Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 92, Issue 1
Displaying 1-6 of 6 articles from this issue
  • Mikio NAKAZAWA, Shoichi IMAI
    1988 Volume 92 Issue 1 Pages 1-9
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The principles of nuclear magnetic resonance (NMR) spectroscopy were explained and its application to biomedical research discussed. With 31P-NMR, it is feasible to conduct a continuous, non-invasive measurement of the contents of myocardial high-energy phosphate compounds and the intracellular pH (determined by monitoring the pH dependent shift of the inorganic phosphate peak relative to that of creatine phosphate), and to correlate them with the mechanical function. The determination of the free magnesium concentration is also possible on a similar principle to that for pH determination (the shift of MgATP peaks relative to ATP is utilized in this case). It is estimated to be 0.3 mM and was found not to be changed during ischemia. Several examples of studies including our own conducted to delineate the ischemic derangements of the myocardial energy metabolism and the effects of various interventions thereupon were illustrated. Finally a brief mention was made of the saturation transfer technique. This is the only method with which one can study the kinetics of the enzyme reactions under in vivo conditions. The application of the method for analysis of the creatine kinase reaction and the ATP synthesis was demonstrated.
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  • Michio TERASAWA, Noriko TOMOMATSU, Yutaka MARUYAMA
    1988 Volume 92 Issue 1 Pages 11-16
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The anti-allergic actions of traxanox sodium pentahydrate (traxanox) were examined using experimental allergic rhinitis models. Traxanox (10 and 30 mg/kg, p.o.), tranilast (30 and 100 mg/kg, p.o.) and disodium cromoglycate (DSCG, 3 and 10 mg/kg, i.v.) dose-dependently inhibited the increase of dye leakage in rats actively sensitized with dinitrophenol-coupled ascaris extract. Traxanox was about 4 times more potent than tranilast. In this test, the inhibitory activity of traxanox (30 mg/kg, p.o.) was not affected by predosing with the same dose for 7 days. In addition, traxanox (1-10 mg/kg, i.v.) inhibited the allergically induced increase in nasal resistance of guinea pigs actively sensitized with egg albumin, while tranilast (10 mg/kg, i.v.), DSCG (100 mg/kg, i.v.) and mepyramine (1 mg/kg, i.v.) had little effect. These results suggest that traxanox may be clinically effective in treating patients with nasal allergies.
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  • Sachiko GOTOH, Kyosuke MIYAZAKI, Junichi ONAYA, Takashi SAKAMOTO, Kiyo ...
    1988 Volume 92 Issue 1 Pages 17-27
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Using the model of knee pain reaction induced by intra-articular injection of endogenous pain substances, especially bradykinin (BK) in rats, the mechanism of the analgesic effect of sodium hyaluronate (SPH) was investigated. The simultaneous administration of prostaglandin E2 with BK or hyaluronidase digestion of endogenous hyaluronic acid (HA) in our experiments brought remarkable hyperalgesia on BK-induced knee pain. These results suggest that higher sensitivity to the pain reaction is induced in a diseased joint (higher prostaglandin content, lower concentration and molecular size of HA in synovial fluid) than in a normal one. SPH definitely decreased BK-induced pain, and its analgesic effect was observed for a longer period, depending on its dose in pre-treatment and the degree of its distribution in synovial tissues. As the analgesic effect of SPH was observed in the hyaluronidase-treated joint as well, it is suggested that the increasing viscosity of synovial fluid caused by increasing HA concentration can decrease the pain even without normalizing molecular size of HA in the joint. HA oligomer and other compounds with similar viscosity or with similar polyanionic character as SPH showed no analgesic effect. From these results, it seems that the characteristic steric configurations of higher molecular HA are needed for the manifestation of the analgesic effect. SPH seems to show its analgesic effect by covering pain receptors in synovial tissues and holding endogenous pain substances in its molecule.
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  • Hideo NAKAMURA, Satoru MOTOYOSHI, Katsumi ISHII, Toshiaki KADOKAWA
    1988 Volume 92 Issue 1 Pages 29-38
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Effect of AD-1590 on allergic inflammations was investigated. AD-1590 and indomethacin at an oral dosage as high as 32 mg/kg did not show any significant inhibitory activity on rat passive cutaneous anaphylaxis, a type-I allergy, although prednisolone and cyproheptadine produced strong inhibition. Against rat adjuvant arthritis, type-III and -IV allergies, AD-1590 showed potent prophylactic (2 and 4 mg/kg/day) and therapeutic (0.4 ?? 1 mg/kg/ day) effects when given orally once a day for 3 weeks beginning from just before and for 1 week starting from 14 to 18 days after adjuvant inoculation, respectively; however, its prophylactic and therapeutic potencies were about one-fourth and one-fifth, respectively, that of indomethacin. The arthritis was strongly inhibited with prophylactic treatment of prednisolone (1 mg/kg/day) or cyproheptadine (40 mg/kg/day). On the other hand, prednisolone (ED50=0.0119 mg/ear, topical) showed strong activity in inhibiting mouse contact hypersensitivity to oxazolone (ear edema), a type-IV allergy, but cyproheptadine only had weak activity. AD-1590 (0.318 mg/ear) and indomethacin (0.699 mg/ear) produced rather strong inhibition; in particular, AD-1590 produced almost complete inhibition at high dosages, whereas most of the non-steroidal anti-inflammatory drugs (NSAID) tested showed weak inhibition or a partial inhibition of about 50% even at the highest dosage. The oral potency of AD-1590 was about 2 and 100 times those of indomethacin and ibuprofen, respectively. These results demonstrate that in allergic inflammation, the pharmacological properties of AD-1590 are somewhat different from those of other NSAID and different from those of prednisolone and cyproheptadine.
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  • Keiichiro HAGA, Kiyoshi ASANO, Kunio OSUGA, Yutaka MARUYAMA
    1988 Volume 92 Issue 1 Pages 39-47
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    In pylorus ligated rats, OPZ inhibited gastric acid secretion dose-dependently, with a potency greater than that of FMD. At the same time, OPZ increased gastric K+ secretion and inhibited pepsin and Na+ secretions at the highest dose. In Heidenhain pouch dogs, single injection of OPZ inhibited gastric acid secretion induced by histamine to a degree almost equal to that by FMD. In the case of repeated administration, anti-secretory activity of OPZ was enhanced by up to several days and then remained constant. After several days, the inhibitory activity of OPZ was more potent and longer than that of FMD, and it still had not ceased 22hr after administration. In pylorus ligated rats, OPZ prevented gastric ulceration, and the potency was greater than that of FMD. OPZ promoted healing of gastric and duodenal ulcers induced by acetic acid in rats. At the same doses, FMD failed to promote the healing of both ulcers. In water-immersion stressed rats, OPZ prevented formation of gastric erosions, with a potency greater than that of FMD. In addition, OPZ prevented formation of gastric erosions induced by ethanol in rats. These results indicate that the anti-secretory and anti-ulcer activities of OPZ are superior to those of FMD, so that OPZ should have excellent therapeutic application for peptic ulcers.
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  • Hisato KITAGAWA, Fumiyo TAKEDA, Toshihiro HAYASHI, Masayo IZUMITA, Hir ...
    1988 Volume 92 Issue 1 Pages 49-60
    Published: 1988
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The effects of oxitropium bromide (Ba 253) on respiratory, cardiovascular, digestive and urogenital systems were studied. Ba 253 increased heart rate in anesthetized cats at low doses (0.1 ?? 0.3 mg/kg, i.v.) and decreased blood pressure in dogs and cats at high dose (3 mg/kg, i.v.). Aerosol inhalation of a high concentration of Ba 253, however, did not influence the heart rate. Ba 253 enhanced the isoproterenol-induced inotropic action and vasodilation. Intestinal transport of mice were inhibited by Ba 253 (s.c.), but not inhibited by oral administration. Ba 253 (1 ?? 30 mg/kg, i.v.) enhanced the motility of rat uterus in vivo, but inhalation of the Ba 253 aerosol did not have any affect. Ba 253 had no effects on vasoconstriction, spontaneous motility of the ileum, bile secretion, urinary excretion and spontaneous motility of the urinary bladder. These results indicate that intravenous or subcutaneous administration of Ba 253 decreased blood pressure, enhanced uterus motility and inhibited intestinal transport, but the inhalation or oral administration, even at high doses, has no effects on the cardiovascular system and uterine motility.
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