Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 90, Issue 3
Displaying 1-7 of 7 articles from this issue
  • Johji YAMAHARA, Shuji MIKI, Hisashi MATSUDA, Goro KOBAYASHI, Hajime FU ...
    1987 Volume 90 Issue 3 Pages 133-140
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    We have previously reported on the Ca2+-blocking activity and active constituents of natural products. In the course of screening, UNCARIAE RAMULUS ET UNCUS, a chinese herbal medicine, was found to possess such activity. In this paper, we attempted to characterize its active constituent which plays an important role in Ca2+-blocking activity. Its active principles were identified to be oxyindole-type alkaloids, rhynchophylline, corynoxeine, isorhynchophylline and isocorynoxeine, that showed inhibitory effects, similar to that of verapamil, on contractile response to high concentration of potassium ion (rats), CaCl2 (rats), norepinephrine in normal and Ca2+-free medium (rats and rabbits) and 45Ca2+-uptake (rats) in thoracic aorta with an activity two orders of magnitude less than the activity of verapamil.
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  • Shigeru ISHIGURO, Akira NISIO, Noboru MIYAO, Yoshio MORIKAWA, Kazu TAK ...
    1987 Volume 90 Issue 3 Pages 141-146
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    When young Wistar rats (body wt. 50 g) were maintained on a magnesium-deficient diet (0.001% Mg) for eight days, the splenic weight and histamine content increased about 2-fold and 30-fold, respectively, compared with those of the control rats. There was no significant difference in the number of splenic mast cells between the magnesium-deficient and control rats. More neutrophilic, eosinophilic and basophilic granular cells were found in the spleen cells isolated from the magnesium-deficient rats than in those from the control rats. Of the isolated cells from magnesium-deficient rats, 7.6% were basophilic granular cells; however, no basophilic granular cells were observed in the spleen cells isolated from the control rats. In the cytochemical study, the yellowish fluorochrome formed by the interaction of o-phthalaldehyde and histamine was found in basophilic granular cells. These results suggest that the increase in the histamine content of the spleen of magnesium-deficient rats is related to the increased number of basophilic granular cells.
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  • Kazuo IMAEDA, Keiko OHSAWA, Takaho WATANABE
    1987 Volume 90 Issue 3 Pages 147-153
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The optimum analytical conditions for studying the composition of skin surface lipid were examined by high-performance liquid chromatography equipped with a photo-diode array detector. Optimum conditions were as follows: ULTRON N-C18 (150 × 4.6 mm) as stationary phase, acetonitrile / tetrahydrofuran / water (55/35/10, V/V) as eluent at the flow rate of 1.0 ml/min, and column temperature of 40°C. The peaks were detected by monitoring the absorbance at 210 nm. Effect of sex-hormone on composition of skin surface lipids was examined. Gonadectomized Sprague-Dawley rats were injected with either testosterone (50 mg/kg, s.c.) or estradiol (5 mg/kg, s.c.) for 12 days. Amount of crude lipid from the skin surface was decreased at 8 days after castration; estradiol dosing to castrated rats also decreased the amount. The other hand, in ovariectomized rats, testosterone injection increased skin surface lipids. It is recognized that sex-hormone dosing after gonadectomy changes the percentage composition of squalene and cholesterol in male rats, but does not charge them in females.
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  • Comparison of sleep-inducing activities between young and elderly rhesus monkeys
    Ken-ichi YAMAMOTO, Yukio NAITO, Tohru SAWADA
    1987 Volume 90 Issue 3 Pages 155-162
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The sleep-inducing activities of 450191-S (rilmazafone hydrochloride) were compared among two groups of elderly and one group of young rhesus monkeys, and the relationship between blood levels of five active metabolites of 450191-S and sleep-inducing activities was also examined. Oral administration of 450191-S, 1 mg/kg, caused the quick appearance of slow wave deep sleep (SWDS) and its stable continuity in elderly monkeys, and no significant differences in various sleep parameters were observed among the two groups of eight elderly monkeys. An increase of SWDS was always accompanied by a high blood level of active metabolite M-2. On the other hand, in the young rhesus monkey group, the amount of SWDS and its mean continuity were significantly less, and differences were evident in sleep parameters obtained from a nocturnal 14 hr observation. In conclusion, the difference of sleep-inducing activities between elderly and young monkeys seem to be caused by a difference in the blood level of active metabolites of 450191-S, particularly M-2.
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  • Katsuhiko FUKUTAKE
    1987 Volume 90 Issue 3 Pages 163-169
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The inhibiting action in vitro of urinastatin on blood coagulation was studied for the purpose of therapeutic application against thrombotic disorders, and the following results were obtained: 1) Partial thromboplastin time of normal human plasma was prolonged dose-dependently by the addition of urinastatin to the reaction mixture, but prothrombin time was little inhibited by the addition of urinastatin. Thrombin time was also prolonged with urinastatin dose-dependently. 2) Using chromogenic synthetic peptide substrates, the amydolytic activities of XIIa, plasma kallikrein and Xa activated with RVV were inhibited by the addition of urinastatin to the reaction mixtures. 3) Activated partial thromboplastin time of normal plasma was prolonged by the addition of urinastatin or heparin, and simultaneous application of both urinastatin and heparin to the reaction mixture resulted in an additional inhibitory effect on APTT. Therefore, it was assumed that the different molecular structures of the clotting factors were concerned with the inhibitory actions of urinastatin and antithrombin III. Furthermore, urinastatin was indicated to have an important role in antithrombotic remedy, since it has no inhibitory action against protein C. 4) In the comparison with purified human plasmin and plasma plasmin activated with streptokinase, the strong inhibitory action of urinastatin on purified plasmin was demonstrated, but the inhibitory action of urinastatin was decreased markedly in plasma. Therefore, it is suggested that plasma may contain an inhibitory factor against the action of urinastatin.
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  • Kiyoshi OHSHIMA, Keiko SHIMIZU, Akira AKIMOTO, Takeshi TSUDA, Nagashig ...
    1987 Volume 90 Issue 3 Pages 171-175
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Effect of OU-1308 (17s, 20-dimethyl-6-oxo-prostaglandin E1 methyl ester) on uterine motility in anesthetized rats and monkeys was examined by means of the balloon catheter or openend catheter method and compared with that of PGF. OU-1308 and PGF exhibited uterine contractile activity at the dose of 30μg/kg, i.v., on day 8 of pregnancy and 10 μg/kg, i.v., on day 20 of pregnancy in rats. In monkeys on day 50 ?? 120 of pregnancy, both compounds enhanced uterine motility at 10, ug/kg, i.v. Intragastric administration of OU-1308 at 500 μg/kg, however, was without effect in monkeys. These results indicate that when administered intravenously, OU-1308 was as potent as PGF in terms of uterine contractile activity in pregnant rats and monkeys.
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  • Masahiko OKIYAMA, Koichi UENO, Shigeru OHMORI, Takashi IGARASHI, Haruo ...
    1987 Volume 90 Issue 3 Pages 177-186
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    In this report, we studied drug interaction between oxazepam and imipramine in rats. Oxazepam (20 mg/kg) and imipramine (20 or 50 mg/kg) were administrated orally. The oxazepam concentration in plasma, brain and liver were measured by the method of HPLC. The concomitant use of imipramine induced extension of the elimination half life (T1/2β) and an increase of the area under the concentration time-curve (AUC) on the plasma concentration of oxazepam. With the concomitant use of imipramine, the AUC of oxazepam brain concentration increased approximately 1.42 to 1.56 in contradistinction to oxazepam alone. The anti-pentylenetetrazol effect of oxazepam at 1 hr after administration was increased by the concomitant use of imipramine, but there were no combination effects at 4 hr. The motor incoordination effect of oxazepam and diazepam was measured by the rotarod method. Oxazepam has little effect on the motor incoordination as compared with diazepam. The plasma protein binding of oxazepam was not changed by the combined use of imipramine both in vitro and in vivo. The pharmacodynamic effects of oxazepam were increased by the concomitant use of imipramine, and these effects were in reasonably good agreement with the change in brain concentration of oxazepam.
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