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Volume 84 (1984)
- Issue 6 Pages 471-
- Issue 5 Pages 411-
- Issue 4 Pages 327-
- Issue 3 Pages 259-
- Issue 2 Pages 155-
- Issue 1 Pages 1-
Volume 84, Issue 2
Displaying 1-7 of 7 articles from this issue
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Pharmacology of a 1H-1, 2, 4-triazolyl benzophenone derivative (450191-S), a new sleep-inducer (III)Behavioral study on interactions of 450191-S and other drugs in miceNobuhiro IBII, Masahito HORIUCHI, Ken-ichi YAMAMOTO1984 Volume 84 Issue 2 Pages 155-173
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSInteractions between 450191-S and other representative drugs which might be clinically used with 450191-S were behaviorally investigated in mice, and compared with the cases of nitrazepam, estazolam and triazolam. The potencies of 450191-S and nitrazepam in preventing pentetrazol convulsions were markedly decreased by aminopyrine, whereas that of estazolam was remarkably increased by phenytoin. Administration of nitrazepam with other drugs, except aminopyrine, or of estazolam together with haloperidol exhibited an anticonvulsive pattern different from the case of dosing with either drug alone. Only the effect of triazolam was not influenced by any drugs used. The potency of haloperidol against apomorphine-induced climbing behavior was significantly reduced by nitrazepam, and the pattern of the haloperidol effect was changed by treatment together with 450191-S or estazolam. However, triazolam had no influence on the effect of haloperidol. The antagonistic activity of imipramine to reserpine-induced hypothermia was slightly decreased by 450191-S, estazolam and triazolam, but little affected by nitrazepam. In the protection from maximal electroshock convulsions (MEC), the potency of phenytoin was significantly decreased by 450191-S and triazolam. Moreover, the anti-MES pattern of phenytoin was altered by nitrazepam. Estazolam exerted no significant influence on the effect of phenytoin. Analgesic activities of morphine and/or aminopyrine were potentiated by pretreatment with sleep-inducers, but not 450191-S. Thus, judging from the potency and stability of the anti-pentetrazol effect, 450191-S seems to be inferior to triazolam, but superior to nitrazepam and estazolam. Also, 450191-S may be differentiated from other sleep-inducers by the fact that only 450191-S did not potentiate the analgesic activities of morphine and aminopyrine.View full abstractDownload PDF (9691K) -
General pharmacological activitiesKen-ichi YAMAMOTO, Motohiko UEDA, Atsushi KUROSAWA, Katsumi HIROSE, Ma ...1984 Volume 84 Issue 2 Pages 175-212
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSGeneral pharmacological activities of 450191-S were studied in various species of animals and compared with those of reference benzodiazepines (BDZ). 450191-S at doses of 10 mg/kg slightly decreased (-5°C) the rectal temperature of rabbits. 450191-S decreased respiratory and heart rates in anesthetized cats, but the effects were less than those of diazepam or triazolam. 450191-S increased respiratory and heart rates in conscious dogs, but had no effect on the blood pressure, electrocardiogram and autonomic nervous system in cats and dogs. The drug displayed a slight spasmolytic activity in the small intestine of guinea pigs and a slight inhibitory effect on isolated non-pregnant and pregnant uteri of rats. These effects were less than those of diazepam or nitrazepam. Below doses of 25 mg/kg, 450191-S did not affect urinary volume and electrolyte excretions in rats. It also decreased brain norepinephrine (NE) turnover rates in rats, but decreased NE and dopamine turnover rates in mice. These effects of 450191-S were less than those of nitrazepam. 450191-S was found to be minimally irritating to the ocular mucosa in rabbits and did not irritate the stomach and small intestine in rats. These effects were also compared with those of active metabolites of 450191-S, M-1, M-2, M-A, M-3 and M-4, and the superiority of the mother compound over its metabolites was clarified.View full abstractDownload PDF (17793K) -
Makoto TANAKA, Hiroshi KOJIMA, Akira AKASHI1984 Volume 84 Issue 2 Pages 213-219
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThis investigation was undertaken to analyze the EEG synchronizing effects of timiperone in cats. The effects of timiperone on the brain-stem reticular and hypothalamic activating system, diffuse and specific thalamic projection system, and caudate spindle were investigated by the electroencephalographic method. Timiperone produced a weak inhibition of EEG arousal response induced by electrical stimulation of the sciatic nerve almost without affecting that which was induced by stimulation of the mesencephalic reticular formation. Furthermore, timiperone suppressed the activation of neocortical EEG in response to stimulation of the posterior hypothalamus more selectively than that of limbic EEG. Neither the recruiting response to stimulation of the centro-median nucleus of the thalamus nor the augmenting response to stimulation of the ventro-postero-lateral nucleus of the thalamus was modified by timiperone. In addition, timiperone significantly potentiated the caudate spindle. The EEG effects of haloperidol were qualitatively similar to those of timiperone. These results indicate that the synchronizing effect of timiperone may be mediated by a suppression of an ascending reticular activating system and may influence the conscious levels and sleep-wakefulness cycle in cats.View full abstractDownload PDF (3859K) -
Hiroyuki YOSHIMURA, Nobuya OGAWA1984 Volume 84 Issue 2 Pages 221-228
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe present study was conducted to investigate the effects of psychotropic drugs on agonistic behavior between resident and intruder mice. The effects of four doses of the following drugs were assessed in either resident or grouphoused intruder mice: chlordiazepoxide (0, 5, 10 and 20 mg/kg, i.p.), haloperidol (0, 0.25, 0.50 and 0.75 mg/kg, i.p.) and imipramine (0, 5, 10 and 20 mg/kg, i.p.). Residents and intruders were drugged on alternate test days, and all animals received different sequences of each of the drug conditions according to a random schedule. The injection-test interval was 30 min. When resident mice were treated with chlordiazepoxide the resident's aggressive episodes (sideways posture, attack bite, tail rattle) were significantly suppressed. Both haloperidol and imipramine also showed a similar suppressive effect on the resident's aggressive episodes, but haloperidol significantly suppressed locomotor activity at all doses. When intruder mice were treated with chlordiazepoxide, attack bites by untreated residents were significantly increased in a dose-dependent manner, and the frequency of defensive upright posture displayed by intruder animals were significantly decreased. Haloperidol and imipramine did not alter resident's behavior and intruder's upright posture when intruders were drugged. The results suggest that chlordiazepoxide has specific effects on both the hostility of the resident and the anxiety of the intruder, differing from haloperidol and imipramine.View full abstractDownload PDF (4396K) -
Toshiki WATANABE, Kunio MATSUHASHI, Satoshi TAKAYAMA, Haruka MORITA1984 Volume 84 Issue 2 Pages 229-241
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe drugs acting on the autonomic nervous system were administered intravenously to dams or intraperitoneally to the 20-day-old fetuses maintained by umbilical and placental circulation. The fetal heart rates were accelerated by the administration of isoproterenol, epinephrine, norepinephrine, tyramine and dopamine to fetuses, and they were decelecated by the injection of propranolol and methacholine to fetuses. However, the tachycardia caused by the fetal injection of isoproterenol and the bradycardia by methacholine were inhibited by the pretreatment of propranolol and atropine. The fetal bradycardia and hypoxia caused by the administration of epinephrine under the pretreatment of propranolol to fetuses were inhibited by the injection of alpha-adrenergic receptor blockers such as phentolamine and yohimbine. Furthermore, the tyramine treatment to fetuses produced significant acceleration of the fetal heart rate on day 19-20 of gestation, but not on day 18. These findings suggest that fetal cardiac beta-adrenergic, muscarine-cholinergic receptors and vascular postsynaptic alpha-adrenergic receptor may be sensitive enough to respond to sympathomimetic and sympatholytic drugs, and the fetal cardiac sympathetic innervation between the adrenergic nerve terminal and synapse effector cells may be developed on day 18-19 of gestation.View full abstractDownload PDF (6503K) -
Shohei HIGUCHI, Yuuko OSADA, Yoko SHIOIRI, Nobuko TANAKA, Susumu OTOMO ...1984 Volume 84 Issue 2 Pages 243-249
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSAcute inflammatory paw edema of rats was formed by the injection of 0.5% Mycobacterium tuberculosis-liquid parraffin suspension into the hind paw, and then the pain threshold of the inflamed paw decreased. At that time, the rats showed a three-legged gait, namely, the lame walking reaction. The reaction was inhibited by acidic nonsteroidal anti-inflammatory drugs, e.g., indomethacin, ibuprofen and aspirin, inhibitors of prostaglandin biosynthesis, at a lower dose level than those in the Randall-Selitto test using yeast edematous rats and in the flection tests using adjuvant arthritic or silver nitrate arthritic rats. On the other hand, basic nonsteroidal anti-inflammatory drugs, e.g., tiaramide HC1, mepirizole and perisoxal citrate, not inhibitors of prostaglandins biosynthesis, were less potent than the acidic nonsteroidal anti-inflammatory drugs in the inhibition of the lame walking reaction. When prostaglandin E2 was injected into the inflamed paw, the inhibitory effects of acidic nonsteroidal anti-inflammatory drugs on the reaction disappeared, but those of the basic nonsteroidal anti-inflammatory drugs didn't disappear. Bradykinin had no influence on the effects of both acidic and basic nonsteroidal antiinflammatory drugs in the inhibition of the reaction. Analgesic evaluation with the lame walking reaction is more sensitive than with the Randall-Selitto or the flection methods. Morphine, pentazocine and acetaminophen inhibited the reaction, and these effects didn't disappear by the injection of prostaglandin E2 into the inflamed paw. These results suggest that prostaglandins play important roles in inflammatory pain, and the lameness test can serve as a new method for evaluating analgesics such as anti-inflammatory drugs and for investigating the mechanism of inflammatory pain.View full abstractDownload PDF (3195K) -
Hiroshi TAKEDA, Kiyoshi SHIMOYAMA, Miwa MISAWA, Saizo YANAURA, Mitsuo ...1984 Volume 84 Issue 2 Pages 251-257
Published: 1984
Released on J-STAGE: March 07, 2007
JOURNAL FREE ACCESSThe effects of brovanexine (BvX) and BR-227 on sectetory activities of tracheal submucosal glands (SG) including behavior of mucus glycoproteins in the cells were investigated. BvX, BR-227 or bromhexine (BH) was given repeatedly at a dose of 10 or 20 mg/kg p.o. a day, to rats for 1, 3, 7 or 14 days. Then, the trachea was excised and drug effects were determined according to our histological/histochemical technique. The outer diameter of the acini of SG did not change, but the inner diameter markedly increased by the drug given for 3-14 days. The ratio of the acinar inner diameter to the tracheal wall thickness (AIWR) was increased with the 3, 7, and 14 day treatments with BvX or BR-227 at a dose of 10 mg/kg a day. On the other hand, these drugs at a dose of 20 mg/kg a day caused an increase in AIWR when drug was given for 1-14 days. BH (10 mg/kg a day)-induced increase in AIWR was shown when drug was administered for 7 and 14 days. The number of SG cells stained blue with alcian blue (pH 2.5)/periodic acid-Schiff decreased with the 1, 3, 7 and 14 day treatments, and a part of SG cells became red with the 7 and 14-day treatments. There was no significant difference in the effects among the three drugs both qualitatively and quantitatively. These findings indicate that repeated treatments with BvX and BR-227 have an effective secretagogic action on SG, and in addition, a mucolytic action toward acid glycoprotein in granules of the cells. The onset of mucolytic action of any of these drugs seemed to be ahead of that of the secretagogic action.View full abstractDownload PDF (3952K)
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