The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Volume 29, Issue 3
Displaying 1-24 of 24 articles from this issue
  • Hiroshi SAITO, Moriyoshi TSUCHIYA, Shinichi NAKA, Keijiro TAKAGI
    1979 Volume 29 Issue 3 Pages 319-324
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Pole-climbing and shuttle-avoidance tests were employed to study the acquisition of conditioned avoidance response (CAR) and discrimination behaviour (DB) in male Wistar rats which had been given extracts from Panax Ginseng root intraperitoneally or orally. Neither a lipid soluble fraction (GNo. 5) nor a ginsenoside Rg fraction (GRg) produced significant changes in the acquisition of CAR. GRg given intraperitoneally produced a significant acceleration in the acquisition of DB between a 500 Hz signal sound followed by an electric shock (SD) and a 1000 Hz signal sound without a shock (SJ) in rats which had learned to avoid the shock following SD at a rate of over 95 %. Small doses of GNo. 5 produced a significant depression in the acquisition of DB.
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  • Youichi ABE, Takeshi OKAHARA, Taketoshi KISHIMOTO, Kenjiro YAMAMOTO
    1979 Volume 29 Issue 3 Pages 325-333
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    A reduction of renal arterial pressure in mongrel dogs to 70 mmHg resulted in marked increases in plasma renin activity and plasma levels of angiotensin I (AI) and angiotensin II (AII). Production of renin and AI but not AII in the kidney was observed. A reduction of renal arterial pressure also resulted in a redistribution of blood flow from the outer to inner cortex. An arterial infusion of AII (200 ng/min), however, failed to affect the intrarenal distribution of the blood flow. An intrarenal infusion of AII rather restored the normal pattern of the distribution of intrarenal blood flow altered by the pressure reduction. These results indicate that the renin-angiotensin system is probably not involved in the control of renal hemodynamics through the intrarenal formation of AII, and that the intrarenal hemodynamic changes caused by pressure reduction is due to the intrinsic difference in myogenic force in different cortical zones.
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  • Masaomi MIYAMOTO, Shigehiko NARUMI, Yasuo NAGAI, Takashi SHIMA, Yuji N ...
    1979 Volume 29 Issue 3 Pages 335-347
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    The mechanism of stimulatory action of thyrotropin-releasing hormone (TRH) on spontaneous motor activity was investigated in rats. TRH produced a significant hyperactivity with intraperitoneal administration of 20 mg/kg or bilateral injection of 10 μg into the nucleus accumbens septi (NAS). Following bilateral injection of 6-hydroxydopamine into the mesolimbic dopamine (DA) pathway, the hyperactivity induced by TRH was not altered, whereas the response to apomorphine given intraperitoneally or DA injected into the NAS was clearly enhanced. The TRH-induced hyperactivity was remarkably suppressed by α-methyltyrosine and in contrast, augmented by pargyline. Systemic injection of aminooxyacetic acid in a dose producing behavioral depression reduced markedly the TRH-induced hyperactivity. Bilateral injection of ethanolamine O-sulphate (100 μg) into the NAS produced no behavioral depression per se, but remarkably attenuated the hyperactivity response to TRH or DA (20 μg) given intraperitoneally or into the NAS. Both TRH (10-5 and 10-4 M) and methamphetamine (10-6-10-4 M) increased the spontaneous release of 14C-DA from rat NAS slices. These findings suggest that TRH induces hyperactivity by enhancing DA release from nerve terminals in the NAS without a direct stimulation of the post-synaptic DA receptors. TRH and GABA, independently or via interaction between them, may play a reciprocal regulatory role in the activity of the mesolimbic DA system.
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  • Yumiko IWAYAMA, Issei TAKAYANAGI, Yutaka KASUYA
    1979 Volume 29 Issue 3 Pages 349-356
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Phenylephrine, a selective a-adrenergic stimulant, caused a maximal relaxation of the taenia from guinea pig caecum in the concentration of 10-6 g/ml. Phenylephrine in this concentration did not influence intracellular cyclic AMP and cyclic GMP levels. Although phenylephrine abolished the spontaneous spike discharge, no change was detected in 45Ca-uptake and 45Ca-efflux on the tissue level after phenylephrine. Ca-uptake and Ca-release on the subcellular level were also not influenced by phenylephrine. In Ca free-solution phenylephrine inhibited the response to CaCl2. Phenylephrine increased 42K-efflux in the normally polarized taenia and also in the K-depolarized taenia.
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  • Ichiro YANO, Hitoo NISHINO, Tadashi MURANO
    1979 Volume 29 Issue 3 Pages 357-366
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    The effect of naloxone given at various times after morphine administration on the development of tolerance to and dependence on a single dose of morphine was studied. Naloxone antagonized the analgesic effect of morphine and the development of tolerance to and dependence on morphine, dose dependently. The time course of the development of tolerance to a single dose of morphine almost paralleled that of dependence on morphine but the time course of the disappearance of tolerance did not coincide with that of dependence. When start of the duration of action of morphine was blocked by naloxone for various time intervals, the degree of tolerance to and dependence on morphine was antagonized, time dependently. When the end of the duration of action of morphine was antagonized by naloxone for various time intervals, tolerance and dependence which developed up to that time was completely antagonized by naloxone.
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  • Yohkazu MATSUSHIMA, Munekazu GEMBA
    1979 Volume 29 Issue 3 Pages 367-374
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Correlative studies on transports of Ca2+ and Na+ and the properties of Ca2+ transport were carried out in rat kidney cortex slices. Ouabain had no effect on the Ca2+ transport but did inhibit the Na+ transport extensively. With addition of 2, 4-dinitrophenol to the incubation medium, or under the anaerobic conditions, the effluxes of Ca2+ and Na+ were inhibited while the Ca2+ influx was enhanced significantly. Sulfhydryl inhibitors such as ethacrynic acid, mersalyl and p-chloromercuribenzoic acid suppressed Ca2+ efflux and stimulated Ca2+ influx. When the slices of kidney cortex were treated with these inhibitors, there was a reduction in the content of cellular ATP. The present results suggest that Ca2+ transport may be partly independent of Na+ transport, and that Ca2+ efflux may require energy-yielding processes.
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  • Isao YAMAGUCHI, Yoshiaki AKIMOTO, Hiromichi NAKAJIMA, Akio KIYOMOTO
    1979 Volume 29 Issue 3 Pages 375-383
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Effect of diltiazem on insulin secretion was investigated in the perfused rat pancreas. Experiments were also carried out in anesthetized dogs and conscious rats with and without glucose loading. In the perfused rat pancreas, diltiazem reduced both glucose- and tolbutamide-induced insulin secretion and these effects of diltiazem were reversed with removal of the compound. Inhibition of the glucose-induced insulin secretion caused by diltiazem was counteracted by increasing the concentration of calcium ion. In experiments on intact animals, diltiazem at vasoactive doses produced no significant influence on the basal level of plasma insulin or glucose-induced insulin secretion. These data taken together with findings in previously reported work suggest that diltiazem reduces insulin secretion from pancreatic B-cells in vitro possibly by the calcium-antagonistic property, while the compound exhibits practically no inhibitory action on the insulin secretion in vivo.
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  • Hisashi KURIKI, Taketoshi SAIJO, Yoshitaka MAKI, Morio KANNO
    1979 Volume 29 Issue 3 Pages 385-397
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    A newly synthesized compound, 6-ethyl-3-(1H-tetrazol-5-yl)chromone (AA-344) given intravenously or orally inhibited considerably the 72-hr passive cutaneous anaphylaxis (72-hr PCA) induced by IgE in rats. The antiallergic action of AA-344 was neither due to the antihistamine or antiserotonin effect nor was it mediated via adrenergic mechanisms. The results obtained in a double sensitization with two IgE antibodies suggest that AA-344 may not impair antigen-antibody combination but probably prevents the release of chemical mediators including histamine. This assumption was supported by observation that AA-344 inhibited a reduction in the skin histamine content caused by the 72-hr PCA, without effect on the compound 48/80-induced histamine reduction. AA-344 also partially inhibited the IgGa-mediated 3-hr PCA in rats. These results indicate that the inhibitory action of AA-344 on the immediate hypersensitivity reactions is due to prevention of the release of chemical mediators from the mast cells, by acting on some process in sequential events leading to the mediator release following antigen-antibody combination.
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  • Toshio ISHIKAWA, Minoru YAMAMOTO
    1979 Volume 29 Issue 3 Pages 399-403
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Involvement of the cholinergic and catecholaminergic mechanisms in the caudate spindle recorded from the anterior and posterior sigmoid gyri was examined in cats. Physostigmine (0.01 to 0.1 mg/kg i.v.) abolished the appearance of the caudate spindle. These inhibitory effects were antagonized by the administration of atropine (0.25 to 1 mg/kg i.v.). The caudate spindle was inhibited by high frequency stimulation of the mesencephalic reticular formation: This inhibitory effect was antagonized by atropine. On the other hand, L-DOPA (25 to 50 mg/kg, i.v.), L-DOPA+MAO inhibitor and methamphetamine (0.5 to 5 mg/kg i.v.) did not influence the caudate spindle. These results suggest an involvement of cholinergic mechanism in depression of the caudate spindle.
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  • Junko MORI, Takeo FUKUDA
    1979 Volume 29 Issue 3 Pages 405-411
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    In anesthetized immobilized rats, pallidal unit activities were recorded extracellularly through glass microelectrodes. Spontaneous activities were converted to an interspike interval histogram and an autocorrelogram by a medical computer and a correlator. Following pentylenetetrazol injection (20 mg/kg i.v.), burst discharges increased remarkably and the bursts tended to synchronize with repetitive spikes in electrocorticogram. Following administration of liocaine (5 mg/kg i.v.) the bursts increased by pentylenetetrazol were facilitated in approximately 70% neurons, whereas pentobarbital showed obvious reduction of the bursts in 80% neurons, although both drugs reduced the firing rate. Facilitation of burst discharges was also observed with high doses of lidocaine alone. These results indicate that lidocaine, as compared with pentobarbital, may block more easily inhibitory rather than excitatory neurons.
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  • Ryoichi ISHITANI, Hisako KIN, Toyoyasu KUWAE, Kayoko MOROI, Tetsuo SAT ...
    1979 Volume 29 Issue 3 Pages 413-421
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Carboxylesterase (CEase) was solubilized from rat liver microsomes by autolysis followed by cholate treatment and then purified by the combination of ammonium sulfate fractionation, gel filtration, chromatography on DEAE Sephadex A-50 and hydroxyapatite and preparative Disc electrophoresis. The overall purification was 25-fold with a yield of 6 % of the original enzyme activity. Analytical Disc electrophoresis of the final enzyme preparation showed a single band. However, SDS polyacrylamide gel electrophoresis revealed one main band of 93 % and three other minor bands. To investigate the interaction between CEases of rat, monkey, pig and rabbit liver microsomes, rabbit antibody to the above enzyme preparation was prepared and immunological analyses, i.e., Ouchterlony's test and immunoelectrophoresis, were performed. In the comparative double diffusion test, the partial fusion of precipitation line between anti-rat CEase and the enzymes of other species was observed. In the second analysis, sharp arc precipitation lines also could be seen in all specimens and, furthermore, mobilities of each enzyme were different. These observations suggest that rat liver CEase seems to be immunologically related in part but not completely identical with the CEases of other species and the charge difference may exist in these specimens.
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  • Masao ENDOH, Tetsuo SHIMIZU
    1979 Volume 29 Issue 3 Pages 423-433
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Effects of carbachol, dbcGMP and 8-bromo-cyclic GMP on the positive inotropic actions of sympathomimetic amines and dbcAMP were studied on the canine isolated right ventricular myocardium. Carbachol alone did not substantially change the developed tension of the muscle, but did markedly shift the dose response curve for isoprenaline on the developed tension to the right and depressed the maximal response to the drug in a concentration dependent manner. The positive inotropic action of phenylephrine was affected by carbachol in the same manner as that of isoprenaline. DbcGMP in concentrations of 10-3 M and higher produced a significant increase in the developed tension. The positive inotropic action of dbcGMP was partly inhibited by a β-adrenoceptor blocking agent, pindolol. In the presence of dbcGMP, isoprenaline produced an action similar to that seen in the control experiment, but this action was not maintained on such a steady level as in the control. This rapid decline of the effect of isoprenaline in the presence of dbcGMP was prevented by adding ascorbic acid to the organ bath. The positive inotropic actions of phenylephrine and of dbcAMP were not substantially affected by dbcGMP. 8-Bromo-cyclic GMP in a concentration of 10-4 M did not change either the basal developed tension or the positive inotropic actions of noradrenaline and of isoprenaline. The present results indicate that these cyclic GMP derivatives are not able to mimic the antagonistic action of cholinergic stimulation on the positive inotropic action of adrenergic stimulation on the canine ventricular myocardium.
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  • Makoto OKA, Kiyoko YAMADA, Chiaki KAMEI, Kouichi YOSHIDA, Masanao SHIM ...
    1979 Volume 29 Issue 3 Pages 435-445
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    The interaction between neuroleptics and an anticholinergic, biperiden, in the antiavoidance, catalepsy and ptosis tests was investigated in mice for the purpose of predicting the extrapyramidal side-effects of neuroleptics. The cataleptic effect of most neuroleptics used was antagonized to some extent by biperiden, while the ptotic effect was hardly influenced. The antiavoidance effect of neuroleptics was differentially antagonized by biperiden. The antiavoidance effect of haloperidol, trifluperidol and perphenazine was markedly antagonized and that of chlorpromazine moderately. However, the effect of thioridazine, chlorprothixene, levomepromazine and clozapine was little antagonized. In neuropharmacological tests, haloperidol, trifluperidol and perphenazine exhibited a selective antidopaminergic activity, while chlorprothixene, levomepromazine and clozapine showed antidopaminergic, antiadrenergic and also anticholinergic activities when similar doses were given. These results indicate that biperiden antagonism may be marked in the tests related to the extrapyramidal symptoms and in drugs liable to induce extrapyramidal side-effects, however, there would be little or no antagonism in drugs possessing the anticholinergic property and eliciting few extrapyramidal side-effects
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  • Kyoichi SHIMOMURA, Masaaki TOMOI, Jo MORI
    1979 Volume 29 Issue 3 Pages 447-456
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Tranylcypromine (TCP), a monoamine oxidase inhibitor, induced a hyperpyrexia in rats which had been given repeated doses of LiCl. This hyperpyrexia was not prevented by the pretreatment with α-adrenergic blockers (phenoxybenzamine and phentolamine), β-adrenergic blocker (DL-propranolol), histamine blockers (promethazine and diphenhydramine), anticholinergic agent (atropine), inhibitors of prostaglandin synthesis (acetylsalicylic acid and sodium salicylate). Among the dopamine (DA) blockers tested, chlorpromazine, thioridazine, fluphenazine, perphenazine and haloperidol, all of which are reported to inhibit the DA-sensitive adenylate cyclase, prevented the hyperpyrexia. On the other hand, sulpiride and metoclopramide, which are reported not to inhibit the DA-sensitive adenylate cyclase, were without effects on the hyperpyrexia. The hyperpyrexia was potentiated by injection of theophylline, a nucleotide phosphodiesterase inhibitor. The cyclic AMP level in the caudate nucleus was significantly increased only when TCP produced the hyperpyrexia in the LiCl-pretreated rats. The cyclic AMP level in the hypothalamus remained unchanged. These results suggest that DA produced the hyperpyrexia by mediation of the cyclic AMP in the caudate nucleus, but not in the hypothalamus.
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  • Tetsuji HIRONAKA, Shoji MORIMOTO
    1979 Volume 29 Issue 3 Pages 457-466
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    The present study describes the potentiating effect of dimorpholamine on twitch contraction of skeletal muscle and its mechanism on a cellular basis. Low concentrations (about 2×10-5 g/ml) of dimorpholamine potentiate the twitch contraction of frog sartorius muscle. In relatively high concentrations of 10-4-10-3 g/ml, however, the potentiation was followed by depression. Endplate potential was not affected by the drug. Dimorpholamine depolarized slightly the muscle membrane. The contracture tension vs. membrane potential relationship was hardly affected by the drug in the presence of 2×10-7 M tetrodotoxin. Action potentials recorded from muscle fibers treated with ethylene glycol showed marked and progressive increases in duration during exposure to the drug, and were finally blocked. It was concluded that twitch potentiation caused by dimorpholamine is due to the prolongation of the action potential. A likely molecular mechanism of this drug is discussed in terms of the kinetic model proposed by Adrian et al. (J. Physiol. 208, 607-644, 1970) for the excitable membrane of frog sartorius muscle.
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  • Katsuaki ITO, Hideaki KARAKI, Norimoto URAKAWA
    1979 Volume 29 Issue 3 Pages 467-476
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Effects of palytoxin (PTX) on isolated papillary muscles of guinea pigs were studied in an attempt to elucidate the mechanical and electrical activities. Inotropic effects of PTX above 3×10-9 g/ml were; an early positive inotropic effect, slowly developing contracture accompanied by decline in phasic tension, appearance of aftercontractions and arrhythmias at high doses. The positive inotropic effect of PTX was enhanced in high Ca2+ medium but was not modified by propranolol. PTX induced a sustained depolarization and decrease in the amplitude, upstroke velocity and duration of action potential. During development of depolarization, arrhythmias occurred, which lasted for 5-10 min and reappeared 30-60 min after. Oscillatory afterpotential often appeared. Neither reserpine nor practolol prevented the PTX-induced arrhythmia while propranolol prevented it. Tetrodotoxin slowed the development of depolarization due to PTX and inhibited PTX-arrhythmias. In low Na+ medium, PTX exerted fewer effects on resting and action potentials and produced no arrhythmia. The results suggest that PTX-induced depolarization is responsible for the generation of contracture and arrhythmia and that the depolarization is due to the change in membrane Na permeability.
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  • Romeo LISCIANI, Annarosa BALDINI, Daniela BENEDETTI, Sofia PUTZOLU
    1979 Volume 29 Issue 3 Pages 477-479
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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  • Tomitaro KITA, Taeko HATA, Junko IIDA, Ryozo YONEDA, Sadahiro ISIDA
    1979 Volume 29 Issue 3 Pages 479-482
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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  • Hiroaki FURUTA
    1979 Volume 29 Issue 3 Pages 483-485
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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  • Nobuhiro INATOMI, Yasunobu ISHIHARA, Susumu OKABE
    1979 Volume 29 Issue 3 Pages 486-488
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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  • Shigenobu SHIBATA, Ryozo OISHI, Showa UEKI
    1979 Volume 29 Issue 3 Pages 489-492
    Published: 1979
    Released on J-STAGE: December 19, 2006
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  • Shigenori WATANABE, Masayoshi INOUE, Showa UEKI
    1979 Volume 29 Issue 3 Pages 493-496
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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  • Yoshiki MATSUI, Toshiharu KAMIOKA
    1979 Volume 29 Issue 3 Pages 496-499
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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  • Sumiko FUJINO, Hideki TSUKADA, Mamoru TANAKA, Takashi IGARASHI, Katsuj ...
    1979 Volume 29 Issue 3 Pages 499-502
    Published: 1979
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
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