Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 72, Issue 8
Displaying 1-10 of 10 articles from this issue
  • Hitoo NISHINO
    1976 Volume 72 Issue 8 Pages 941-954
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Unit activity of lateral hypothalamic area (LHA) and ventromedian nuclei (VMN) was recorded in urethane anesthetized male rats. A 5 to 10 sec, a 3 to 5 min and a circadian rhythmicity were observed. In about 15% of all neurons, spontaneous activity of LHA and VMN showed reciprocal relationships. Subthreshold stimuli applied at a slow rate in the septum and the suprachiasmatic nuclei (SCN) suppressed the rhythms without changing firing rates. On the other hand stimulation of the optic nerve at a rate of 5 to 10/sec in creased firing rates in one third of neurons of SCN. Iontophoretically applied acetylcholine increased 80% of tested neurons of SCN, whereas norepinephrine, dopamine and 5HT inhibited 64%, 60% and 75% of SCN neurons, respectively. These inhibitions were much stronger in neurons, the activity of which was increased by optic nerve stimulation. Stimulation of the SCN inhibited the tonic activity in cervical sympathetic nerves. These data suggest that SCN plays a significant role in controlling the rhythmic activity of LHA, VMN and the pineal gland. Dopamine and 5HT may be involved in regulation of the firings of SCN neurons.
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  • Tsutomu SHIMADA, Yoshiki NUNOURA, Eiryo KITANAKA, Shozo IWAGAMI, Yasuk ...
    1976 Volume 72 Issue 8 Pages 955-967
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Kanechlor (KC)-300, 400, 500, and 600 consisting of polychlorinated biphenyls (PCB) containing 43, 48, 55, and 61 io chlorine respectively, were administered in a single dose of 100 mg/kg to mice and rats. The effect of PCB was investigated by determining pentobarbital sleeping time, liver microsomal hemoprotein contents, PCB level and gaschromatography (GC) pattern in tissue. Pentobarbital sleeping time was prolonged 2 to 4 times longer than that of control level after 3 to 4 hr of KC treatment in both ICR and ddN strain mice and KC-300 was the most effective. Forty-eight hr after treatment, however, this sleeping time was half that of the control. Sleeping time in ICR strain mice returned to control level 8 days after the treatment with KC-300 and KC-500, but the decrease in sleeping time continued in ddN mice. Conversely, the prolongation of sleeping time in rats was only 20% the control level at 3 hr after KC-300 treatment, but the shortening of sleeping time was more marked than in mice. Both the prolongation of sleeping time in mice treated with KC-300 and the shortening of sleeping time in rats treated with KC-500 were more rapidly effected when an oral dose rather than when a intraperitoneal one was given. Induction of liver microsomal cytochrome P-450 level was maximum in rats treated with KC-600 and increase of hemoprotein level and shortening of sleeping time were proportional to the chlorine content of PCB. The CO-difference spectrum of microsomes from rats treated with KC had an absorbance maximum at 448 nm. Direct relationship between storage of PCB in adipose tissue and the induced effect by KC has also been demonstrated in rats. PCB level in the liver of rats was higher for about 8 hr after KC-500 treatment given orally and was lower than the PCB level in adipose tissue after 8 hr. The GC-pattern of PCB stored in tissues was different from that of standard KC, indicating that all components were not metabolized at the same rate and that the components of the KC with the longer retention time were metabolized to a lesser degree than those with the shorter retention time.
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  • Mutsuko CHIBA, Norihisa MIYAKE, Terumi TAMADA, Yasuo FUJIMOTO, Susumu ...
    1976 Volume 72 Issue 8 Pages 969-978
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    CD-3400 developed by Nippon Chemiphar Co. Ltd., is a new antihypertensive agent belonging to the class of rauwolfia alkaloids. Influence of the agent on gastric mucosa, healing process of acetic acid-induced gastric ulcer and gastric juice in rats was investigated and compared with effects of reserpine and rescinnamine. CD-3400-induced gastric lesions were fewer in number than those produced with reserpine and rescinnamine in fasted rats. After a three day treatment of CD-3400 to fed rats, however, there were few gastric lesions, while reserpine and rescinnamine-induced gastric lesions were aggravated to a greater extent than when a single administration was given to fasted rats. Influence of CD-3400, reserpine and rescinnamine on the healing process of acetic acid-induced ulcer was insignificant, but treatment with high doses of reserpine and rescinnamine resulted in death. Pretreatment with CD-3400 and reserpine produced a decrease in gastric acid and K+, and an increase in Na+. Repeated administration of reserpine for 5 days resulted in a decrease of both gastric volume and acid, while such was not seen with CD-3400. Treatment with anticholinergic agents such as atropine sulfate and atropine methylbromide inhibited CD-3400 and reserpine-induced gastric lesions. From these results, it would appear that cholinergic factors play a role in the pathogenesis of CD-3400-induced gastric lesions, as is the case with reserpine, and that the responses of these lesions to reserpine and CD-3400 correlate with changes of ionic fluxes in gastric juice.
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  • Kazuo HASEGAWA
    1976 Volume 72 Issue 8 Pages 979-984
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    A bipolar electrode was stereotaxically implanted in or near the medial forebrain bundle at the level of the posterior lateral hypothalamus of male albino Wistar-Imamichi rats. The relationship between the adrenergic system and the lateral hypothalamic self-stimulation(SS) behavior was investigated by intraventricular injection (by the use of the modelled hypodermic needle) of catecholamines. l-Epinephrine(Ep), l-norepinephrine (NE) facilitated the SS behavior dose-dependently. On the other hand, l-isoproterenol and dopamine revealed no detectable effects. Phentolamine inhibited the SS behavior, but propranolol had no marked effects. Facilitation by NE for the SS behavior was not induced when the current was cut off at the time of the injection of NE. These results suggest the following: a) the adrenergic or the noradrenergic system in the brain may play a more important role in the positive reinforcement of the lateral hypothalamic SS behavior than does the dopaminergic system. b) The action of Ep or NE may be facilitated through α-receptors rather than through β-receptors. c) Facilitation by NE for the lateral hypothalamic SS behavior may not be due to the non-specific facilitation of lever pressing, but rather may be related to intracranial stimulation.
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  • Kazuo HASEGAWA
    1976 Volume 72 Issue 8 Pages 985-990
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    A bipolar electrode was stereotaxically implanted in the substantia nigra of male albino Wistar-Imamichi rats. Effects of l-norepinephrine(NE), dopamine(DA) and γ-aminobutyric acid (GABA), injected into the lateral ventricle, on the substantia nigral self-stimulation(SS) behavior, and the effects of α- and β-adrenergic receptor antagonists on the facilitation induced by NE were investigated. NE but not DA facilitated the SS behavior and GAGA showed no constant effects on the behavior. Facilitation by NE of SS behavior was inhibited by phentolamine, but not by propranolol. These results suggest that the noradrenergic system in the brain may play a more significant role in the positive reinforcement of the substantia nigral SS behavior than does the dopaminergic or GABA-ergic system, and that the action of NE may be facilitated through α-receptors rather than through β-receptors.
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  • Norihisa MIYAKE, Yoshio HASEGAWA, Terumi TAMADA, Yasuo FUJIMOTO
    1976 Volume 72 Issue 8 Pages 991-1000
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of methyl O-(4-hydroxy-3-methoxycinnamoyl)reserpate (CD-3400), a new antihypertensive agent, on the peripheral nervous system in mice, rats and guinea pigs were investigated and compared with effects of reserpine and rescinnamine. Oral administration of CD-3400 in doses from 40 to 320 mg/kg revealed a miotic action and such was weaker than that seen with reserpine and rescinnamine. The intestinal propulsion in mice was accelerated by pretreatment with reserpine, but no so with CD-3400. In isolated guinea pig vas deferens, CD-3400 at a concentration of 1 × 10-5M inhibited on norepinephrine-induced contraction non-competitively. However, in isolated rat vas deferens pretreated with CD-3400 (1 mg/kg, i.p.) for 5 days, norepinephrine-induced contraction was potentiated and this effect was weaker than that seen with reserpine and rescinnamine. In isolated rat vas deferens pretreated with CD-3400 for 1, 2 and 5 days, the contraction induced by tyramine (3 × 10-5M) was significantly inhibited. The effect was qualitively similar to those of reserpine and rescinnamine. The intravenous administration of these three rauwolfia alkaloids in doses of 1, 2 and 4 mg/kg had no effect on the spontaneous movement of rat uterus. In isolated rat uterus pretreated with CD-3400, no significant effect was observed on oxytocin and isoproterenol-induced responses. The peripheral actions of CD-3400 are attributed to a deterioration in the function of the sympathetic nerve resulting in depletion of catecholamine stores. Effects of CD-3400 were slightly weaker than those of reserpine and rescinnamine.
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  • Kimikazu ITAYA, Jiosuke KIYONAGA, Muneyoshi ISHIKAWA
    1976 Volume 72 Issue 8 Pages 1001-1011
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Investigations were performed in male Wistar rats to determine the effects of γ-oryzanol on circadian rhythm of stress ulcer and on various kinds of experimental ulcers, and the modification of antiulcerogenic action of this drug when combined with the inhibitors or precursors of amine metabolism. Circadian rhythms were observed in stress ulceration with a peak at 2 : 00 p.m. and a reduction at 8 : 00 p.m. The inhibitory action of γ-oryzanol was significant when stress was loaded for 6 hr from 2 : 00 a.m., 5 : 00 a.m., 11 : 00 a.m. or 2:00 p.m. An 8-day treatment with γ-oryzanol, 100 mg/kg, s.c., showed a significant inhibition of fasting ulcer, while the 5-day pretreatment exerted slight effects on ulcers by pylorus-ligation or stress-atropine. A 10-day treatment with the same dose of γ-orzanol in acetic acid ulcers lowered the serum level of gastrin. Treatment with reserpine, α-MT or PCPA prior to stress loading abolished the anti-ulcer effect of γ-oryzanol, 100 mg/kg, s.c. for 5 days in stress ulcer. Treatment with L-DOPA or 5-HTP revealed a tendency toward restoration of the anti-ulcer effect of γ-oryzanol. It is suggested that the monoaminergic neuron system is involved in the anti-ulcer action of γ-oryzanol.
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  • Jun NAITO, Tetsuro KUGA
    1976 Volume 72 Issue 8 Pages 1013-1023
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of perimetazine on the motility of the isolated smooth muscle of guinea pig (ileum, taenia coli, uterus, vas deferens and trachea) and the ileum of rabbit were studied. The results obtained are as follows: Perimetazine showed a specific antihistamine, antiadrenaline and antiserotonin action. Moreover, antiacetylcholine and anti-BaCl2 actions were observed with high doses of perimetazine as well as chlorpromazine and such actions were attributed to the nonspecific direct action on the smooth muscle. Both the spontaneous movement and the tonus of guinea pig taenia coli were also inhibited by a high concentration of perimetazine. The spontaneous membrane action potentials of the taenia coli recorded by the use of the sucrose-gap method were inhibited by a high concentration of perimetazine both in frequency and in amplitude with relaxation of the tonus. The action potentials were abolished however and change in the resting membrane level was not clearly observed.
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  • Shozo MASUMOTO, Chiharu MASUDA
    1976 Volume 72 Issue 8 Pages 1025-1031
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Inhibitory effects cf 2-(2-fluoro-4-biphenylyl) propionic acid (Flurbiprofen, FP-70) on prostaglandin (PG) synthesis and PG activity were investigated both in vivo and in vitro. FP-70 at 0.64 μM showed 50% inhibitory effect on PG synthesis from arachidonic acid in cell-free homogenate of guinea pig lung. PGE2 and PGF in the sample of lung homogenate incubated with arachidonic acid were separated by thin-layer chromatography in solvent AI system. FP-70 inhibited strongly both synthesis of PGE2 and PGF, at 3 μM, but inhibited more extensively the synthesis of PGE2 than that of PGF at 0.3 μM. FP-70 at 1 mg/kg, p.o. inhibited mostly arachidonic acid potentiation of carrageenin-induced edema in the rat paw, but did not inhibit PGE2 potentiation of carrageenin-induced edema. FP-70 also did not inhibit the contraction of rat stomach strip induced by PGE2. From the above and previously5) reported results, FP-70 proved to inhibit PG synthesis but not PG activity. It is suggested that the potent anti-inflammatory action of FP-70 is the result of inhibition of PG synthesis.
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  • Hideaki FUKUSHIMA, Toshiharu OKA, Yukio ASAMI, Sumio KITAGAWA
    1976 Volume 72 Issue 8 Pages 1033-1044
    Published: 1976
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of ID-540, a new benzodiazepine derivative, on operant behavior were studied and compared with those of diazepam in rats for the purpose of determining the characteristics on behavioral pharmacology. Four schedules used were as follows: Fixed interval (FI-60sec) of food reinforcement and differential food reinforcement of low rate (DRL20sec) for positively reinforced behavior, Sidman-type avoidance response for negatively reinforced behavior and conflict behavior induced by simultaneously rewarding with food and punishing with electric shock. In the experiments on FI-60sec schedule, the responses at the early stage (0 ?? 30 min after administration of the drug) were increased by both ID-540 and diazepam at lower doses (0.5 ?? 4 mg/kg p.o.), but inhibited at higher doses (8 ?? 32 mg/kg p.o.). The effect of ID-540 lasted longer than that of diazepam. In the experiments on DRL20sec schedule, neither drug accelerated the responses, but decreased the lever-press response and total number of reinforcements at higher doses (4 mg/kg or more) showing the disturbance of discrimination on time. In Sidman-type avoidance responses, ID-540 did not show any inhibitory effect, thus a neuroleptic-like effect of ID-540 was not demonstrated. In experiments on FI-60sec and Sidman-type avoidance schedules, the effect of ID-540 was not changed by a consecutive administration for 10 days. Conflict behavior is considered to resemble the anxiety states in humans, and in related experiments, ID-540 increased the lever-press response which delivered a food-pellet and an electric shock simultaneously at a dose of 0.0625 mg/kg (i.p.). Change in other behavior was not observed at this dose level. Maximum effect of ID-540 was observed at a dose of 0.5 mg/kg (i.p.). Maximum effect of diazepam on conflict behavior was seen at a dose of 4 mg/kg (i.p.). The potency of ID-540 on conflict behavior was estimated to be about 8 times that of diazepam.
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