainable by the combination of sodium santoninate, allantolactone and hydrogen sulfide. From the above-mentioned results it may be said that, though ascaris dwells usually in the human intestine and possesses some resistance to hydrogen sulfide, it would be paralysed or killed when deprived of his resistance under the influence of santonin.
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  • Teruo OMIYA, Nobuhide FUJITAKE
    1953 Volume 49 Issue 2 Pages 84-88,en11
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    The toxicology and curarimimetic properties of 27 aromatic glucosides were studied in mice and compared with Myanesin, each of which, however, has been proved inferior to the latter.
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  • Report II. Protection of the cholinesterase activity from cholinesterase inhibitors by.anti-cholinergic drugs
    Hiroshi TAKAGI
    1953 Volume 49 Issue 2 Pages 89-95,en11
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    The relation between the anti-cholinergic drugs and brain cholinesterase (ChE) activity was studied in vitro as well as in vivo, in which ChE activity was determined by titration after Hall & Lucas' method. Result : Atropine sulphate, choiced as one of the anticholinergics, does not promote the ChE activity by itself, nevertheless, it is recognizable that the ChE activity is protected from the inhibitory action of DFP, eserine, and prostigmine after atropine (10-3-10-4 : mol) either in vitro or in vivo, while atropine protects the ChE activity from the inhibitory action of DFP after DFP. Analogous protections are also proved in vitro in each case of the following anti-cholinergics : hyoscyamine, eumydrine, homatropine, scopolamine, mydriatine, trasentine, ephedrine, banthine, parpon, parpon methobromide, benadryl, and 3015 R.P., especially being remarkably observed by the administration of quaternary ammonium salt : eumydrine, banthine, and parpon methobromide. The other drugs tested, such as cocaine, tropacocaine, benzoylcholine, urethane, and pilocarpine, exert no protecting ability for the ChE activity from DFP. From the results obtained it is concluded that (1) anti-cholinergic drugs possesses more or less some protecting ability for the ChE activity and (2) such an ability plays an important role in the antagonism between ChE inhibitors and anti-cholinergics.
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  • Masaichi YAMAMOTO
    1953 Volume 49 Issue 2 Pages 96-111,en11
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    The author has come to the following conclusion from the observations of time-concentration curves after subcutaneous injections of active principles of digitalis purpurea in the aqueous solution, as the dose of 1/40 (cc) body weight of Rana nigromaculata at the room temperature of 25°C. (1) The variations of the potency of leaves, dried either with sunlight or with infrared ray, were almost the same to each other. (2) The method of extraction of digitalis powder from leaves dried was proved more excellent than that from leaves without any treatment. (3) There were far less amount of glycosides contained in flowers than iu leaves. (4) In comparison of the amount of active principles of digitalis dried the newer leaves were the richest in amount, according to the length of the preservation period. (5) The difference in activity between the same species of digitalis ranged in one to four, according to thier cultivating location. (6) The method, in which the active principles have been extracted from the leaves in the cold infusion with methanol at first and then with ethanol as the first step of purification, seemed as the most excellent. (7) The principles extracted from leaves with ethyl acetate exerted a rapid effect, which appeared to contain genins as a main constituent. (8) The principles with a slow effect, contained in the aqueous solution of the extract, was strongly destroyed by acid, and all of the active principles were deprived of their effectiveness by alkali. (9) The active principles with rapid effect existing in the leafpowder or dried extracts were more labil than that with slow effect under the 'humidity in room and by the sunlight, but when kept with the leafpowder it was comparatively stable. (10) The aqueous solution of extracts prepared by methanol, was hardly changed in its effect, even if it was heated up to 95°C for half an hour. (11) Butoben and 1 per cent of the aqueous solution of glucose were of use to making glycosides stable, while glycerol and alcohol were little of use, and propylene glycol was rather harmful against the digitalis action. (12) Most of the commercial preparations of digitalis contained chiefly the active principles with rapid effect and their potency inclined to be overestimated. (13) When the feature of ventricular arrest of frog's heart were taken into consideration, digitoxin was proved as the cardiotonic with the most slow effect and k-strophanthin was more slower than the purpurea glycosides in effect. (14) The ratio of toxic dose to the effective dose was smaller in k-strophanthin than in digitoxin, where the cardiotonic effect of digitoxin and raw extract of digitalis appeared earlier than k-strophanthin.
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  • (1) Pharmacological properties of 3-(2'-methylphenoxy) -propane-1, 2-diol (Myanesin) and 3-(2'-methoxyphenoxy) -propane-1, 2-diol
    Teruo OMIYA
    1953 Volume 49 Issue 2 Pages 112-118,en12
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    The muscle-relaxing potency and anticonvulsant activity against the convulsions induced by strychnine, picrotoxin and metrazol were conparatively studied with 3- (2'-methylphenoxy) -propane-1, 2-dial (Myanesin) and 3- (2'-methoxyphenoxy) -propane-1, 2diol (Hustosil) in white mice. Result : Against strychnine revealed Myanesin the most powerful anticonvulsant activity, while, Hustosil did against metrazol convulsion. As to the anti. convulsant activity against picrotoxin both of these drugs was relatively weak and just resembled in its degree each other.
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  • (2) Pharmacological properties of phenyl-glucosides
    Teruo OMIYA
    1953 Volume 49 Issue 2 Pages 119-123,en13
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    The muscle-relaxing and anticonvulsant properties of ο-tolyl-α-glucoside (1), ο-tolyl-β-glucoside (2), guaiacol-α-glucoside (3) and guaiacol-β-glucoside (4) have been comparatively studied with the same method as in the previous report (see No. 13 of this Breviaria). Result : All of these compounds possessed no anticonvulsant effect on the covulsions induced by strychnine, picrotoxin and metrazol, except that (1) and (3) revealed only a weaker antagonistic effect against the metrazol action than Myanesin or Hustosil.
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  • III. Combination of 4-n-octyl-6-chlororesorcinol and 4-n-octylresorcinol
    Hidemasa YAMASAKI, Chuzaburo MANNAMI, Tateo TAKAOKA
    1953 Volume 49 Issue 2 Pages 124-132,en13
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    On the combination of 4-n-octyl-6-chlororesorcinol (O.C.R.) and 4-n-octylresorcinol (O.R.), marked potentiation was observed as to the ascaricidal power in vitro (1 : 1000) as well as to the clinical anthelmintic efficacy. The most efficient ratio of the mixture was 70 parts of O.C.R. to 30 parts of O.R. (equivalent to O.C.R. ca. 2mol : O.R. ca. 1 mol.), and its efficacy was obviously more excellent than hexylresorcinol. As to the oral toxicity to mice and the irritant action to the mucous membrane (on the conjunctiva of rabbits and human tongues), this mixture lay between O.R.and O.C.R., and was far weaker than hexylresorcinol. A 0.2 g per kg dose was almost harmless to the dog's gastric mucosa. Possible relationship between the potentiation of the ascaricidal property and some physical changes observed such as a lowering of interfacial tension of solution and a fall of melting point of the mixtures was discussed.
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  • Hidemasa YAMASAKI, Chuzaburo MANNAMI, Tateo TAKAOKA
    1953 Volume 49 Issue 2 Pages 133-137,en13
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
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    Two samples obtained by distillation of the chlorinated product of 4-n-octylresorcinol (O. R.) under the higher temperature with lower reduced pressure than is ordinarily used were both proved to be superior in the anthelmintic efficacy against ascaris in man, than pure 4-n-ecty1-6-chlororesorcinol (O.C.R.). These samples were (1) lower in melting point, (2) more distinctly colored by the diazo-reaction, (3) stronger in interfacial activity of the solution, (4) more efficacious in ascaricidal action in vitro, (5) slightly more toxic and irritant and (6) contained less chlorine than pure crystal of O.C.R.. If we assume that all this chlorine depends upon O.C.R., then these samples must contain 23.8 and 27% impurities which have no chlorine respectively. Mixtures of O.C.R. and O.R. have excellent anthelmintic efficacy, when percentage of the latter lies between 20 and 30 (refer to preceding report), besides having biological and physico-chemical properties which are almost similar, in both quality and quantity, to the samples above mentioned. Moreover, a fairly large amount of O.R. together with traces of resorcinol and 6-chlororesorcinol besides O.C.R. was identified in these samples by a paper chromatographic method, and it was proved that these impurities could be produced by thermal decomposition of O.C.R.. Occasional differences in efficacy of O.C.R. preparations in manufactural lots may be explained in most part to be caused by the concomitant of O.R..
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  • Kikuji TOKITA, Sbige IWASAKI, Fusae YUI
    1953 Volume 49 Issue 2 Pages 138-142,en14
    Published: May 20, 1953
    Released on J-STAGE: September 07, 2011
    JOURNAL FREE ACCESS
    The frog's lethal doses in the four-hour-method and the doses to open the mouth or to cause vomiting in frogs were given with the digitalis preparations as in the table below. It has been assumed from these results that digicorin, digoxin and digitalis leaves were more rapidly detoxicated than the others. The opening motion of mouth began within several minutes after aglycones injection, while it required more than thirty minutes with the other preparations. The maximal patterns of this motion were reached within one or two hours after the administration, whereby it was even seen a few of frogs drawing their stomachs out of their mouths. The frogs, decerebrated or centrally anesthetized, opened their mouths by the digitalis adminstration, while the frogs, middle-brain or medulla removed, spinal cord destructed or anesthetized with phenobarbital, showed no reaction as such. The frogs, cardiac nerves of which had been cut, opened their mouths by the intravenous injection of digitalis preparations. The hepatectomized or gastroectomized frogs opened their mouths. From the results it is concluded that the digitalis preparations caused vomiting under the influence from the middle-brain reflex pathway, but not from the reflexes passing from the heart, liver or stomach.
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