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Volume 68 (1972)
- Issue 6 Pages 619-
- Issue 5 Pages 495-
- Issue 4 Pages 385-
- Issue 3 Pages 255-
- Issue 2 Pages 129-
- Issue 1 Pages 1-
Volume 68, Issue 6
Displaying 1-14 of 14 articles from this issue
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Effect of intracerebrally administered β-phenylethylamines on behavioural changes in miceShinobu SAKURADA, Takeshi TADANO, Keisetu SHIMA, Kensuke KISARA1972 Volume 68 Issue 6 Pages 619-625
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSInfluence 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.View full abstractDownload PDF (438K) -
1st report: Effects of NEM on sympathetic synapses in guinea-pigsTakafumi KITANO1972 Volume 68 Issue 6 Pages 626-635
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESS1) 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.View full abstractDownload PDF (2234K) -
2nd report: Inflammatory and hyperglycemic properties of NEM in ratsNobuyuki OKADA1972 Volume 68 Issue 6 Pages 636-649
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESS1) 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.View full abstractDownload PDF (1623K) -
Rachiro USUI, Seimei OSUMI, Noboru TODA, Motohatsu FUJIWARA1972 Volume 68 Issue 6 Pages 650-661
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSSystemic blood pressure of dogs anesthetized with amobarbital sodium decreased transiently following intravenous injections of guaiacol glycerol ether mononicotinate (GGEMN) (0.3 to 10mg/kg). Treatment with atropine, hexamethonium, diphenhydramine and propranolol did not inhibit the hypotenisve effect of GGEMN. Carotid and femoral blood flow of anesthetized dogs was increased by intravenous (0.3 to 3.0mg/kg) and intraarterial injections (3 to 30μg/kg) of GGEMN in a dose-dependent manner. The flow increase was not inhibited by atropine, tolazoline, hexamethonium and propranolol. Guaiacol glycerol ether (GGE), nicotinic acid and a mixture of these drugs were apparently less potent in increasing the blood flow than GGEMN. The heart rate and the ECG pattern of unanesthetized, restrained rabbits were not influenced by intravenous injections of GGEMN in doses up to 30mg/kg and by oral administrations of the drug in doses up to 10g/kg. The tension of spirally-cut strips of rabbit thoracic aortae and superior mesenteric arteries was significantly decreased by GGEMN (10-4 to 3×10-3g/ml). Treatment of aortic strips with GGEMN shifted the dose-contractile response curves of noradrenaline and Ba++ to the right and downward. Contractile responses of aortic strips to transmural electrical stimulation were inhibited by GGEMN. The rate and the contratile force of isolated rabbit atria were not influenced by GGEMN in concentrations lower than 10-4g/ml but moderately reduced at 3×10-4g/ml. It may be concluded that an increase in the peripheral blood flow by GGEMN is due to a decrease in the peripheral vascular resistance, which would not be asso-ciated with interference with autonomic innervation but with direct (papaverine-like) actions on vascular smooth muscles. It appears that GGEMN is markedly less cardiotoxic than papaverine.View full abstractDownload PDF (1703K) -
Anti-inflammatory and analgesic actionsKaito TSURUMI, Masakatsu NOZAKI, Motohide HAYASHI, Azuma YAMAGUCHI, Ya ...1972 Volume 68 Issue 6 Pages 662-682
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSAnti-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.View full abstractDownload PDF (1266K) -
General pharmacological effectsKaito TSURUMI, Motohide HAYASHI, Kazumasa NAKANO, Koichiro GO, Hajime ...1972 Volume 68 Issue 6 Pages 683-703
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSIn 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.View full abstractDownload PDF (4086K) -
Hiroshi KANETO, Masao KOIDA, Fumiyo TSUCHIE1972 Volume 68 Issue 6 Pages 704-715
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSTreatment 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.View full abstractDownload PDF (784K) -
Showa UEKI, Nobuya OGAWA, Shigenori WATANABE, Yutaka GOMITA, Yasunori ...1972 Volume 68 Issue 6 Pages 716-761
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSDoxepin 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.View full abstractDownload PDF (2972K) -
Isao OTSUKI, Jyunichi ISHIKO, Mariko SAKAI, Kuniyo SHIMAHARA, Tokuko M ...1972 Volume 68 Issue 6 Pages 762-799
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSDoxepin 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.View full abstractDownload PDF (12256K) -
Blood Brain Barrier and Arsenite in Relation to FoodsShunkichi TAMURA, Shigeru NOZAKI1972 Volume 68 Issue 6 Pages 800-808
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThese 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.View full abstractDownload PDF (2828K) -
Shigenori WATANABE, Yasuto MORIMOTO, Showa UEKI1972 Volume 68 Issue 6 Pages 809-836
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSElectroencephalographic (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.View full abstractDownload PDF (1742K) -
Yoshio MONMA1972 Volume 68 Issue 6 Pages 837-847
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSUsing 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.View full abstractDownload PDF (677K) -
Fumio TAKENAKA, Takafumi ISHIHARA, Makie HIGUCHI, Ichiya HIRAKI, Tetsu ...1972 Volume 68 Issue 6 Pages 848-856
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSEffects 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.View full abstractDownload PDF (544K) -
Effect of Components of Milk on Arsenic Tolerance in the Digestive TractShigeru NOZAKI1972 Volume 68 Issue 6 Pages 857-868
Published: 1972
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESS1) 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.View full abstractDownload PDF (684K)
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