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Volume 71, Issue 8
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[in Japanese], [in Japanese]1975 Volume 71 Issue 8 Pages 753-755
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSDownload PDF (1032K) -
Hideaki TAMURA, Yoshiaki SHIRASAWA, Heiji HORI, Shoichi KONDO1975 Volume 71 Issue 8 Pages 757-768
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe effects of a new coronary vasodilator (dilazep) on isolated intestine, taenia coli, trachea, vas deferens, uterus, aorta and coronary arteries were investigated in rats, guinea pigs, rabbits and dogs. Dilazep showed relaxant effects on isolated smooth muscle in a concentration of 10-5 ?? 3 × 10-4 M and non-competitive inhibition on contraction induced by agonists (pD'2: 4.40 ?? 5.05). In guinea pig taenia coli, dilazep had a relaxant effect on K-contracture. The effect was qualitatively similar to that of papaverine. In guinea pig taenia coli, dilazep showed a Ca++ antagonistic effect in a concentration as high as 3×10-6M. The potency was stronger than dipyridamole, NaNO2 and aminophylline and equalled that of papaverine and hexobendine. In guinea pig taenia coli, dilazep potentiated relaxant effects induced by adenosine and adenine nucleotides in a concentration as high as 10-8 M. The potency was stronger than that of dipyridamole. From these results, it is suggested that the potentiating effect of both adenosine and adenine nucleotides and Ca++ antagonistic effect of dilazep may play an important role in producing the coronary vasodilating effect.View full abstractDownload PDF (4677K) -
Shinobu SAKURADA, Tooru SHOJI, Kensuke KISARA1975 Volume 71 Issue 8 Pages 769-777
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSInfluence of tyramine (Ty) on behavioural changes in mice was studied and the following resuls obtained : 1) 30 min after Ty (160 μg, i.c.), brain noradrenaline and serotonin levels decreased while dopamine levels increased. 2) When Ty was injected i.c. into isocarboxazide (Iso) pretreated mice, spontaneous motor activity (SMA) measured by photo-cell counters method increased markedly but SMA by wheel cage method decreased. 3) When Ty was injected i.c. into Iso and p-chlorophenylalanine (p-CPA) (400mg/kg, i.p., daily×2) pretreated mice, SMA measured by photo-cell counters method increased. While, SMA increased from 30 to 90 min after Ty, SMA measured by wheel cage method decreased till 30 min after Ty. 4) When Ty was injected i.c. into Iso and α-methyl-ptyrosine (α-MPT) (125 mg/kg, i.p., daily × 2), SMA measured by photo-cell counters method decreased markedly when compared with Iso+saline treated group. When SMA was measured by wheel cage method, a difference between α-MPT+Iso-Ty treated group and Iso-saline group was not obtained. 5) When Ty was injected i.c. into p-CPA+α-MPT+Iso pretreated mice, SMA measured by photo-cell counters method did not show any increase compared with control group. 6) SMA produced by Iso-Ty in mice pretreated with haloperidol was significantly inhibited. A 50% dose of inhibition was seen with 0.3 mg/kg. From our results, it appears that an increase of SMA induced by Iso+Ty as revealed by the photo-cell counters method may be related to brain catecholamines and serotonin while a decrease of SMA in wheel cage method may be related to brain serotonin.View full abstractDownload PDF (3908K) -
Shinobu SAKURADA1975 Volume 71 Issue 8 Pages 779-787
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffects of drugs on head-twitches induced by tyramine (Ty) in isocarboxazide (Iso) pretreated mice were studied and the following results obtained : 1) In β-phenylethylamine derivatives, p-hydroxyamphetamine in non-treated and Iso-pretreated mice and Ty in Iso-pretreated mice produced headtwitches. 2) Injection of 5-HTP (i.c. and i.p.) into mice induced head-twitches. 3) Although headtwitches were not induced by a low dose of 5-HTP (20 mg/kg, i.p.), in Iso pretreated mice, the number of headtwitches increased markedly in the Iso-Ty treated group when Ty was injected i.c. in Iso+5-HTP (20 mg/kg) pretreated mice. 4) When Iso-Ty was injected into a-methyl-p-tyrosine pretreated mice, the number of head-twitches increased markedly compared with Iso-Ty treated group. 5) When Iso-Ty was injected into mice sustained with p-chlorophenylalanine, the number of headtwitches decreased markedly compared with the Iso-Ty treated group. 6) The number of headtwitches decreased markedly when Iso-Ty was injected into dimetotiazine pretreated mice, however the administration of Iso-Ty in haloperidol pretreated mice had no influence on head-twitches. 7) It is concluded that serotonin is the acting mediator in the heed-twitch response.View full abstractDownload PDF (3866K) -
Showa UEKI, Michihiro FUJIWARA, Kazuhide INOUE, Yasufumi KATAOKA, Nobu ...1975 Volume 71 Issue 8 Pages 789-815
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe effect of maprotiline (N-methyl-9, 10-ethanoanthracene-9(10H)-propylamine) on animal behavior was investigated in mice and rats and compared with those of amitriptyline and imipramine. Maprotiline inhibited reserpine hypothermia in mice and tetrabenazine ptosis in rats, while it potentiated the effects of methamphetamine, L-DOPA and apomorphine in mice, in a similar manner to that of amitriptyline and imipramine. Maprotiline was more potent than amitriptyline and imipramine in antagonizing haloperidol-induced catalepsy as well as in suppressing muricide induced by either olfactory bulbectomy or delta-9-tetrahydrocannabinol in rats. Maprotiline potentiated anesthesia induced by thiopental or ether in mice to a lesser degree than did amitriptyline, and failed to counteract the lethal effect of physostigmine or oxotremorine tremor in mice, indicating that this drug has no central anti-cholinergic effect. Maprotiline markedly inhibited hyperemo tionality of the rat with either septal lesions or olfactory bulb ablations, suggesting that it does have a tranquilizing effect. Inhibition of conditioned avoidance response of the rat in shuttle box and reduction of methamphetamine group toxicity with maprotiline were similar to those with amitriptyline. Maprotiline exaggerated pentetrazol convulsion, decreased muscle tone and impaired coordinated motor activity in mice to a much lesser degree than amitriptyline and imipramine. LD50 of maprotiline was approximately twice that of imipramine and three times that of amitriptyline. These results indicate that maprotiline is a new type of antidepressant, has a low toxicity and shares both potent antidepressant and some tranquilizing effect, without possessing central anticholinergic action.View full abstractDownload PDF (13626K) -
Masafumi KOBAYASHI, Toshio NOMURA, Kunio SAWA, Yoshiko WAKAMATSU, Etsu ...1975 Volume 71 Issue 8 Pages 817-822
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSInfluence of hyper-and hypothyroidism on amphetamine activity was observed by measuring the effects on hyperthermia and brain amphetamine and norepinephrine levels. Hyperthyroidism was obtained in rats injected with tri-iodothyronine 0.2mg/kg i.p. every day for 5 days. Controls were treated with the vehicle 1.0 ml/kg i.p. for the same period. On the 6th day, d-amphetamine (10 mg/ kg i.p.) was administered to the two groups of animals and the body temperature and brain amphetamine and norepinephrine contents were measured at O min, 15 min, 30 min and 60 min. Hyperthyroid rats showed a more marked hyperthermia than did the control animals. On the other hand “amphetamine-induced release of norepinephrine” of hyperthyroid rats was not so marked as in the control rats, however amphetamine levels did not differ in the two groups. Hypothyroidism was evident in the thyroidectomized rats. Controls for this group underwent a sham-operation. All animals were injected with amphetamine 21 days later. Amphetamine did not cause a hyperthermia in thyroidectomized rats. On the other hand, amphetamine levels were considerably higher than in the control rats, but the degree of norepinephrine release was comparable in the two groups.View full abstractDownload PDF (2717K) -
Hiroshi AZUMA, Tsuyako MIYAZAWA1975 Volume 71 Issue 8 Pages 823-831
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSIt has been reported that doxapram exhibits a remarkable stimulating effect on respiration in humans and various experimental animals. The present experiment was an attempt to investigate whether or not doxapram inhibits an atrial arrest induced by transmural stimulation and exogenously applied nicotine. Doxapram and dimorpholamine used as comparative agents showed transient and slightly positive responses followed by a negative one in the atrium preparation. Transmural stimulation under a condition of 30 V intensity with 0.3 msec duration at a frequency of 10 Hz for 2 sec caused an atrial arrest for about 3 sec followed by negative chronotropic and inotropic responses, and a positive one. All responses caused by transmural stimulation were hardly affected by pretreatment with doxapram at a concentration of 10-5g/ml or less, while dimorpholamine at a high concentration (10-5 g/ml) showed an inhibition of atrial arrest and following negative responses. Negative chronotropic and inotropic responses caused by an application of nicotine were significantly inhibited by pretreatment with doxapram or dimorpholamine. Both doxapram and dimorpholamine at higher concentrations also inhibited the positive responses of the atrium caused by nicotine. Neither doxapram nor dimorpholamine affected the ACh-induced responses. NA-induced responses were uneffected by pretreatment with doxapram, while the responses were slightly potentiated by dimorpholamine. The action mechanisms of doxapram and dimorpholamine are discussed.View full abstractDownload PDF (3576K) -
Kaito TSURUMI, Akira ABE, Tomohisa SHIBUYA, Hajime FUJIMURA1975 Volume 71 Issue 8 Pages 833-841
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSFrom the screening of a number of new pyrazole derivatives, the title compound, PZ-177, was selected as the most significant derivative for analgestic and anti-edematous actions. In this paper, we report the anti-edematous activity of PZ-177 as assessed by detailed analysis. PZ-177 showed a markedly inhibitory effect against rat paw edema induced by various phlogists (carrageenin, dextran, egg albumin, serotonin, formalin and bradykinin). It also inhibited edema induced by anti-rat rabbit serum. The activity of PZ-177 was more potent than that of mepirizole and the same as that of phenylbutazone. Though this agent has a central depressive effect, it is considered that the action has actually little influence on anti-edematous effect, as carrageenin-induced edema was inhibited in spinal rats. On the other hand, the anti-edematous effect of PZ-177 was reduced significantly in adrenalectomized rats. It is therefore suggested that the potent anti-edematous action of PZ-177 is exerted partially by a direct action at the inflamed site and mediated partially by stimulation of the hypophysis-adrenal system.View full abstractDownload PDF (3586K) -
Kaito TSURUMI, Isamu MORII, Masakatsu NOZAKI, Hajime FUJIMURA1975 Volume 71 Issue 8 Pages 843-856
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSWe have already reported that PZ-177 was found to have potent inhibitory activity on acute inflammatory edema. In this paper, the anti-inflammatory, analgesic and antipyretic properties of PZ-177 were assessed by a battery of standard tests. PZ-177 inhibited the increased vascular permeability induced by histamine, xylene and acetic acid. The activity was the same as the anti-edematous one and was more potent than that of mepirizole. PZ-177 did not inhibit ultraviolet erythema in guinea pigs, proliferation of granulation tissue in cotton pellet and granuloma pouch tests of rats and adjuvant arthritis in rats. Wound healing was not prolonged and the agent was weak in ulcerogenic action. PZ-177 did not affect heat denaturation of bovine serum albumin at pH 5.3, but inhibited hyperthermic hemolysis at pH 7.4 and exerted a stabilizing effect on biological membranes. This is considered to be one of the mechanisms of action. When analgesic action was tested by the writhing and Haffner's methods in mice, the compound revealed a more potent activity than did mepirizole and aminopyrine. Utilizing the Randall-Selitto's analgesic method in rats, a significant rise in pain threshold was obtained only at the inflamed foot. The antipyretic action was less than aminopyrine in febrile rabbits. From the above results, PZ-177 may be classified as a potent analgesic and anti-inflammatory agent but has no effect on proliferation of granu lation tissue and chronic inflammatory disease.View full abstractDownload PDF (6457K) -
Yutaka MARUYAMA, Michio TERASAWA, Koretake ANAMI, Yukinobu KADOBE1975 Volume 71 Issue 8 Pages 857-873
Published: 1975
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSA newly synthesized anti-inflammatory agent, Y-8004 demonstrated a greater inhibition than did indomethacin(IM). on inflammatory response such as ultraviolet erythema in guinea pigs, carrageenin edema, evans blue and carrageenin-induced pleuritis and acetic acid-induced peritonitis in rats. On the other hand, the inhibition of Y-8004 was to the same extent as IM regarding granuloma formation around cotton pellet and the development of adjuvant arthritis in rats, however, Y-8004 was only half as effective as IM regarding exudation in granuloma pouch. In addition, the agent was effective in alleviating established adjuvant arthritis, the anti-inflammatory activity was not mediated by stimulation of the adrenals, and glucocorticoid-like activity could not be demonstrated. Furthermore, analgesic and antipyretic activities were to the degree as seen with IM, and the anal gesic property of Y-8004 was considered to be peripheral as is the case with IM. The ulcerogenic activity of Y-8004 was observed to be mainly in the jejunum and ileum of the rat, but compared to IM, there were considerable differences between the ulcerogenic and the effective doses. As Y-8004 has a wider therapeutic margin than IM, this non-steroidal anti-inflammatory agent should be quite applicable for clinical purposes.View full abstractDownload PDF (7458K)
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