巻号一覧
28 巻, 1 号
選択された号の論文の23件中1～23を表示しています
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Koichiro GO, Kaito TSURUMI, Hajime FUJIMURA1978 年 28 巻 1 号 p. 1-12
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーSince it had been demonstrated that L-5418 has an anti-convulsant effect with no relation to its anti-inflammatory properties, comparative studies were carried out with the use of currently available anti-convulsant agents as controls. L-5418 inhibited tonic convulsions induced by maximal electroshock and strychinine in mice and prevented animals from the death sequence. L-5418 had an inhibitory effect on tonic convulsions induced by pentetrazol and N-sulfamoyl-hexahydroazepinc (SaH 41-178), but not on clonic convulsions by those compounds at even a high dosage or on clonic convulsions induced by picrotoxin and bemegride. Trimethadione produced an inhibitory effect on both tonic and clonic convulsions. The hypnotic agents, phenobarbital and glutethimide inhibited both convulsions, but a higher dose was required in the case of clonic convulsions. Anti-convulsant agents are classified into three different groups according to their mode of action. L-5418 had the same mode of action as seen with diphenylhydantoin and carbamazepine. As L-5418 did not inhibit tremor induced by tremorine, an anti-Parkinson effect was ruled out. When L-5418 was administered alone, the animals did not lose the righting reflex nor show muscle relaxation observed in inclined screen and rotarod tests. Moreover, the compound had no influence on the aggressive behavior induced by electrical stimulation or olfactory bulb ablation. L-5418 possesses a selective anti-convulsant effect, yet has no sedative, tranquilizing or disturbing effects on movement such as equilibrium disturbance or muscle relaxation. L-5418 may prove useful for grand mal epilepsy as it is less toxic than diphenylhydantoin and carbamazepine.抄録全体を表示PDF形式でダウンロード (520K) -
Tomio SEGAWA, Hiroko MURAKAMI, Hiroshi OGAWA, Haruaki YAJIMA1978 年 28 巻 1 号 p. 13-19
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーEffect of methionine-, leucine-enkephalin(met-, leu-enkephalin) and substance P on the transmission in mouse vas deferens was studied. Both met and leu-enkephalin inhibited electrically induced contraction of vas deferens at 10-8-10-7 M, met-enkephalin being 1.4 times more active than leu-enkephalin. Nalorphine (10-6 M) antagonized these effects. Substance P (10-9-10-7 M) had no effect on the contraction. Met-and leu-enkephalin (10-7-10-5 M) decreased the high potassium induced [3H]-norepinephrine release from vas deferens, while substance P (10-5 M) significantly increased it. Nalorphine (10-5 M) reversed the inhibitory effect of met-enkephalin. These results indicate that these peptides modify the transmission of sympathetic nerve in mouse vas deferens.抄録全体を表示PDF形式でダウンロード (290K) -
Kenji TASAKA, Koiti ENDO, Hidemasa YAMASAKI1978 年 28 巻 1 号 p. 21-31
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーThe electric capacitance of isolated rat mast cells and its change under the influence of either n-decylamine or toluidine blue was investigated. Since the electric circuit employed in the detection unit is the one merely sensitive for the capacitance changes, output signals pertain to the capacitance of the tested cell alone. N-decylamine released histamine without accompanying degranulation; and it caused a marked swelling of mast cells and a striking decrease of capacitance, although electric capacitance is usually proportional to the size of the cell. Morphological changes induced by toluidine blue are seemingly correlated with the changes in capacitance. At the concentrations (25-50 μg/ml) in which the mast cell became enlarged, electric capacitances exceeded the control value. However, at the concentrations higher than 100 μg/ml in which the cell became shrunken, the capacitance values were less than control value. Pretreatment with DNP (0.1 mM) or oxyphenbutazone (0.05-0.2 mM) was of little effect in inhibiting the histamine release, morphological alterations and capacitance changes due to n-decylamine, but pretreatment with either prevented all of those changes produced by toluidine blue. The mechanism of the capacitance changes in mast cells induced under influence of those compounds is discussed.抄録全体を表示PDF形式でダウンロード (653K) -
Seigo FUJIMOTO, Shiro HISADA1978 年 28 巻 1 号 p. 33-40
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーEffects of intracerebroventricularly (i.c.v.) injected PGE2 and PGF2α on the urine outflow were studied in ethanol-anaesthetized rats. PGE2 and PGF2α, when injected i.c.v., caused dieresis which was followed by antidiuresis. Phentolamine, when perfused i.c.v., was an antidiuretic and inhibited the diuretic and antidiuretic effects of PGE2. Diphloretin phosphate inhibited both effects of PGE2. Polyphloretin phosphate (PPP) and propranolol blocked completely the PGE2-induced diuresis and consequently remarkable antidiuresis was observed after the combined treatments with PGE2 and PPP or propranolol. When PGE2 was perfused i.c.v., a sustained diuresis was obtained and antidiuretic effects of noradrenaline, γ-aminobutyric acid and L-glutamate were potentiated, inhibited and unaffected by the perfusion with PGE2, respectively. It was indicated that the antidiuretic effect of PGE2 could be dissociated from the diuretic effect and that both effects were mediated through adrenergic mechanisms. The present result also suggested that central PGE2 might act as a modulator of some neurotransmitters involved in water metabolism.抄録全体を表示PDF形式でダウンロード (351K) -
Yoshiro OKANO, Takeshi MIYATA, Shiang-Huey HUNG, Toshiro MOTOYA, Mikik ...1978 年 28 巻 1 号 p. 41-47
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーPiperidine is one of pharmacologically active biogenic amines While two pathways for piperidine production have been reported, little is known about metabolism of the compound. In the present study, piperidine and its hydroxylated, conjugated and unknown metabolites were detected in rat urine by radiochromatographic analysis. Using GC-MS technique, it was confirmed that 3-hydroxypiperidine and 4-hydroxypiperidine are major metabolites of piperidine of either exogenous or endogenous origin. The findings substantiate the existence of a mechanism which inactivates piperidine in the living body, since both metabolites lack the potent pharmacological activities as those induced by piperidine.抄録全体を表示PDF形式でダウンロード (324K) -
Seigo FUJIMOTO, Shiro HISADA1978 年 28 巻 1 号 p. 49-56
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーEffects of centrally affecting drugs on the diuretic and antidiuretic actions of intracerebroventricularly (i.c.v.) injected prostaglandin (PG) E2 in ethanol-anaesthetized rats were studied. PGE2, when injected i.c.v. at a dose of 1 nmole, produced diuresis followed by antidiuresis. When morphine (0.1 mM) was perfused i.c.v., urine outflow decreased and neither diuretic nor antidiuretic effects of i.c.v. PGE2 was apparent. The perfusions with picrotoxin, γ-aminobutyric acid and L-glutamate inhibited either the diuretic or the antidiuretic effect of PGE2. On the other hand, when pentobarbital, diazepam, isoniazid and strychnine were perfused i.c.v., the diuretic action of PGE2 was diminished and antidiuresis in response to PGE2 remained unchanged. These results suggested that the diuretic and antidiuretic effects of PGE2 could be separated. The development of the diuretic effect of PGE2 was completely blocked by amitriptyline and antidiuresis was increased. In rats pretreated i.c.v. with reserpine, the diuretic effect of PGE2 was prolonged and antidiuresis in response to PGE2 was not observed. An antidiuretic action of i.c.v. norepinephrine was not varied by reserpine. Mechanisms for both effects of PGE2 are discussed.抄録全体を表示PDF形式でダウンロード (387K) -
Yoshiaki SHIRASAWA, Kyozo KOKETSU1978 年 28 巻 1 号 p. 57-60
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーBullfrog sympathetic ganglion cells treated with nicotine are hyperpolarized with application of 5-HT. This 5-HT hyperpolarization, however, was not observed if preparations were pretreated with d-TC before being treated with nicotine. When preparations were treated with ACh or carbamylcholine, which transiently depolarizes ganglion cells, hyperpolarization did take place. Such was also observed in the presence of Ringer's solution if preparations were pretreated with the K+-free Ringer's solution. These results suggested that ganglion cells were hyperpolarized by the action of 5-HT when the Na+-pump of these cell's was accelerated by accumulation of intracellular Na+, as the result of a transient depolarization or extracellular K+ deficiency.抄録全体を表示PDF形式でダウンロード (158K) -
Eiichi HAYASHI, Jun YAMADA, Masaru KUNITOMO, Mamoru TERADA, Masaru SAT ...1978 年 28 巻 1 号 p. 61-72
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーEffects of L-ascorbate 2-sulfate (AAS) on lipid metabolism and on pathological changes of aorta and visceral organs were investigated in cholesterol fed rabbits, with ascorbic acid (AA) and clofibrate (CPIB) as reference compounds. Administration of AAS (300 and 150 mg/kg) inhibited an increase in the levels of serum total cholesterol, free cholesterol, triglycerides and phospholipids caused by cholesterol feeding. A high dose of AAS prevented an increase of liver weight. An increase in the level of liver cholesterol was inhibited by a high dose of AAS. Both doses of AAS effectively prevented an accumulation of cholesterol in the aorta. The area rate of atheromatous plaque in aorta was less in specimens from both groups of AAS than in those from control I. Pathological changes in intima and media of aorta were milder in specimens from both groups of AAS. Development of pathological changes in arteries of various organs were prevented with both doses of AAS.抄録全体を表示PDF形式でダウンロード (873K) -
Kinya KURIYAMA, Kazuo NAKAGAWA, Katsumi NAITO, Makoto MURAMATSU1978 年 28 巻 1 号 p. 73-84
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーThe effects of consecutive oral administration of morphine on the cyclic AMP synthesizing system and cyclic AMP dependent protein kinase activity in the cerebral cortex of mice were examined. The administration of morphine (2-4 weeks) induced an increase of the cyclic AMP formation by activating adenylate cyclase, whereas responses of the cyclic AMP synthesizing system to biogenic amines (norepinephrine, dopamine and histamine) added in vitro was found to be significantly attenuated in these animals. Cyclic AMP dependent protein kinase activity in the cerebral cortex was also increased following a consecutive oral administration of morphine. These changes in the activities of adenylate cyclase and protein kinase were found mainly in crude mitochondrial and/or synaptosomal fractions. Morphine induced decrease in the response of the cyclic AMP synthesizing system to biogenic amines was rapidly reversed, and a significant increase of the cyclic AMP formation in the presence of added norepinephrine compared with that found in morphinized animals was observed following the administration of levallorphan, a narcotic antagonist. On the other hand, the changes in adenylate cyclase and cyclic AMP dependent protein kinase activities were not affected significantly by levallorphan administration. These results suggest that alterations in activities of cyclic AMP synthesizing system and of cyclic AMP dependent protein kinase may be involved in processes of the formation of morphine dependence. Possible involvement of abrupt increments in the sensitivity of “norepinephrine receptor-adenylate cyclase” system and a subsequent increase in cerebral cyclic AMP is also suggested as a cause of morphine withdrawal syndrome.抄録全体を表示PDF形式でダウンロード (589K) -
Ryoichi ISHITANI, Takio IWAMOTO1978 年 28 巻 1 号 p. 85-92
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーBinding of H3-imipramine, H3-dimetacrine and S35-chlorpromazine to synaptosomes of rat cerebral cortex was studied using a centrifugation method, and kinetic analysis of the experimental data. Three psychotropic drugs were shown to be rapidly bound to synaptosomes at 2°C, representing a typical binding mode with two classes of binding components, i.e., saturable and non-saturable binding. A double reciprocal plot of the saturable binding component of these drugs revealed that H3-dimetacrine and S35-chlorpromazine represented a single binding mode, whereas H3-imipramine showed a multiple one. When the synaptosomes were treated by freezing and thawing 15 times, a high affinity binding component of H3-imipramine was not observed, while the other two drugs showed a single binding mode as well as those of the undisrupted synaptosomes. To investigate the specificity of this multiple binding mode, comparative binding studies of H3-imipramine were carried out using myelin fragments of rat cerebral cortex. In the myelin fragments preparation, two typical classes of binding mode as shown in the synaptosomes were also recognized. However, a double reciprocal plot of the saturable binding component showed only a straight line, i.e., single binding mode. These findings suggest that imipramine has multiple binding sites to synaptosomes and a high affinity binding component is affected by freezing and thawing procedure.抄録全体を表示PDF形式でダウンロード (370K) -
Koichiro GO, Kaito TSURUMI, Hajime FUJIMURA1978 年 28 巻 1 号 p. 93-104
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーL-5418 has an anti-convulsant effect which is similar to that of diphenylhydantoin. the effects of L-5418 on EEG activity in rabbits with acute and chronic implantation of electrodes were studied in comparison with those of currently available anti-convulsants. Intraveneous administration of L-5418 increased a slow-wave sleep pattern in the spontnaneous EEG, which was also induced by diphenylhydantoin. With respect to the focal seizure in the cerebrai cortex induced by local appliaction of penicillin, L-5418 showed suppressive effects on the frequency and duration of seizure discharge, and on the spread of seizure discharge to other parts of the brain. The efficacy was about twice that of dipnenylhydantoin. L-5418 and diphenylhydantoin did not increase the threshold of seizures induced by bemegride while trimethadione raised the threshold. L-5418 also showed suppressive ellects twice as active as diphenylhydantoin on after-discharge induced by electrical stimulation of the hippocampus and amygdala. This suppressive effect on after-discharge of the limbic system may be parallel with the suppressive effect on psychomotor seizure. From these results of L-5418 on an experimental model of epilepsy, it is suggested that L-5418 has suppressive eifects similar to that of diphenythydantoin on convulsion and the efficacy proved to be twice that of diphenylhydantoin in the EEG study.抄録全体を表示PDF形式でダウンロード (500K) -
Yoshio HATANO, Noboru TODA1978 年 28 巻 1 号 p. 105-114
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーEffects of fentanyl and morphine on chronotropic responses to transmural stimulation applied to the S-A node were studied in isolated rabbit atria. The stimulation caused a frequency-dependent negative chronotropism followed by positive chronotropism, the former abolished by atropine and the latter suppressed by propranolol. The former response at 5 and 20/sec was attenuated in a dose-dependent manner by fentanyl and morphine. Potency ratio of fentanyl to morphine was approx. 50-100. The inhibitory effect of fentanyl and morphine on the response to stimulation of cholinergic nerves was partially prevented or reversed by both naloxone and levallorphan, and also partially reversed by repeated washing of the preparations. Antagonism by naloxone was appreciably greater than that of levallorphan. The negative chronotropic response to transmural stimulation was reduced by levallorphan but not by naloxone. Dose-chronotropic response curves of acetylcholine were unaffected by treatment with fentanyl and morphine. High concentrations of fentanyl and morphine attenuated the response to stimulation of adrenergic nerves, while dose-chronotropic response curves of noradrenaline were not influenced by these narcotics. Naloxone was ineffective in preventing or reversing the effect of fentanyl and morphine. It is therefore concluded that fentanyl and morphine activate opiate receptors located in cholinergic nerve terminals innervating the S-A node, thereby interfering with the release of acetylcholine. Further, it appears that high concentrations of fentanyl and morphine interfere with the release of noradrenaline from postganglionic adrenergic nerve terminals in rabbit atria; however, this action is not related to opiate receptors.抄録全体を表示PDF形式でダウンロード (436K) -
P.Y.D. WONG, C.H. YEUNG1978 年 28 巻 1 号 p. 115-123
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーThe rate of fluid reabsorption in the cauda epididymidis of rat has been measured in vitro. Both adrenaline and isoprenaline produced a prompt, reversible and dose dependent increase in the reabsorption rate. These effects were completely blocked by propranolol. The response to noradrenaline consisted of two components. In the presence of an alpha blocker, noradrenaline caused an increase, while in the presence of a beta blocker, it produced an inhibition in the rate of fluid reabsorption. The effects of these adrenergic agents were only observed when sodium ions were present in the intraluminal fluid, suggesting that they only affect the Na+-dependent component of fluid reabsorption. The possibility that they may affect the active transport of sodium in the duct was discussed. The effects of these adrenergic agents were interpreted in terms of the presence of alpha and beta receptors in the epithelium of the rat cauda epididymidis.抄録全体を表示PDF形式でダウンロード (389K) -
Tsukasa SAKURADA, Kensuke KISARA1978 年 28 巻 1 号 p. 125-132
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーFreely moving rats with chronically implanted electrodes were used and the electroencephalogram (EEG) from the occipital cortex and the dorsal hippocampus, the electromyogram (EMG) and the electrooculogram (EOG) were simultaneously recorded. The REM (rapid eye movement) sleep stage was significantly shortened without a marked change of the Non-REM sleep from the 24th to the 32nd hr following injection of 40 μg of SPD. The waking stage significantly increased, and the Non-REM sleep and REM sleep markedly decreased immediately after the injection of 40 μg of SPM to the 8th, and from the 24th to the 32nd hr. The amount of total sleep significantly shortened from the 72nd to the 80th hr following injection of 40 μg of SPD. The administration of 40 μg of SPM significantly reduced the amount of total sleep in every period measured for 8 hr. Marked change was observed from the 24th to the 32nd hr following injection of 100 μg of PUT, and Non-REM sleep and total sleep produced a significant decrease. These results show that the intraventricular administration of polyamines including PUT inhibits the amount of normal sleep.抄録全体を表示PDF形式でダウンロード (334K) -
Eiichi HAYASHI, Jun YAMADA, Masaru KUNITOMO, Mamoru TERADA, Yoshinori ...1978 年 28 巻 1 号 p. 133-143
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーEffects of L-ascorbate 2-sulfate (AAS) on lipid metabolism were studied in guinea pigs maintained on diet I with sufficient L-ascorbic acid (AA) supplement or on diet II without AA supplement. AAS (300 mg/kg) inhibited an increase in serum and liver levels of lipids to a greater degree than AA (175 mg/kg), a reference compound, in hyperlipidemic guinea pigs induced by cholesterol feeding with diets I or II. AAS also induced a decrease in serum and liver levels of lipids in guinea pigs which had been previously maintained for 6 weeks on diet II containing 1.0 % cholesterol. AA administration significantly increased AA level in various organs of animals maintained on both the diets containing cholesterol. It also rectified the AA level lowered by previous maintenance on diet lI containing cholesterol. AAS showed a slight AA replacing effect on the AA level. Both AA and AAS exerted preventive and curative effects on several symptoms due to chronic AA deficiency.抄録全体を表示PDF形式でダウンロード (442K) -
S. MOTOMURA, O.-E. BRODDE, H.J. SCHÜMANN1978 年 28 巻 1 号 p. 145-153
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーExperiments were carried out on the isolated rabbit papillary muscle driven at 0.5 Hz in order to further elucidate the mechanism of the positive inotropic effect evoked by dopamine. The dose-response curve for dopamine was not affected by the antagonists pimozide (10-6 M), yohimbine (10-5 M), pindolol (3×10-8 M) and phentolamine (10-6 M), when these agents were given separately. Only the simultaneous administration of yohimbine plus pindolol and phentolamine plus pindolol, respectively, shifted the entire curve to the right. This shift was not further influenced by pimozide. Dopamine (10-4 M) increased the cyclic AMP content of the papillary muscle by about 50%; this increase was not affected by pimozide, but was markedly elevated by yohimbine and completely depressed by pindolol. From the present results it is concluded, that dopamine produces its positive inotropic effect through stimulation of myocardial α- as well as β-adrenoceptors to about the same degree; stimulation of specific dopaminergic receptors, however, is not involved. The stimulation of β- adrenoceptors is accompanied by an increase of the cyclic AMP level, while that of α-adrenoceptors is not.抄録全体を表示PDF形式でダウンロード (430K) -
Tsutomu URUNO, Keiichi TABATA, Mitsuo YAMADA, Kazuhiko KUBOTA1978 年 28 巻 1 号 p. 155-157
発行日: 1978年
公開日: 2006/12/19
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Tomio SEGAWA, Hiroko MURAKAMI, Akemi INOUYE, Yasue TANAKA1978 年 28 巻 1 号 p. 158-160
発行日: 1978年
公開日: 2006/12/19
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Shigetoshi CHIBA, Miyoharu KOBAYASHI, Yasuyuki FURUKAWA1978 年 28 巻 1 号 p. 160-162
発行日: 1978年
公開日: 2006/12/19
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Tadahiro SHIKIMI, Chiyoko INAGAKI1978 年 28 巻 1 号 p. 162-165
発行日: 1978年
公開日: 2006/12/19
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Kazuo KAWASAKI, Hideo TAKESUE, Akira MATSUSHITA1978 年 28 巻 1 号 p. 165-168
発行日: 1978年
公開日: 2006/12/19
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Teruaki KAWANO, Masami NIWA, Yuhzo FUJITA, Masayori OZAKI, Kazuo MORI1978 年 28 巻 1 号 p. 168-171
発行日: 1978年
公開日: 2006/12/19
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Mizuo MIYAZAKI, Hideki OKUNISHI, Tadamitsu KOMORI, Kenjiro YAMAMOTO1978 年 28 巻 1 号 p. 171-174
発行日: 1978年
公開日: 2006/12/19
ジャーナル フリーPDF形式でダウンロード (161K)
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