The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
23 巻, 1 号
選択された号の論文の15件中1~15を表示しています
  • M.L. GUPTA, T.K. GUPTA, K.P. BHARGAVA
    1973 年 23 巻 1 号 p. 1-4
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    The effect of reserpine and phenoxybenzamine pretreatment has been studied on copper acetate induced ovulation in rabbits. It has been observed that neither reserpine nor phenoxybenzamine prevented the ovulatory response of the copper salt. These findings indicate that copper induced ovulation does not appear to be mediated through the involvement of central adrenergic mechanisms.
  • T.K. GUPTA, R. KUMAR, Basheer ALI, Surendra S. PARMAR
    1973 年 23 巻 1 号 p. 5-8
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    Substituted quinazolone salicylhydrazides exhibiting anticonvulsant activity against pentylenetetrazol and maximal electric shock (MES) seizures were found to potentiate nembutal induced hypnosis in mice. All these compounds were found to inhibit selectively in vitro oxidation of pyruvic acid and α-ketoglutaric acid. The relative electronegativity of the substituents at position 6 of the quinazolone nucleus in no way paralleled their enzyme inhibitory effects.
  • Koichi NAKAYAMA, Hiroyuki KOIKE, Takeshi OSHIMA, Koroku HASHIMOTO
    1973 年 23 巻 1 号 p. 9-16
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    The antiarrhythmic activities of N-propyl ajmaline was evaluated in anesthetized dogs. N-propyl ajmaline was effective on aconitine-induced atrial and ouabain-induced ventricular arrhythmias. Antiarrhythmic activity of N-propyl ajmaline was ten times more potent than that of ajmaline. Rapid infusion of N-propyl ajmaline induced ventricular flutter and fibrillation, but these effects were abolished by pre-treatment with β-adrenergic blocking agent.
  • Shoji MARUYAMA
    1973 年 23 巻 1 号 p. 17-27
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    The electrophysiological and antiarrhythmic effects of LB-46 on the membrane potentials of Purkinje fibers and ventricular muscle fibers of the dog were studied by means of the microelectrode technique in comparison with those of propranolol. The effects of LB-46 on the membrane potential of Purkinje fibers consisted of a reduction in amplitude of the action potential due to a diminution or loss of overshoot and unchanged resting potential, an acceleration of repolarization, a prolongation of latency, and a decrease in mean rate of rise. Nearly the same electrophysiological effects were produced by propranolol at a lower concentration. LB-46, as well as propranolol, prevented the isoproterenol-induced arrhythmia by blocking the increase in diastolic depolarization. The antiarrhythmic action of LB-46 may be due considerably to direct action on the cardiac cell membrane and partly to a beta-receptor blockade. It is very probable that LB-46 is more specific in beta-receptor blocking and little weaker in antiarrhythmic activity than propranolol.
  • Hiroyuki NABATA, Hiroshi SAITO, Keijiro TAKAGI
    1973 年 23 巻 1 号 p. 29-41
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    Pharmacological studies of neutral saponins (GNS) of Panax Ginseng root, were performed. GNS showed CNS-depressant action in inhibition of spontaneous and exploratory movements, and in potentiation of CNS-depressant. A specific blocking action of conditioned response by GNS was significantly confirmed in small doses and did not produce loss of righting reflex, motor incoordination or myo-relaxation. Analgesic, anticonvulsant and antipyretic effects were recognized. From the tests described above in addition to those of traction, hypothermia, fighting behavior and ratio of two reflexes, GNS appears to have neuroleptic activity. There was neither hemolytic nor vasodilator action on the hind leg or coronary vascular beds.
  • Hiroshi SAITO, Mariko MORITA, Keijiro TAKAGI
    1973 年 23 巻 1 号 p. 43-56
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    Pharmacological properties of a crude saponin fraction (GF-DS-I) and saponins (GF-DS-II) which were obtained from Panax Ginseng leaves, were estimated by blind screening consisting of three tests : 1) neuropharmacological observations in mice, 2) tests on the respiratory and cardiovascular system in rats, and 3) tests on the guinea-pig isolated ileum. GF-DS-I appeared to have CNS-depressive, neuroleptic, analgesic, hypertensive, cholinergic, and histamine-like activities, while GF-DS-II, had CNS-depressive, neuroleptic, analgesic, hypotensive, atropine-like and papaverine-like activities.
    These neuroleptic activities, were examined and confirmed by tests on motor activity, exploratory movements, muscle tone, motor coordination, hypothermia and potentiation of CNS-depressant, and pole climbing, anticonvulsant and analgesic tests. No effects were seen on hemolysis.
  • Shingo YANO, Masatoshi HARADA
    1973 年 23 巻 1 号 p. 57-64
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    A stress method in mice which develops gastric erosions was devised. This stress procedure consisted of restraint and water immersion. Maximal development of gastric erosions was observed when mice were restrained and immersed at 25°C for 18 hr. There was no apparent sex difference in the susceptibility to this method. Drug study was performed to evaluate the drug sensitivity of this stress method. From the results, it can be concluded that this stress method is a good testing ground for drug sensitivity.
    Conclusively, the present stress method in mice is suggested to be of advantage in studying gastric ulceration and evaluating the ability of drugs to inhibit gastric erosions.
  • Norihide TAKEYA, K.K. CHEN
    1973 年 23 巻 1 号 p. 65-76
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    The effects of DCI or BW 62-235 on the arrhythmia caused by 3 erythro-phleum alkaloids, 6 aglycones and 2 glycosides were investigated in the cat anesthetized with sodium secobarbital.
    Generally speaking, these agents were ineffective against coumingine or erythro-phleine arrhythmia, although arrhythmia shortening action was observed in a few cases with cassaine.
    These agents were ineffective against gitaloxigenin arrhythmia, however, did show evident antiarrhythmic action against digitoxigenin or periplogenin.
    In the cases of arrhythmia produced by hellebrigenin, bufalin or cinobufagin these agents tend to reduce the duration of the arrhythmia.
    In arrhythmias elicited by glycosides, duration of thevetin arrhythmia was reduced. by DCI and BW 62-235, however, the arrhythmia of scillaren A was not clearly shortened by these agents.
    From these results it can be concluded that there is no relationship between the effectiveness of these antiarrhythmic agents and the chemical structures of the arrhythmia inducing drugs, although some question does remain in the case of erythro-phleum alkaloids concerning intrinsic local anesthetic action. A certain relationship between the effectiveness of these agents and arrhythmic action of these cardiotonics was observed, i.e., the antiarrhythmic agents was effective against the arrhythmia caused by the drugs which have a fleeting arrhythmic action.
  • Chung Shin LIAO, Issei TAKAYANAGI, Keijiro TAKAGI
    1973 年 23 巻 1 号 p. 77-82
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    The effects of external divalent cations on drug-receptor interaction were examined using guinea pig taenia. The effects of histamine on membrane potential of taenia in various solutions were also examined using the sucrose gap method.
    Ca2+ and Me2+ played an important role in the combination of histamine with its receptor. Sr2+, Mn2+ and Co2+ do not substitute for. Ca2+ and Me2+ in this interaction.
    None of divalent cations used were involved in the competitive antagonist-receptor interaction or in the irreversible antagonist-receptor interaction.
    Histamine which induced membrane depolarization and increased tension in normal Locke Ringer solution had no effect on the membrane potential and tension in Mg2+-free Se2+-solution. The mechanism for this phenomenon has been discussed herein.
  • Sukehiro CHIBA, Yuji NAGAWA
    1973 年 23 巻 1 号 p. 83-96
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    The inhibitory effect of benzodiazepine-type agents such as 8-chloro-6-phenyl-4H-s-triazolo [4, 3a] [1, 4] benzodiazepine (D-40TA), diazepam and nitrazepam on the spinal and supraspinal polysynaptic reflexes was compared with that of mephenesin, methocarbamol, chlorzoxazone and chlormezanone in cats. Benzodiazepines did not depress the spinal and supraspinal polysynaptic reflexes or reflex potentials in the spinal and the gallamine-immobilized cats. In these respects, chlormezanone resembled benzodiazepines. On the other hand, mephenesin, methocarbamol and chlorzoxazone blocked these reflexes in all kinds of preparations such as the anesthetized, the spinal, the decerebrate and the gallamine-immobilized preparations. D-40TA depressed gamma rigidity at the dose below that necessary to depress alpha rigidity. Moreover, it inhibited more profoundly the tonic stretch reflex than the phasic one. Spontaneous and evoked discharges of the muscle spindle in the decerebrate cat were significantly depressed by D-40TA, while those of spinal cat were unaffected.
    These results suggest that skeletal muscle relaxation by benzodiazepines including D-40TA is attributed to the primary depression of the brain stem reticular system and in turn the ascending inhibitory action via the gamma system on the spinal and supraspinal polysynaptic neurons. It should be stressed that the integrity of the connection between the brain stem and gamma system in the spinal cord and its related muscles is also required for eliciting the depression of supraspinal polysynaptic reflex by these agents. Mephenesin-type agents presumably inhibit directly the interneurons at the spinal and supraspinal levels.
  • Eiichi OGAWA, Shiro SUZUKI, Hiroshi TSUZUKI, Mutsuko KAWAJIRI
    1973 年 23 巻 1 号 p. 97-105
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    Cadmium chloride solution (contained 146 PPM of Cd) was administered to mice as drinking fluid for 90 days. Carbonic anhydrase activity was unaffected in blood, liver and kidneys 10 days after administration, however, enzymic activity was significantly reduced in all three organs thereafter. Catalase activity was unchanged until day 31, but was significantly reduced in all organs thereafter. Hemoglobin levels remained unchanged after 10 and 20 days administration, but were significantly reduced thereafter.
    Time course of response of carbonic anhydrase and catalase activities and blood hemoglobin level to CdCl2·21/2H2O in a dose of 10 mg/kg were examined at intervals ranging from 4 to 24 hr after a single s.c. injection. Carbonic anhydrase activity in liver, kidney and blood was significantly decreased every time, however, catalase activity in the above organs as well as the blood hemoglobin level did not change at any time.
    Whole-body retention of orally administered 115mCdCl2 with or without the carrier was examined at one week intervals for 30 days. Whole-body retention of 115mCd was significantly less in the carrier group than in the carrier-free group. Average Cd uptake for 30 days was 0.56 μg/day in the carrier-free group and 0.1 mg/day in the carrier group. Cd concentration in liver and kidneys on day 31 was 0.04 and 0.15 PPM respectively in the carrier-free group and each 24 PPM in the carrier group.
  • Nobuo NAKAMURA, Yoshihisa KOYAMA, Tetsuo KOJIMA, Hiroshi TAKAHIRA
    1973 年 23 巻 1 号 p. 107-120
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
    Caerulein produces an acceleration of motility of rabbit ileum (in situ). The effect appears to be based on peripheral action. Sympathetic nerve endings appear not to be involved in the action. In the small intestine transit test (mouse) caerulein accelerated the transit when carbon powder was present. It is therefore considered that caerulein does not induce generalized muscle contraction but rather a coordinated propulsion in the intestinal tract. Caerulein in a larger dose discontinues flow of content out of the stomach probably due to pyloric spasm.
    Caerulein produced contraction of rabbit gallbladder (in situ) at doses lower than the threshold dose of ileum motility acceleration.
    In isolated ileum of guinea-pig, caerulein produced contraction at low doses. The action of caerulein appears to be mediated through the nerve : it appears to act on non-nicotinic receptor of the cholinergic nervous element and accelerate liberation of acetylcholine. It also appears to act, at least in part, on the atropine-resistant nervous element.
    In isolated guinea-pig gallbladder, as different from the in situ case, caerulein produced contraction at doses almost equal to the threshold of contraction in isolated guinea-pig ileum. The action of caerulein appears to be a direct action on the gallbladder smooth muscle.
    Caerulein had no effect on isolated was deferens and uterus. For this reason, the action of caerulein is considered to be of organ specificity.
  • Tomio SEGAWA, Koichi KAWASAKI, Haruaki YAJIMA
    1973 年 23 巻 1 号 p. 121-123
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
  • Chikako TANAKA, Seisuke TANAKA, Yoshinori ITOKAWA, Shuji TAKAORI
    1973 年 23 巻 1 号 p. 123-125
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
  • Atsuko MINAMIDATE, Shizuko TAKANO, Toshiko HASHIKAWA, Yasushi ABIKO
    1973 年 23 巻 1 号 p. 126-128
    発行日: 1973/02/01
    公開日: 2011/03/23
    ジャーナル フリー
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