Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 74, Issue 5
Displaying 1-10 of 10 articles from this issue
  • Yasuo GOMI, Hidetada KOMATSU
    1978 Volume 74 Issue 5 Pages 539-548
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of cocaine on acetylcholine-induced contracture of isolated rat tracheal preparation were determined. The sensitivity of the preparation to acetylcholine but not methacholine and carbachol was increased by cocaine. The maximum responses induced by choline esters were not augmented by cocaine. The potentiation of acetylcholine was remarkable in calcium-deficient medium and cocaine augmented acetylcholine-contracture of the preparation suspended in calcium-free Tyrode solution. Calcium-contracture of the preparation suspended in isotonic 60 mM or 100 mM-K+ Locke-Ringer solution was not augmented by cocaine. Extrapolating the time course of decrease in acetylcholine-contracture in calcium-free Tyrode solution, rates of calcium movement from and into calcium-stores were determined and it was found that cocaine did not change the calcium-content and rate of calcium-efflux but the rate of calcium-uptake was apparently increased with cocaine. The contribution of anticholinesterase activity of cocaine to potentiation of acetylcholine appeared negligible and the affinity of acetylcholine-receptor to acetylcholine and atropine was not changed with cocaine. Thus, cocaine increases acetylcholine-induced calcium-release and potentiates acetylcholine-contracture of isolated rat tracheal preparation.
    Download PDF (5233K)
  • Hiroshi MAEKAWA, Junnosuke YAMAMOTO, Yoshiko KATO, Atsushi SEKIYA
    1978 Volume 74 Issue 5 Pages 549-558
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Recent clinical studies have suggested an association of tolbutamide (TB) therapy with an increased incidence of cardiovascular deaths. In this study, the effects of a newly synthetized hypoglycemic agent, gliclazide (GC), on the cardiovascular system were investigated, and compared with those of TB. Results are as follows: GC was found to be about ten times as active as TB in decreasing blood glucose in rabbits. GC and TB produced a dose-dependent increase in blood pressure and little change in heart rate in rats and rabbits. In driven left rat and rabbit atria, these agents produced a positive inotropic effect. The positive inotropic effects of these drugs were not altered by pretreatment with propranolol, or theophylline. These agents produced little change in the rate in spontaneous beating rat, rabbit and guinea pig atria. Higher doses produced a slightly negative chronotropic response. Neither agent potentiated the inotropic effects of isoproterenol on the rabbit and guinea pig left atria. In isolated perfused working rabbit hearts, these compounds produced a slight decrease in coronary flow. It is concluded that GC and TB possess positive inotropic effects on isolated atria, and these effects are not mediated either through adrenergic mechanisms or the cyclic AMP system.
    Download PDF (4006K)
  • Hajime TAMAKI, Kenichi SAITO
    1978 Volume 74 Issue 5 Pages 559-571
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of timepidium bromide (TB) on the motility of various smooth muscles and the secretion of digestive juice were examined and the activity was compared with those of hyoscine-N-butylbromide (HB) and atropine sulfate (Atr). In dogs, TB inhibited the spontaneous and bethanechol-induced motility of various regions of the gastrointestinal tract, the activity being almost the same as that of Atr but stronger than that of FIB. All these drugs exhibited a similar inhibitory effect on the motility of the gallbladder. On the contrary, the inhibitory effect of TB on the spontaneous motion of urinary bladder was somewhat weaker than those of HB and Atr, while this effect on the bethanechol-induced motility was nearly equal the effects of HB and Atr. It was also evident that TB inhibited the gastric acid secretion induced by bethanechol: the activity was stronger than that of HB, while it was weaker than that of Atr. Similar effects on the gastric acid secretion were also found in rats. In the case of salivary secretion, however, TB and HB produced much weaker inhibitory actions than Atr. TB even at a higher dose produced little significant effect on the pancreatic and biliary secretion of rats. The uterine contraction induced by methacholine was inhibited by all these drugs. The mydriatic activity of TB in mice was found to be the weakest among the drugs tested.
    Download PDF (5786K)
  • Takeshi MIYATA, Kazuo TAKAHAMA, Abul HASANAT, Kozaburo IKEGAMI, Kazuo ...
    1978 Volume 74 Issue 5 Pages 573-588
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    The bronchodilating effect and other related pharmacological properties of N-AB 365 were studied in comparison with those of isoproterenol, salbutamol and clorprenaline. N-AB 365 was found to produce a bronchodilating effect 1/20 ?? 1/100, 1/10 ?? 1/40 and was 2 to 5 times as strong as effects of isoproterenol, salbutamol and clorprenaline, respectively. The bronchodilating effect of N-AB 365 was sustained more than 10 times as long as those of isoproterenol and salbutamol, and in particular with oral administration, was much more potent. The bronchodilating effect of N-AB 365 seems to be due mainly to excitation of the adrenergic β2-receptor and partially to papaverine-like action. N-AB 365 showed an inhibitory effect on experimentally induced bronchial asthma by spraying of bronchoconstrictors and the effect by oral administration was much stronger than those of isoproterenol and salbutamol. N-AB 365 affected neither the volume output of respiratory tract fluid nor the tracheal ciliary movement with the doses around ED50 in bronchodilating action, however, it increased ciliary activity and decreased the volume output of respiratory tract fluid with large doses. Antitussive effect was also demonstrated only with the large doses. N-AB 365 induced a moderate decrease in blood pressure through vasodilatation but did not influence respiration. The effect of N-AB 365 on heart rate varied. There were cases of no change, slight increase or slight decrease in heart rate.
    Download PDF (7367K)
  • Tamotsu FUKUDA, Mikiko KATAOKA, Azuma YAMAGUCHI, Hisayuki TANIZAWA
    1978 Volume 74 Issue 5 Pages 589-595
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Relationships between the infusion speed and lethal dose of several amino acid solutions of various concentrations were studied in male Sprague Dawley rats. When the amino acid solutions were continuously infused at various speeds, a functional relationship between the dose producing a cardiac arrest (DCA) and infusion speed was established. The DCA/infusion speed was characterized by two ranges with an increasing DCA as increase or decrease of infusion speed and by its intermediate range of a flat minimum with a practically constant DCA regardless of varying the infusion speed. A practically constant LD50 was obtained in the infusion of each amino acid solution within the infusion speed in the intermediate range. The LD50 of each amino acid solution was dependent on the crystalloid osmotic pressure.
    Download PDF (3000K)
  • Showa UEKI, Shigenori WATANABE, Michihiro FUJIWARA, Tsuneyuki YAMAMOTO ...
    1978 Volume 74 Issue 5 Pages 597-614
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Triazolam was 4 to 5 times as potent as diazepam in reducing hyperemotionality of either septal-lesioned or olfactory bulbectomized rats (O. B. rats), and in suppressing muricide in O. B. rats. This agent was equipotent with diazepam in inhibiting fighting behavior of long-term isolated mice, but was longer in duration of action. Triazolam was approximately 4 times more potent than diazepam in preventing pentetrazol convulsion, but was 10 times less potent in inhibiting maximal electroshock convulsion in mice. The muscle relaxant effect of triazolam as assessed by the inclined screen test was 34 times, and the effect on rotarod performance was 17 times more potent than that of diazepam in mice. Triazolam (0.2 ?? 0.5 mg/kg i.v.) changed the EEG to a drowsy pattern in unanesthetized rabbits with a chronic electrode implant, and suppressed the EEG arousal response to auditory stimulation and electrical stimulation given to either the mesencephalic reticular formation or posterior hypothalamus. The limbic afterdischarges induced by either hippocampal or amygdaloid stimulation were also markedly inhibited by triazolam. These EEG effects of triazolam were qualitatively similar to, but were 4 to 5 times more potent than those of diazepam. These results indicate that triazolam is a potent tranquilizer with a longer duration of action, and the muscle relaxant effect is considerable as compared with diazepam.
    Download PDF (8001K)
  • Yutaka GOMITA, Hiroko GOMITA, Hatsumi NAKAEBISU, Yasufumi KATAOKA, Sho ...
    1978 Volume 74 Issue 5 Pages 615-628
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Effects of triazolam on various types of conditioned behavior were investigated and compared mainly with diazepam in rats. The active conditioned avoidance response of the rat in a Shuttle box was inhibited by triazolam and diazepam only at large doses. The passive avoidance response in a step-down method was not affected by either triazolam or diazepam, but was markedly suppressed by chlorpromazine. The low rate response of hypothalamic self-stimulation behavior was markedly increased by triazolam at doses ranging from 2 to 40 mg/kg p.o., but was suppressed at doses over 80 mg/kg p.o. The high rate response was unaffected by triazolam even at doses of 40 ?? 180 mg/kg p.o. The low rate response was increased by diazepam at doses of 1 ?? 10 mg/kg p.o. and was suppressed at 80 mg/kg p.o. The high rate response was reduced by diazepam at 180 mg/kg p.o. In the conflict situation of the rat subjected to food reward and foot-shock punishment, the lever press response in the unpunished period was reduced by triazolam at doses of 1 ?? 5 mg/ kg p.o., whereas that in the punished period was markedly increased. Similar effects were observed with diazepam at doses of 15 ?? 20 mg/kg p.o. Triazolam appeared to be 10 ?? 15 times more potent than diazepam in this anticonflict effect. Thus, triazolam appears to be a potent antianxiety agent.
    Download PDF (5874K)
  • Makizo HIRABAYASHI, Masahiro IIZUKA, Sakutaro TADOKORO
    1978 Volume 74 Issue 5 Pages 629-639
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    A hand-made apparatus which is easily manipulative, cheap, durable and clean was used to measure ambulatory activity of a mouse. The apparatus was assembled with the same type of two plastic round basins commercially available (25 cm in diameter) put one upon another. A pivot was fixed at the center of the outsurface of the inner basin (A), and its open end was inserted into the open socket fixed at the center on the bottom of the outer basin (B). Three microswitches equipped on the brim of (B) at equal intervals were activated and the counts were recorded according to the tiltings of (A) through the movements of the mouse. In order to examine accuracy of the measurement, effects of d-amphetamine (1.25 ?? 5.0 mg/kg), methamphetamine (1.0 ?? 4.0 mg/kg), cocaine (10 ?? 40 mg/kg) and morphine (5.0 ?? 20.0 mg/kg) on the ambulatory activity were investigated. Marked accelerating effects were observed dose dependently after the administrations of all the drugs. Furthermore, the patterns of the activity showed characteristic properties of each drug. This method is especially useful to measure the acute effect of drugs on the ambulatory activity in mice, and many units can be set up at the same time.
    Download PDF (5179K)
  • Kenji ONODERA, Takeshi TADANO, Kenji SAKAI, Kensuke KISARA, Yasumi OGU ...
    1978 Volume 74 Issue 5 Pages 641-648
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    The emotional behavioral aspects and the interaction between the changes of the polyamine contents and muricide response in thiamine deficient rats were investigated. In the thiamine deficient group, there was evidence of muricide and such increased progressively with advanced thiamine deficient feeding. This muricide was characteristic in the following respects; 1) the killer-rats did not eat but only kill a mouse and it was quite difficult to remove a sacrificed animal from the cage. 2) they bit at random into any body region of the mouse. 3) the killer-rats did not bite inanimate objects such as nails nor chalk. 4) the muricide induced by thiamine deficiency could not be suppressed by a single injection of thiamine HCl. On the 30th day of the experimental feeding, both spermidine and spermine levels in the brain of the thiamine deficient group decreased significantly as compared to the control and the pair-fed groups. Both spermidine and spermine levels were reversed to the control levels with a intraperitoneal administration of thiamine. There were no significant differences in spermine and spermidine levels between the killer-rats and non-killer-rats in the thiamine deficient group.
    Download PDF (3779K)
  • Kenji ONODERA, Kensuke KISARA
    1978 Volume 74 Issue 5 Pages 649-652
    Published: 1978
    Released on J-STAGE: March 29, 2007
    JOURNAL FREE ACCESS
    Male Wistar rats weighing 75 to 85 g and maintained on a thiamine deficient diet for 33 days showed growth inhibition with the principal manifestation of significant weight loss from about the 28 day of experimental feeding. Symptoms of polyneuritis were also evident. On the 20th day of feeding and thereafter, rats on the thiamine deficient diet had a persistent erection. This was observed in 7% of the rats on a thiamine deficient group on day 20, 30.7% on day 25, 63.6% on day 30, and 100% on day 33. Effects of thiamine hydrochloride, in a single dose of 1 mg/kg given subcutaneously on the symptoms of thiamine deficiency were investigated. The treated rats recovered from the polyneuritic symptoms, and persistent erection disappeared in one out of 5 rats on the 3rd day and in 2 more rats on the 7th day. Persistent erection disappeared completely in rats maintained on a thiamine sufficient diet 3 days after single subcutaneous administration of thiamine HCl. These observations suggest that persistent erection was brought on as a consequence of thiamine deficiency.
    Download PDF (1988K)
feedback
Top