Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 83, Issue 1
Displaying 1-8 of 8 articles from this issue
  • Jun SUZUKI, Masayasu KIMURA
    1984 Volume 83 Issue 1 Pages 1-10
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    The selective sensitivities to the blended Chinese traditional medicines (Kampo Hozai) applied for diabetes mellitus were pharmacologically studied utilizing the diabetic models: genetically diabetic KK-CAy mice and alloxan diabetic mice. The hypoglycemic response to sulfonylurea (tolbutamide) was observed in the KK-CAy mice as well as that to metformin, giving evidence which supported the difference of diabetic features between KK-CAy mice and alloxan diabetic mice. The hypoglycemic potencies of the blended medicines were determined in alloxan diabetics: Chikuyosekkoto>Byakkoka-Ninjinto≈Bakumondoto >> Hachimigan≈Ninjinto>Goreisan. A similar order of potency was shown in the fasted KK-CAy mice. In the nonfasted KK-CAy mice, Hachimigan selectively had the more marked hypoglycemic effect. In conclusion, it is compatible that the effects of Kampo Hozai may be classified into plural types of action mechanism by utilizing etiologically different diabetic models.
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  • Hiroshi MAEKAWA, Atsushi SEKIYA, Hiroko NOMURA, Junnosuke YAMAMOTO
    1984 Volume 83 Issue 1 Pages 11-15
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    Several investigators have comfirmed that β-adrenergic blocking agents produced a sustained pressor action in anesthetized rats. In this experiment, rat hindquarters were perfused with the rat's own blood under a constant perfusion rate. The effect of propranolol administered intraarterially to the hindquarters was studied. Propranolol (0.001 ?? 0.1 mg/ml, 5 μl intraarterial injection) produced a sustained rise in the perfusion pressure dose-dependently. In contrast, propranolol did not produce any sustained rise in the perfusion pressure of guinea pigs and rabbits. These results support that the β-adrenoceptive vasodilation in skeletal muscle is stronger in rats than in guinea pigs and rabbits.
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  • Masaru MINAMI, Machiko SANO, Hiroko TOGASHI, Tohru ENDO, Iwao SAITO, A ...
    1984 Volume 83 Issue 1 Pages 17-31
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    Rat and human plasma catecholamines were measured simultaneously by HPLC-THI, HPLC-ECD and REA, and the three methods were compared. An attempt was also made to determine the factors affecting the estimated value of plasma catecholamine concentration. Our study showed that: 1) Sensitivity and reproducibility to norepinephrine and epinephrine were identical in all three methods. 2) One advantage of the REA method is that comparatively smaller sample volumes are required to produce similar results. Plasma dopamine concentration in peripheral blood samples was determined by the HPLC-ECD rather than the HPLC-THI method. 3) Withdrawal of 5 ml of blood produced a significant increase in norepinephrine, epinephrine and dopamine in rat plasma. The catecholamine concentration in these cases was determined by the REA method. 4) Plasma norepinephrine concentration did not increase with age in Wistar Kyoto rats. However, plasma norepinephrine concentration increased significantly with age in stroke-prone spontaneously hypertensive rats (SHRSP). Plasma norepinephrine concentration in male SHRSP was greater than that in female SHRSP. SHRSP-plasma norepinephrine concentrations rose in parallel to increases in blood pressure. The plasma norepinephrine concentration in SHRSP with cerebral hemorrhage rose significantly as compared with the plasma norepinephrine levels in SHRSP without cerebral bleeding. Because each method of determination of plasma catecholamine concentration has both merits and demerits, selection should be determined by sample size and amount of catecholamines in the plasma samples. Factors affecting the estimated value of plasma catecholamine concentration should be taken into consideration.
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  • Masato MIZOBUCHI, Nobuo MATSUOKA, Yasushi SAITO, Sho YOSHIDA, Akira KU ...
    1984 Volume 83 Issue 1 Pages 33-37
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    The effects of mazindol which is known as a anorexigenic agent on the free fatty acid metabolism in the brain were studied. One-half mg of mazindol was orally administered to rats weighing 500 g for 5 days. Body weight was reduced by 10%, compared to the control. Serum levels of free fatty acid, triglyceride, total cholesterol and phospholipid were decreased. The effect of mazindol on the incorporation of [ 1-14C] palmitic acid into various lipids in the brain were studied. When mazindol (5 mg) was administered one hr before injection of [1-14C] palmitic acid to the internal carotid artery of rats ad libitum, incorporation of [1-14C] palmitic acid into free fatty acids in the cerebrum and diencephalon was lower than that of the control, but incorporation into phospholipid and triglyceride were higher than that of the control. When mazindol was injected into fasting rats, incorporation into free fatty acid in cerebrum and diencephalon was increased compared with the control, and the incorporations into phospholipid and triglyceride were decreased.
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  • Kohji YOSHIMURA, Masahito HORIUCHI, Yuzuru INOUE, Ken-ichi YAMAMOTO
    1984 Volume 83 Issue 1 Pages 39-67
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    The present study examined comparative self-administration of some typical CNS-affecting drugs with a new sleepinducer, 450191-S, in rats. Most animals self-administered both methamphetamine and cocaine in an extremely stable and invariable fashion with cycles of alternating responding and non-responding periods during the day and at night. Response frequency increased in proportion to a fixed-ratio value. An initial increase in response rate followed by cessation of the responding was observed during extinction. Sixty-five percent of the rats tested selfadministered morphine in a relatively variable and less stable fashion. Total daily morphine intake was directly related to the unit dose. Eighty-three percent of the rats self-administered pentazocine. Fifty and sixty-four percent of the rats maintained self-administration of phenobarbital and diazepam, respectively, with higher intake at night than during the day. Responding persisted at a low rate for several days during extinction. Abrupt withdrawal of 450191-S caused the same slight weight loss and moderate decrease in food intake as those seen with diazepam and nitrazepam, and cross-physical dependence between 450191-S and diazepam was found. Selfadministration of 450191-S at 0.5-2.5 mg/kg/infusion was observed with 2 out of 11 rats, which was much less than that found with diazepam. These results suggest that 450191-S possesses little, if any, drug dependence liability of the tranquilizer type.
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  • Endoscopical evaluation of healing processes of acetic acid ulcer in rats (2): Healing, recurrence and relapse of ulcer
    Kazunaga FUKAWA, Osamu KAWANO, Noriyuki MISAKI, Masayuki UCHIDA, Osamu ...
    1984 Volume 83 Issue 1 Pages 69-77
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    The progress of acetic acid-induced gastric ulcers in rats were sequentially observed with an endoscope for 365 days, and the influences of the ulcer-induced site, age and sex on the healing, recurrence and relapse of these ulcers were investigated. 1) Submucosal injections of 20% acetic acid at the region between the fundus and the pylorus on the anterior wall of the stomach (site A) in 7 weeks old male rats produced active round-shaped ulcers with blood coagulation and debris on the 3rd day after ulcer induction. The ulcers diminished in size with the progress of time (10 ?? 50 days), and 50% of the ulcerated rats healed with convergences of mucosal folds (35 ?? 154 days). On and after the 50th day, some diminished or healed ulcers showed signs of relapse (37% of used rats) or recurrence (40% of healed rats, 21% of used rats), with the cumulative relapse and recurrence percentage (CR%) reaching 59% on the 365th day. 2) Ulcers in the glandular portion on the greater curvature (site B) healed significantly faster than those in site A. All of the ulcers in site B healed within 133 days and did not recur or relapse. 3) The cumulative healing percentage (CH%) and the CR% of the ulcers in site A in 25 weeks old male rats were 33% and 67%, respectively, and those of the ulcers in site A in 7 weeks old female rats were 60% and 60%, respectively. From the above results, the healing, the recurrence and the relapse of ulcers induced by acetic acid were found to be affected by age, sex and especially by the ulcer-induced site.
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  • Junichi HASEGAWA, Masakatsu NOZAKI, Hajime FUJIMURA
    1984 Volume 83 Issue 1 Pages 79-83
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    In the presence of various drugs, the concentration of free bilirubin which was released from the first binding site of bilirubin in serum albumin was evaluated, using a sensitive method based on static fluorescence quenching of dansyl serum albumin. Bilirubin bound to human serum albumin more strongly than to bovine serum albumin. Non-steroidal anti-inflammatory drugs, fenamates and allylphenyl propionic acids, affected the bilirubin-serum albumin interaction. Flufenamic acid and ketoprofen released bilirubin from human serum albumin. The bilirubin bound to the serum albumin was not influenced by the presence of indomethacin, but clidanac strongly dissociated bilirubin from the bilirubin-serum albumin complex. Sulfa-drugs, antibiotics, steroidal agents, warfarine, tolubutamide and phenytoin showed no significant effects on the bilirubin-serum albumin interaction. The fluorescence quenching method may be useful to evaluate the interaction of drug-bilirubin-serum albumin.
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  • Junichi HASEGAWA, Tamaki NAKAYAMA, Masakatsu NOZAKI, Hajime FUJIMURA
    1984 Volume 83 Issue 1 Pages 85-91
    Published: 1984
    Released on J-STAGE: March 07, 2007
    JOURNAL FREE ACCESS
    The serum albumin-interaction of suprofen (SPF), a novel anti-inflammatory drug, was compared with those of indomethacin (IM) and ketoprofen (KTP). The binding constants of these drugs were determined with difference absorption spectra based on the binding to bovine serum albumin (BSA). The constants for SPF and IM were nearly equal, and the value for KTP was smaller than those of the other drugs. The magnitude of the inhibitory effect on heat denaturation of BSA reflected the difference in these binding constants. In the presence of these drugs, the tryptophan fluorescence in BSA was quenched (IM, SPF and KTP, in this order). The metachromagy based on the binding of an azodye, HABA, to BSA was potentiated by IM or SPF. Phenylbutazone suppressed the absorption of the metachromagy. SPF displaced only the binding of the fluorescent Site II probe, dansylproline, to human serum albumin (HSA), and both the bindings of dansylproline and dansylamide (Site I probe) to HSA were inhibited by KTP or IM. KTP released bilirubin from BSA and HSA, but SPF and IM did not show any effects on the bilirubin-serum albumin binding. These results all support that there is considerable interaction between SPF and serum albumin and that the mode of the interaction differs from those of KTP and phenylbutazone.
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