Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 70, Issue 6
Displaying 1-12 of 12 articles from this issue
  • Masaru KUNITOMO, Toshiyuki NAGAKURA
    1974 Volume 70 Issue 6 Pages 735-746
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    It has been demonstrated in our laboratory that 1-[2-(dodecyloxy)ethyl]pyrrolidine hydrochloride (DEP) has a strong wormcidal action on Ascaris lumbricoides suum. In this study, effects of DEP on the carbohydrate metabolism in Ascaris muscle were investigated with the following results. DEP was found to have a slight inhibitory effect on the glycolytic enzyme activities in Ascaris muscle cytoplasm. In Ascaris muscle mitochondria, DEP significantly inhibited the succinate formation from malate, but it did not affect the fumarase and malic enzyme activities. The succinate cytochrome c reductase, succinate methylene blue reductase and malate cytochrome c reductase activities in Ascaris muscle mitochondria were also strongly inhibited by DEP. The degree of inhibition of these enzyme activities by DEP was quite similar over a range of the DEP concentrations between 0.3 and 10 × 10-5 g/ml. DEP greatly stimulated the reoxidation of cytochrome c reduced by succinate or malate in Ascaris muscle mitochondria. These results suggest that DEP specifically inhibits enzyme systems associated with mitochondrial membrane such as succinate dehydrogenase and NADH dehydrogenase in Ascaris muscle.
    Download PDF (4833K)
  • Kumiko MASAMOTO, Yuichiro ARAI, Yukio KUROIWA, Yasuhiko KUROSAWA, Haji ...
    1974 Volume 70 Issue 6 Pages 747-756
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of ethyl and butyl alcohol on five different MAO preparations in beef liver, such as homogenate, mitochondria, soluble and 2 different solubilized preparations, were investigated, and morphological changes of rat liver mitochondria by these agents were observed under electron microscope. Ethyl alcohol increased MAO activities in all five preparations at concentrations of 0.1% to 1%. However, MAO activity was inhibited at concentrations of more than 10%. Butyl alcohol inhibited mitochondrial MAO activity in rat liver at concentrations of 0.01% to 10%, while ethyl alcohol at the same concentration increased the activity. Butyl alcohol was added to the mitochondrial preparation in final concentrations of 0.01% to 10% after which the mixtures were centrifuged at 8, 500×g for 10 min. The precipitate was fixed with OSO4 and morphological changes were observed under electron microscope. Swollen mitochondria, lack of matrix and cristae were observed at concentrations of 0.1% to 1%. At a concentration of 10%, structure of the mitochondria disappeared. Ethyl alcohol at a concentration of 0.1% resulted in a decrease of electron density in matrix and swelling of cristae while at a concentration of 10%, desquamation of outer membrane and at 40% agglutination and vacuolization of matrix were observed.
    Download PDF (5838K)
  • Tetsuhiro KUBOTA, Tadaharu SASAKI, Masayuki NAKAZAWA
    1974 Volume 70 Issue 6 Pages 757-766
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    In anesthetized dogs, a single injection (i.v.) of doxapram (0.1 ?? 3 mg/kg) caused a transient rise of systemic blood pressure and increased the rate and volume of respiration, followed by an increase in PaO2 and decrease in PaCO2. When doxapram was infused at a constant rate (0.05 and 0.2mg/kg/min), the same phenomena were observed. These effects of doxapram were compared with those of dimorpholamine anddimefline. The rise of systemic blood pressure induced by doxapram was inhibited by adrenergic blocking agents, ganglionic blocking agents and reserpinization. The same phenomenon induced by doxapram was observed to decrease in spinal dogs. On the other hand, it was potentiated by cocaine. In the heart lung preparation, perfusion pressure, apex contractility, right atrial pressure, cardiac output and heart rate were unaffected by doxapram in any dose applied. Injection of doxapram into the femoral artery increased the femoral blood flow, indicating a decrease in peripheral vessel resistance.
    Download PDF (3866K)
  • Shigenori WATANABE, Hiromu KAWASAKI, Showa UEKI
    1974 Volume 70 Issue 6 Pages 767-784
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Electroencephalographic (EEG) effects of maprotiline, a new antidepressant, were compared with those of imipramine and amitriptyline in conscious rabbits with chronically implanted electrodes. All drugs were dissolved in isotonic saline and administered i.v.. Maprotiline (5, 10 mg/kg) induced a drowsy EEG pattern, i.e. high voltage slow waves in the cortex and desynchronization of hippocampal theta waves. Imipramine (1, 2, 5 mg/kg) and amitriptyline (1, 2, 5 mg/kg) also elicited similar EEG effects but were more potent than maprotiline in this respect. Maprotiline (5, 10 mg/kg) failed to suppress the EEG arousal responses induced not only by auditory stimulation but also by electrical stimulation of the centromedian thalamus, posterior hypothalamus and mesencephalic reticular formation, whereas imipramine (2, 5 mg/kg) and amitriptyline (1, 2, 5 mg/kg) inhibited these responses. The EEG arousal response induced by i.v. injection of physostigmine 0.1 mg/kg showed little change after maprotiline (5, 10 mg/kg), while the response was significantly suppressed by imipramine (2, 5 mg/kg) and amitriptyline (1, 2 mg/kg). Maprotiline (5, 10 mg/kg) had no effect on the recruiting response induced by electrical stimulation (8 Hz) of the centromedian thalamus and enhanced the limbic after-discharges elicited by hippocampal or amygdaloid stimulation, while imipramine (2, 5 mg/kg) and amitriptyline (1, 2, 5 mg/kg) caused an initial depression followed by sustained enhancement of these after-discharges. These results demonstrate maprotiline to be an anti-depressant of a new type which has no effect on the ascending reticular activating system and a slight central anticholinergic action.
    Download PDF (9506K)
  • Hideo MIZUSAWA, Hiroshi FUJIWARA
    1974 Volume 70 Issue 6 Pages 785-799
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    In helically-cut strips of isolated rabbit aorta, the contractile response to noradrenaline was competitively antagonized by ifenprodil in concentrations ranging from 10-8 to 2 × 10-5 M ; the pA2 value of this agent (7.45) was approx. the same as that of phentolamine (7.64). The addition of ifenprodil at 10-6 to 10-4 M attenuated the contractile response to histamine and serotonin and at 2 × 10-5 to 5 × 10-4 M also attenuated the response to Ba++ and K+. Contractions induced by angiotensin II were inhibited only at the highest concentration used (5 × 10-4M). In rabbit aorta contracted with Ba++, ifenprodil (5 × 10-6 to 10-4 M) caused a dose-related relaxation ; the potency was approx. 1/6.7 that of papaverine. In helically-cut strips of isolated canine cerebral, superior mesenteric, renal and femoral arteries contracted with K+, ifenprodil (5 × 10-6 to 5 × 10-4M) also caused a dosedependent relaxation. The relaxation observed in cerebral and renal arterial strips was greater than that in mesenteric and femoral arteries. The rate and contractility of isolated rabbit atria decreased with application of ifenprodil in a dose-dependent manner. The addition of ifenprodil produced an increase in the contractility of isolated rabbit ileum and uterus and a relaxation of isolated guinea pig tracheal strips. It may be concluded that ifenprodil possesses an alpha adrenergic blocking property in association with a nonspecific, papaverine-like vasodilating action, which appears to be greater in cerebral and renal arteries than in the other arteries studied.
    Download PDF (6884K)
  • Hajime FUJIMURA, Kaito TSURUMI, Yasuzo HIRAMATSU, Koichiro GO, Kazumas ...
    1974 Volume 70 Issue 6 Pages 801-818
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    In a previous paper, ketoprofen, 2-(3-benzoylphenyl)-prop ionic acid, was found to have similarly potent anti-inflammatory and analgesic activities to that of indomethacin. In this paper, the general pharmacological actions of ketoprofen were tested in order to investigate whether or not. the compound had other valuable actions, side effects and indirect anti-inflammatory actions. Ketoprofen was proven to exert slightly sedative and depressive effects on the central nervous system, but the activity was less than that of indomethacin and did not appear at anti-inflammatory doses. Though it decreased urine volume and electrolytes in urine, this property was found not only in ketoprofen, but also in all other acidic nonsteroid anti-inflammatory agents. Ketoprofen showed no other significant pharmacological activities e.g. on the respiratory and cardiovascular system, on the autonomic nervous system, on the smooth and skeletal muscles, on the sugar leveland coagulation in blood and on the local irritation. Moreover, the responses of catecholamine, acetylcholine, histamine, bradykinin, 5-HT and BaCl2 were not affected by ketoprofen. Therefore, it was found to have no antagonistic properties regarding transmitters or chemical mediators. From the above results, it may be considered that ketoprofen does not indirectly exert anti-inflammatory action due to other pharmacological actions, but rather directly potent anti-inflammatory action and has fewer side effects.
    Download PDF (10238K)
  • Kenji TSUZUKI
    1974 Volume 70 Issue 6 Pages 819-830
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of isoproterenol in vivo and in vitro were investigated in order to determine the correlation between release of liver potassium and glycogenolytic action induced by epinephrine. Results are as follows. Intravenous administration of isoproterenol in pentobarbital anesthetized dogs caused a transient rise of serum potassium followed by an after-fall like epinephrine. Hyperkalemic effect of isoproterenol, like cyclic AMP, was about 1/4 as potent as that of epinephrine in so far as these agents revealed almost equivalent responses on hyperglycemia and liver phosphorylase activation. Increase in liver cyclic AMP level induced by isoproterenol was similar to that of epinephrine. Hyperkalemic effect of epinephrine was inhibited by both α and β-adrenergic blocking agents, dihydroergotamine and dichloroisoproterenol, whereas that of isoproterenol was inhibited by only the β-blocking agent. Dog liver adenyl cyclase activity was lowered by potassium in vitro, while increase in the enzyme activity induced by isoproterenol was not altered by a simultaneous addition of potassium.
    Download PDF (5657K)
  • Shunkichi TAMURA, Hiroshi MAEHASHI, Shigeru NOZAKI, Reiko MIZUKAMI
    1974 Volume 70 Issue 6 Pages 831-836
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    When As2O3 was added to the diets, the content of As2O3 in organs decreased according to the amount of milk as the constituent. In the previous study, it was found that this factor was related to the casein. The present study was carried out to ascertain whether polypeptone and polytamine show the same effect or not. Male albino rats of Wistar strain (Tamura, 1950) by closed colony, weighing about 100 g were used. The experimental groups were fed a cereal diet with 20% of polypeptone or polytamine and As2O3 with a 650 ppm. The control group was fed cereal and As2O3 with a 650 ppm. There was no statistically significant difference concerning gain in body weight among the groups. There was no difference in the arsenic content in feces. The arsenic content in the urine and kidney of polypeptone + As group was higher than the other groups, the arsenic content in the brain of polypeptone + As group was lower than the others and the arsenic content in the liver and spleen of polytamine + As group was higher than the others.
    Download PDF (2640K)
  • Shunkichi TAMURA, Shigeru NOZAKI, Hiroshi MAEHASHI, Izumi TANAKA
    1974 Volume 70 Issue 6 Pages 837-841
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    These experiments were carried out to ascertain the effects of the accumulation of AS2O3 in urine, feces, brain, liver, kidney, lung and spleen of rats that had been fed cereal food containing 650 ppm of AS2O3 to which had also been added 1%o methionine, taurine and cysteine. The quantity of As2O3 in urine and feces of rats in the methionine, taurine and cysteine groups was statistically no less than that of As control group. The quantity of As2O3 in brain, liver, kidney, lung and spleen of rats in the methionine, taurine, cysteine groups was also statistically no less than that of the As control group.
    Download PDF (1906K)
  • Shunkichi TAMURA, Reiko MIZUKAMI, Izumi TANAKA
    1974 Volume 70 Issue 6 Pages 843-847
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    When arsenite was added to the diets, the content of arsenite in organs decreased according to the amount of milk as the constituent. In a previous study (S. Nozaki : Folia Pharmacol. japon 68, 857, (1972)), it was found that this factor was related to the casein. The present study was carried out to ascertain the same factor in lactoalbumin and eggalbumin. Male albino rats of Wistar strain (Tamura 1950) by closed colony, weighing about 100 g, were used. The experimental groups were fed cereal diets to which lactoalbumin or eggalbumin had been added in the rate of 20%. Cereal only was given to the control group. Arsenite in dose of 650 ppm was added to every diet and each group was fed for 35 days. There was no statistically significant difference concerning gain in body weight among the groups. There was no difference in the arsenic content in urine, feces, brain, kidney and spleen as determined by the method of atomic absorption spectrophotometry. The arsenic content in the whole liver of the lactoalbumin group was higher than in the control group, but in the organs calculated per g the quantity was the same in all groups. The content of arsenite in the whole lung was much the same as that in the control group, but in the organs per g there was little, and no statistically significant difference.
    Download PDF (2039K)
  • Mariko NAGANUMA, Koji FUKUSHIMA, Shigeshi TOYOSHIMA
    1974 Volume 70 Issue 6 Pages 849-861
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Four novel antitumor amino acid related compounds were labeled with 14C and the distribution was studied in mice. *A-91 was excreted into the bile, and a high level of radioactivity in the blood was maintained throughout the 24 hr of experiment. A high radio-activity was seen in the liver, lung, kidney, urinary bladder, and tumor. *A-145 was rapidly distributed to each tissue from the blood, especially to the pancreas, salivary glands, gastrointestinal tract, tumor, and other growing and secreting tissue. *A-192 was excreted into the bile and a high level of radioactivity was seen in the blood. A high radioactivity was detected in the liver, lung, kidney, uterus, ovary, and tumor, followed by a reduction paralleled with a concentration in the blood. *A-192 was rapidly excreted into the urine and very little radioactivity was observed in almost all organs and tissues, except for the central nervous system. *Cyclophosphamide was also rapidly excreted into the urine and bile, but only slight activity was observed in most organs. *Tryptophan, *isoleucine, *valinethese three had the same distribution patterns, and were incorporated into the growing and secreting tissues, pancreas, salivary glands, gastrointestinal tract, tumor, etc.
    Download PDF (8754K)
  • Yasuo ISHII, Yuichi FUJII
    1974 Volume 70 Issue 6 Pages 863-869
    Published: 1974
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    The inhibitory action of several mild anti-ulcer agents on gastric ulcer in the pylorus ligated rats (Shay rats) and availability of this method were investigated. Food deprivation and ligation times were set at 48 hr and 18 hr, respectively. Drugs were administered orally twice a day during food deprivation and intraduodenally immediately after pyloric ligation. Glutamine, FM 100 (a fraction from licorice root extract) and glucose showed no inhibitory action on ulceration. Methylmethionine sulfonium chloride (MMSCl, 1 or 2 g/kg×5) and chlorophyll (1 g/kg×5) inhibited ulceration dose-dependently though the doses were extremely high compared with clinical ones. A single administration of MMSC1 or chlorophyll immediately after pyloric ligation showed no inhibitory action. Synergistic action between repeated administration of MMSCl and a single administration of atropine, antacids, amylopectin sulfate or FM100 was observed when using this method. Shay rats may therefore be useful for evalution of mild anti-ulcer agents as well as anticholinergic agents, pepsin inhibitors and antacids.
    Download PDF (3513K)
feedback
Top