日本薬理学雑誌
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
68 巻, 6 号
選択された号の論文の14件中1~14を表示しています
  • β-Phenylethylamine誘導体の脳室内投与によるマウス自発運動量の変化について
    桜田 忍, 只野 武, 嶋 啓節, 木皿 憲佐
    1972 年 68 巻 6 号 p. 619-625
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Influence of β-phenylethylamines on behavioural changes in mice was studied andthe following results were obtained.
    1) When noradrenaline or isoproterenol was intracerebrally injected, spontaneousmotor activity (SMA) tested by wheel cage and photo cell counters method decreased.
    2) In mice treated with tyramine, SMA tested by wheel cage method was decrea-sed but SAM in photo cell counters method markedly increased. Dopamine also increased in SMA tested by wheel cage method.
    3) In mice treated with tyramine or dopamine 2 hr after isocarboxazide, SMA tested by both photo cell counters and wheel cage method markedly increased.
  • 第1報主としてモルモット交感神経シナプス機構におけるNEMの影響
    北野 高史
    1972 年 68 巻 6 号 p. 626-635
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    1) In isolated guinea-pig atria preparations, NEM was capable of producing not only elevation of contractile tension and increase in heart rates at earlier stages, but also elevation of resting tension with arrhythmia at later stages. All effects of NEM were, however, completely prevented if cysteine was added simultaneously and in equimolar concentration.
    2) Effects of NEM at earlier stages were blocked by propranolol, guanethidine and reserpine, but restored by pre-incubation with norepinephrine in reserpinized atria.
    3) At earlier stages, NEM enhanced the concentration of vas deferens induced by low frequency stimulation of the hypogastric nerve, but inhibited it at a later stage.
    4) Enhancement by NEM of the contraction of vas deferens induced by sympathe-tic nerve stimulation appears to be dependent on Ca ion concentration in the suspending medium.
  • 第2報 NEMの起炎作用ならびに過血糖効果について
    岡田 信行
    1972 年 68 巻 6 号 p. 636-649
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    1) NEM produced remarkable inflammation in rats. The cause appears to be inhibition of SH radicles in tissues, while any loss in the effectiveness of NEM can be attributed to a binding with red cells.
    2) Hyperglycemia induced by NEM appears to be due to enhanced sugar mobilization from the liver, inhibition of glucose uptake in muscles and increase in epinephrine release from the adrenal medulla.
  • 臼井 八郎, 大隅 清明, 戸田 昇, 藤原 元始
    1972 年 68 巻 6 号 p. 650-661
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    1. Guaiacol glycerol ether mononicotinate (GGEMN) の循環作用を生体位犬および兎と摘出兎動脈および心房標本を用いて検討した.
    2. Amobarbital sodium麻酔犬の頚動脈圧はGGEMN静注 (0.3-10mg/kg) によって一過性に下降した. Atropine, Hexamethonium, DiphenhydramineおよびPropranolol前処置はGGEMNの血圧作用を抑制しなかった.
    3. 麻酔犬総頚動脈および大腿動脈血流量はGGEMN静注 (0.3-3.0mg/kg) によって一過性に増加した. GGEMN 3~30μg/kg総頚動脈ないし大腿動脈内注射はそれぞれの動脈血流量を用量に応じて増加した.
    Atropine, Tolazoline, HexamethoniumおよびPropranolol静注前処置はGGEMNの血流増加作用を抑制しなかった. GGEMNの母体化合物Guaicol glycerol ether (GGE) およびニコチン酸の単独動注ならびにGGEとコニチン酸の等モル混合液動注の血流増加作用はGGEMNの同作用に比して軽度であった.
    4. 無麻酔拘束兎心臓律動数および心電図波形はGGEMN 5~10g/kg経口投与ないし30mg/kg静注によって影響をうけなかった. Papaverine 0.5g/kg経口投与および30mg/kg静注は約半数例に著明な心電國波形の変化と徐脈をもたらし,致死させた.
    5. 摘出兎大動脈および上腸間膜動脈ラセン状条片標本の緊張度はGGEMN (10-5-3×10-4g/ml) 適用によって有意に低下した. GGEMN前処置はNoradrenalineないしBaCl2の用量作用曲線を右下方に移動した. Transmural stimulationによる血管平滑筋の一過性収縮もまたGGEMNによって抑制された.
    6. 摘出兎心房律動数はGGEMN高濃度 (3×10-4g/ml) 適用によって軽度減少し,収縮力は中等度抑制された. GGEMNの心臓作用はPapaverineのそれに比べ明かに軽度であった.
    7. 以上の成績より, GGEMNは支配自律神経を介することなく,血管平滑筋に直接作用して筋緊張を低下する結果,末梢血流を増加すると考える.心臓毒性は弱く,安全域はPapaverineに比べ大であった.
  • 抗炎症作用および鎮痛作用
    鶴見 介登, 野崎 正勝, 林 元英, 山口 東, 平松 保造, 藤村 一
    1972 年 68 巻 6 号 p. 662-682
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Anti-inflammatory and analgesic effects of niflumic acid, 2-arylamino-nicotinic acid corresponding to anthranilic anti-inflammatory agents, were studied by a detailed analysis in comparison with fenamates (flufenamic acid and mefenamic acid). Niflumic acid showed similar inhibitory effects on the increased vascular permeability to flufena-mic acid and a stronger effect than mefenamic acid. In the acute edema test induced by various phiogists, niflumic acid had the same potent anti-edematous properties as fena-mates and phenylbutazone. In the subacute edema test induced by mustard, niflumic acid showed an inhibitory effect similar to flufenamic acid which had stronger effect than mefenamic acid. When the inhibitory effects on the proliferation of granulation tissue were tested by cotton-pellet and granuloma pouch methods, niflumic acid was more potent than mefenamic acid, but somewhat less than flufenamic acid and phenylbuta-zone. Niflumic acid had potent inhibitory action similar to fenamates on the ultra-violet erythema, but the effects of niflumic acid and mefenamic acid on the adjuvant arthritis were weaker than that of flufenamic acid. The analgesic action of niflumic acid was similar to that of mefenamic acid which was more potent than flufenamic acid and phenylbutazone.
    From the above results, niflumic acid was proved to have similar effects to flufena-mic acid and a more potent effect than mefenamic acid on acute inflammation, but similar effects to mefenamic acid and less than flufenamic acid on the subacute or chronic inflammation. Furthermore, it was similar to mefenamic acid and more potent than flufenamic acid regarding analgesic actions. It may, therefore, be considered that niflumic acid has a clinical application similar to mefenamic acid as a non-steroid anti-inflammatory agent.
  • 一般薬理作用
    鶴見 介登, 林 元英, 中野 万正, 呉晃 一郎, 藤村 一
    1972 年 68 巻 6 号 p. 683-703
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    In a previous paper, it was reported that niflumic acid had similar effects to flufenamic acid regarding anti-inflammatory actions and similar effects to mefenamic acid regarding analgesic actions. In this paper, general pharmacological actions of niflumic acid were examined in comparison with those of fenamates.
    Acute toxicity of niflumic acid was somewhat stronger than that of flufenamic acid and the toxic action had the same obstruction on heart function as fenamates, but in doses causing anti-inflammatory activity, it had no effect on the cardiovascular and respiratory systems. Niflumic acid showed weak activities similar to mefenamic acid in such tests as locomotion, rotarod, anti-convulsion, hypnotic potentiation to barbiturates, hypothermic and anti-pyretic actions. Therefore, it appeared not to have side effects on the central nervous system.
    It decreased urine volume, urinary sodium and potassium output, but these acti-vities were comparable to those usually observed with the conventional non-steroid anti-inflammatory agents and it was also free of any effects on the blood sodium, potassium and sugar levels. Although it delayed the excretion rate of phenol red in rabbit like fenamates, a clinical uricosuric action may not be presumed since the activity was weaker than that of phenylbutazone.
    It inhibited the isolated intestinal and uterine movement in a high concentration, but did not show specific antagonistic actions on such spasmogenic substances as histamine, acetylcholine, 5-HT and BaCl2. It was found that niflumic acid caused stomach ulcer and this ulcerogenic action was the only marked effect of niflumic acid.
    From the above results, niflumic acid proved to be slightly stronger in toxicity and side effects on the gastrointestinal tract than fenamates. It may, therefore, be consi-dered that niflumic acid is more prone to acute inflammation than to chronic in toxicity and in side effects as well as in anti-inflammatory activity.
  • 金戸 洋, 小井田 雅夫, 土江 冨美代
    1972 年 68 巻 6 号 p. 704-715
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Treatment of mice with doxepin up to 10 days did not result in a demonstrable tole-rance to the inhibitory effect on spontaneous motor activity. While mice or rats were forced to drink doxepin solution for 30 days or after abrupt withdrawal, abnormal behavior ascribable to physical dependence was not observed. Doxepin did not sup-press abstinence signs which were elicited in barbital dependent mice. Based on these results, it may be concluded that this compound does not have tolerance and physical dependence producing liability.
  • 植木 昭和, 小川 暢也, 渡辺 繁紀, 五味田 裕, 荒木 泰典, 藤原 道弘, 八谷 アツ子, 古謝 武志, 井上 雅義, 大槻 勲夫, ...
    1972 年 68 巻 6 号 p. 716-761
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Doxepin was compared with amitriptyline and imipramine in respect to behavioral pharmacology with rats and mice. Doxepin antagonized reserpine hypothermia and tetrabenazine ptosis and potentiated amphetamine stereotypy and methamphetamine hyperactivity. In this respect doxepin and amitriptyline were equipotent but doxepin was more potent than amitriptyline and imipramine regarding major or minor tranquilizing-like effects, such as reduction of locomotor activity in open-field test, inhibition of conditioned avoidance response, suppression of experimentally induced hyperemotionality, anticonvulsant activity and potentiation of hypnotics and anesthetics. Doxepin is, therefore, characterized as an antidepressant drug having marked tranquilizing activities.
  • 大槻 勲夫, 石河 醇一, 酒井 真理子, 島原 邦代, 籾山 とく子
    1972 年 68 巻 6 号 p. 762-799
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Doxepin caused a fall in blood pressure accompanied by an increase of peripheral blood flow in dogs. Doxepin potentiated the effect of norepinephrine (NE) on blood pressure and nictitating membrane of cats but reduced the effect of epinephrine (E). The pharmacological properties of doxepin resemble those of amitriptyline but differ from imipramine which exhibits a dual effect on blood pressure and a potentiating effect to both NE and E. Doxepin, however, showed less pronounced anticholinergic effects than amitriptyline in the following experiments; spasmolytic action on acetylcholine induced contraction in isolated guinea pig ileum, mydriatic action in mice and protective action against methacholine death in mice. These results suggest that in clinical use, doxepin causes less anticholinergic side effects than amitriptyline.
  • ヒ素とBlood BrainBarrier,とくに飼料のおよぼす影響について
    田村 俊吉, 野崎 茂
    1972 年 68 巻 6 号 p. 800-808
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    These experiments were done to ascertain the function of the blood brain barrier utilizing dyes Bromphenol Blue and Evans Blue.
    1) In rats fed arsenite-added 1000 p. p. m. milk and cereal for 7 days, half of the rats died, however the blood brain barrier was normal, and the brains were not colored by either dye.
    2) In rats fed arsenite-added 650 p. p. m. milk and cereal for 14 days, all rats were healthy, the blood brain barrier was normal and the brains were not colored by either dye.
    3) In rats fed arsenite-added 650 p. p. m. milk and cereal for 35 days, few rats died. In the case of milk fed rats the blood brain barrier was normal and the brains not colored by either dye, but in the cereal fed rats all were abnormal and the brains were colored by Bromphenol Blue, but not by Evans Blue.
    4) Milk appears to be more protective for the brain than cereal.
  • 渡辺 繁紀, 森本 保人, 植木 昭和
    1972 年 68 巻 6 号 p. 809-836
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Electroencephalographic (EEG) effects of doxepin were compared with those of imipramine, amitriptyline, chlorpromazine and diazepam in unanesthetized, unrestrained rabbits and cats.
    1) Doxepin induced high voltage fast waves in spontaneous EEG of the amygdala followed by a generalized drowsy pattern in all brain areas under behavioral sedation.
    2) Doxepin suppressed the EEG arousal responses induced not only by photic or auditory stimulation but also by mesencephalic reticular and hypothalamic stimulation, whereas chlorpromazine blocked only the former without affecting the latter.
    3) Doxepin facilitated the recruiting response and showed no effect on the photic driving response in the visual cortex.
    4) Doxepin exerted a biphasic effect on the limbic afterdischarges elicited by either hippocampal or amygdaloid stimulation; i.e. Doxepin initially depressed them, as did diazepam, but thereafter enhanced them as did chlorpromazine.
    These EEG effects of doxepin were qualitatively similar to those of imipramine and amitriptyline, but different from those of chlorpromazine and diazepam.
  • 門間 芳夫
    1972 年 68 巻 6 号 p. 837-847
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Using Chance-Hagihara's techniques, oxydative phosphorylation was studied on the heart muscle mitochondria isolated from guinea pigs pretreated with an intravenous injection of drugs. Sympathomimetics and adrenergic blocking agents systemically administered, produced a remarkable increase in QO2 at state 4 on oxidative phosphorylation in heart mitochondria. Although the value of respiratory control index showed a dose dependent lowering, ADP/0 ratio was not significantly lowered unless very large doses were given. Epinephrine and norepinephrine when added to the incubation medium, did not produce any direct effect on the respiratory function of isolated mitochondria. Thus, it was postulated that sympathomimetics induced some impairment on mitochondrial respiration by a systemic action.
  • 岳中 典男, 石原 高文, 樋口 マキヱ, 開 一矢, 川越 テツミ, 梅田 照久, 野崎 正義, 竹中 登一
    1972 年 68 巻 6 号 p. 848-856
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    Effects of a new adrenergic beta receptor blocking agent, YB-2 (1-(7-indenyloxy)-3-isopropylaminopropan-2-ol hydrochloride), on coronary circulation and myocardial metabolism, especially in interaction with catecholamines were investigated in isolated blood perfused and in situ heat preparations of the dog. In isolated hearts, intracoronary injection of YB-2 0.1mg did not produce any change in coronary blood flow (CBF), myocardial oxygen consumption (QO2) and redox potential (ΔEh), but caused a slight fall in perfusion pressure (PP) and appreciable decreases in heart rate (HR) and myocardial contractile force (MCF). At the same time, isoproterenol-induced augmentation of CBF, QO2, HR and MCF and reduction of ΔEh were greatly suppressed, while the hypotensive effect was converted to a hypertensive one.
    In situ hearts, YB-2 0.1_??_0.2mg/kg i. v. produced significant reductions in HR, BP, CBF, CO, QO2 and CW, but caused a slight increase in ΔEh. Myocardial uptake and consumption of glucose were approx. the same as controls, while myocardial free fatty acid consumption was decreased after YB-2. YB-2 0.1mg/kg considerably depressed increases in HR, CO, CBF, QO2 and CW induced by epinephrine 1μg/kg i. v, and greatly enhanced the hypertensive effect of the amine.
    It is concluded that YB-2 is a potent adrenergic beta receptor blocking agent and possibly effective as an anti-anginal agent.
  • ヒ素に対する耐容性の発生におよぼす乳汁成分の影響について
    野崎 茂
    1972 年 68 巻 6 号 p. 857-868
    発行日: 1972年
    公開日: 2010/07/30
    ジャーナル フリー
    1) In cases where rats had been raised on whey powder-added or casein-added food containing the arsenite, nutrition was approximately the same as in the milk fed cases.
    2) Cheese had no effect on absorption of the arsenite and did not inhibit transfer of the arsenite into organs.
    3) Butter and whey powder had no effect on the absorption of arsenite but did inhibit the arsenite from transformation into the brain, as well as inhibiting to some extent movement into the kidney.
    4) Casein, like milk, inhibited absorption of the arsenite from transformation into organs.
feedback
Top