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Volume 75, Issue 3
Displaying 1-7 of 7 articles from this issue
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Shinya SHINOZAWA, Yasunori ARAKI1979 Volume 75 Issue 3 Pages 207-214
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSComparative studies were done on the actions of hydrophobic drugs (cepharanthine, papaverine and cholesterol) regarding chemical modifications of Ehrlich ascites tumor cell membranes. Changes in membrane potential monitored by using cyanine dye (diS-C3-(5)) were induced by cepharanthine and papaverine, but not by cholesterol. Increase in membrane permeability of K+ ion induced with lysolecithin was strongly inhibited in the order of papaverine, cholesterol and cepharanthine. Oxygen uptake by the cells was also strongly inhibited by papaverine, but the inhibitory effect by cepharanthine was little and cholesterol had no effect. Membrane fluidity was decreased in the order of cholesterol, cepharanthine and papaverine. From these results, it was suggested that papaverine maintained the compartmentation of K+ ion and membrane fluidity by regulating the intracellular mitochondrial metabolism or by inhibiting the membrane bound ATPase nucleotidase activity. The membrane stabilizing effect of cepharanthine and cholesterol probably was due to decrease in the membrane fluidity because of the hydrophobic association to the lipid bilayer of the cell membranes.View full abstractDownload PDF (10581K) -
Motoo KUKI1979 Volume 75 Issue 3 Pages 215-225
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSMorphine dependence was induced by ten daily administrations of morphine with gradually increasing dosage (40 ?? 160 mg/kg/day s.c.) to male Sprague-Dawley rats, the dosage being divided in 2/day for the first 8 days and 4/day for the last 2 days. Diurnal variation in body weight in morphine dependent rats was the same as in naive rats. Although body temperature in the naive rats showed a diurnal variation with the highest at 3:00 and the lowest at 15:00, in the morphine dependent rats there was no distinct variation. Plasma corticosterone level (PC) in naive rats showed diurnal variation with the peak at 21:00 and the trough at 9:00. PC in morphine dependent rats showed the same diurnal variation as did the naive rats, while such disappeared following pentobarbital anesthesia (80 mg/kg i.p. for 45 min) and PC was low all during the day. The PC increase following formalin administration to morphine dependent rats was higher than in naive rats. 0.1 mg/kg s.c. of dexamethasone completely inhibited PC increase after formalin in naive rats, but the dexamethasone inhibition in morphine dependent rats was not complete even with a larger dose, i.e. 10 mg/kg s.c.. Diurnal variations and other differences were not detected in the adrenal response to ACTH (in vivo, in vitro) between naive and morphine dependent rats. These results suggest that HPA function takes part in the development of morphine dependence.View full abstractDownload PDF (12199K) -
Chihiro ITO, Kazuo YAMAGUCHI, Yasunori SHIBUTANI, Kazuo SUZUKI, Yoshio ...1979 Volume 75 Issue 3 Pages 227-237
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSAnti-inflammatory actions of proteases, bromelain (BR), trypsin (TR) and their mixed preparation (KT) were studied mainly in rabbits using various experimental test methods. Inhibitory action of edema formation induced by carrageenin was observed to be dose dependent with oral administrations of KT. This inhibitory action of KT was more remarkable than actions of BR and TR, suggesting a possible synergism between the latter two. Such action was also observed with non-steroidal anti-rheumatic drugs, phenylbutazone (PB), indomethacin and acetylsalicylic acid. Oral administration of KT exerted definite inhibition or a tendency toward inhibition against paw edema induced by dextran, histamine or egg albumin or skin edema induced by anti-rabbit serum and thermal stimulation. Furthermore, inhibition of vascular permeability increase induced by histamine and bradykinin as well as a tendency toward inhibition against protein exudation in CMC-pouch method were observed. On the other hand, contrary to PB, potent inhibitory action was not manifested in the persistent proliferative inflammation models, the granuloma formation induced formalin soaked filter paper and cotton pellet and the mustard edema. Therefore, it can be deduced that the inhibitory action of KT against edema formation may be dependent mainly on the inhibitory action of vascular permeability increase and the anti-inflammatory action may be specific for acute exudative inflammation.View full abstractDownload PDF (11799K) -
Shigehiko NARUMI, Yasuo NAGAI, Yuji NAGAWA1979 Volume 75 Issue 3 Pages 239-250
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe enhancing effect of TRH on dopamine(DA) release from rat striatal slices was investigated in relation to Ca2+ and cholinergic mechanisms. TRH(10-5 ?? 10-3M) facilitated concentration dependently the uptake of 14C-DA by rat striatal slices, while methamphetamine (10-6 ?? 10-4M) exhibited a considerable inhibitory effect. TRH (10-7 ?? 10-3M) alone did not increase the DA release into the incubation medium, but it clearly enhanced the DA release in the concomitant presence of desipramine (5×10-5M). In the superfusion study, TRH (10-5 ?? 10-3M), methamphetamine (10-6 ?? 10-4M) and KCl (2.5 ?? 5.0×10-2M) enhanced the DA release into the perfusion fluid. The DA releasing effect of TRH was completely blocked by cholinergic blockers (scopolamine, hexamethonium and hemicholinium), Ca2+ chelator(EGTA), Ca2+ antagonist (CoCl2) and Ca2+ influx blocker(D-600) or by the removal of Ca2+ from the medium. The methamphetamine-enhanced DA release, however, was not modified by the above treatments except for a partial decline produced by EGTA coupled with the removal of Ca2+. TRH(10-4M) also facilitated the uptake of 3H-norepinephrine (NE) by rat cerebral cortex slices, but methamphetamine (10-6 ?? 10-4M) exhibited a considerable inhibitory effect. In the superfusion study, TRH (10-5 ?? 10-4M) and methamphetamine (10-7 ?? 10-4M) enhanced the NE release into the perfusion fluid. Therefore, it can be concluded that TRH facilitated the DA release from rat striatal slices by mediating through a cholinergic mechanism and by enhancing the influx of Ca2+.View full abstractDownload PDF (14730K) -
Naohisa FUKUDA, Masaomi MIYAMOTO, Shigehiko NARUMI, Yasuo NAGAI, Takas ...1979 Volume 75 Issue 3 Pages 251-270
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEnhancement by TRH of the dopamine(DA) agonist-induced circling behavior and effect of TRH itself on circling behavior were investigated. TRH(2.5-20 mg/kg, i.p.) remarkably enhanced the circling behavior induced by apomorphine or L-DOPA in the mice lesioned unilaterally in the caudate nucleus by injection of 6-hydroxydopamine (6-OHDA) or by tissue aspiration with subsequent reserpinization. TRH also enhanced the apomorphine-induced stereotypy in reserpinized normal mice. The above TRH-enhancing action of the circling behavior was potentiated, suppressed or unaffected by α-methyl-para-tyrosine (α-MT) or GABAergic drugs. In the 6-OHDA lesioned mice treated with TRH, the cyclic AMP formation by DA or apomorphine was clearly enhanced in the striatal slices taken from the lesioned side but not from the intact side. In the rats lesioned unilaterally in the nigrostriatal DA pathway by 6-OHDA, high doses of TRH injected i.p. (100 mg/kg) or into the non-lesioned caudate nucleus (50 μg) produced circling toward the lesioned side, which was suppressed by haloperidol or α-MT. TRH(10-5 ?? 10-3M) increased the 14C-DA release from the rat striatal slices in vitro. These results suggest that TRH at low doses facilitates the DA postsynaptic transmission in association with an increase of DA-stimulated cyclic AMP formation in the striatum under supersensitization of the DA receptors, and also at high doses enhances the DA neuronal activity by increasing the DA release from the striatal nerve terminals.View full abstractDownload PDF (25685K) -
Part I Effects on the CNSKoroku HASHIMOTO, Shigeyuki SHINTANI, Shuji YAMASHITA, Seiso TEI, Masa ...1979 Volume 75 Issue 3 Pages 271-289
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffects of procaterol (PRO) on the CNS were investigated in comparison with those of salbutamol (SAL) and isoproterenol (ISO). PRO, 15 to 50 mg/kg given subcutaneously suppressed spontaneous movement in mice, rats and rabbits and with a large dose, 1000 mg/kg, the animals became quiet and immobile. In dogs, PRO produced similar symptoms and in addition, there was nausea and vomiting. The animals recovered within 3 ?? 8 hours. ID50's in depressing spontaneous movement were 20.2 and 245 mg/kg for PRO, 51.1 and 133 mg/kg for SAL and 2.37 and 143 mg/kg for ISO, respectively, both by the subcutaneous and oral routes of administration. Methamphetamine induced increase in motility and fighting behavior was also suppressed by PRO when similar doses were given. PRO had no effect on coordinating movement, halothane anesthesia, drug and electric stimulation induced convulsions and body temperature, and there was no muscle relaxant action. However, PRO in large doses prolonged sleeping time with hexobarbital. The analgesic effect of PRO was not observed with Haffner's and Landall Selitto's methods but acetic acid induced writhing was suppressed by PRO. PRO had little effect on spontaneous EEGs either cortical or from deep structures, and EEG arousal responses. The effects of PRO on the CNS were slight and nonspecific, and similar to those of SAL and ISO.View full abstractDownload PDF (22457K) -
(3). General pharmacological actionsMakoto SATO, Yasuhiro ISHIZUKA, Hisayuki TANIZAWA, Tamotsu FUKUDA, Tom ...1979 Volume 75 Issue 3 Pages 291-307
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSGeneral pharmacological actions of M73101, a new non-steroidal analgesic anti-inflammatory drug were investigated in mice, rats, guinea pigs, rabbits, cats and dogs. Intravenous administration of M73101 produced a slight transient fall in blood pressure, an increase in heart rate and a respiratory stimulation, but no remarkable change in the electrocardiogram. The contraction induced by epinephrine in the isolated ear vessels of rabbits relaxed by M73101. In the isolated trachea of guinea pigs, M73101 relaxed the contraction induced by histamine. Furthermore, M73101 inhibited the bronchoconstriction by histamine but not by bradykinin in guinea pigs. These properties of M73101 on the tracheal smooth muscle were similar to those seen with aminopyrine but different from those seen with aspirin which inhibited only the contraction by bradykinin in vivo, suggesting that M73101 is a compcund with properties similar to basic non-steroidal anti-inflammatory drugs. M73101 inhibited the intestinal propulsion in mice and also the gastrointestinal movement in rats and dogs. Moreover, M73101 showed a spasmolytic activity on the isolated ileum of guinea pigs, but such was not due to any specific antagonistic action on the chemical mediators. On the other hand, M73101 had no effect on the isolated uterus and vas deferens of rats. M73101, unlike aminopyrine and phenylbutazone, slightly increased urine volume and electrolytes excretion in rats, indicating that this compound probably does not produce edema. M73101 showed no significant pharmacological activities on the blood sugar level, blood coagulation, platelet aggregation, methemoglobin formation and local irritation.View full abstractDownload PDF (19596K)
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