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Volume 73, Issue 4
Displaying 1-12 of 12 articles from this issue
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Tohru SHOJI, Takeshi TADANO, Kensuke KISARA1977 Volume 73 Issue 4 Pages 371-378
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe present experiments were undertaken to investigate the effects of Ro4-4602 plus L-Dopa on biphasic action induced by metaraminol (MA) in mice. The following results were obtained: Spontaneous motor activity (SMA) suppressed by MA was recoverd by pretreatment of Ro4-4602 plus L-Dopa and increased by more than 100 mg/kg of L-Dopa. However, SMA was increased by more than 400 mg/kg of L-Dopa in saline pretreated mice. In MA pretreated mice, SMA by L-Dopa markedly increased in proportion to the doses of MA. The peak time of SMA by L-Dopa in MA pretreated mice was observed to be faster than that in saline pretreated mice. When L-Dopa was injected into MA and saline pretreated mice, there was no significant difference of brain dopamine content between the two groups. From the above results, it is considered that the enhanced effect of L-Dopa in MA pretreated mice may be due to production of a supersensitivity to catecholamines in the central nervous system. MA induced hyper-motor activity was enhanced by pretreatment of Ro4-4602 plus L-Dopa which have no influence on SMA.View full abstractDownload PDF (3631K) -
Azuma YAMAGUCHI1977 Volume 73 Issue 4 Pages 379-399
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe effects of anti-inflammatory drugs on systemic responses (SR) were measured to determine whether or not the activity, mode of action and features of anti-inflammatory drugs can be distinguished. Items of measurement were body and organ weights, hematological and serum biochemical tests and local swelling. Local swelling was inhibited not only by the drugs effective for chronic inflammatory disease (DECI), but also by basic non-steroidal anti-inflammatory drugs, tranquilizers, a diuretic, a poison and a counter irritant. Decrease in serum albumin and turbidity, and increase of serum lysozyme activity and total polysaccharide protein ratio were markedly improved only by DECI while increase of total serum polysaccharide and mucoprotein polysaccharide was improved by both DECI and a counter irritant. Acceleration of ESR was also improved by DECI, a counter irritant and a poison. Basic non-steroidal anti-inflammatory drugs and other miscellaneous drugs had no beneficial effects on the above mentioned SR. Changes of other parameters (hemoglobin, hematocrit, serum Cu, Fe, ECLT and organ weights) were not uniformly improved even by DECI. These results indicate that the most sensitive and reliable parameters for evaluation of DECI are the behaviour of the serum albumin, turbidity, lysozyme activity and total polysaccharide protein ratio. Therefore, these parameters should be incorporated as standard procedures in laboratories investigating new DECI.View full abstractDownload PDF (10553K) -
(1) Effects of β-blocking agentsHiromi IIZUKA, Yoshito NAKAGAWA, Issei MATSUBARA, Shoichi IMAI, Tomoji ...1977 Volume 73 Issue 4 Pages 401-409
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSβ-Blocking actions of orally administered Kö 1400 and tiprenolol, new β-blocking agents, were studied in unanesthetized rats and dogs, using a fall of blood pressure and an increase in heart rate produced by isoproterenol as a measure of β-receptor activation. Blood pressure was recorded from the aorta of the dog and the caudal artery of rat via indwelling catheter, and heart rate of the dog was recorded by a cardiotachometer triggered by R waves of the lead II electrocardiogram. Mean resting blood pressure was 116 mmHg in rats and 93 mmHg in dogs, and heart rate was 99 beats/min in dogs. Isoproterenol (0.5 μg/kg) was injected via indwelling venous catheter. Kö 1400, tiprenolol and propranolol inhibited the hypotension and tachycardia induced by isoproterenol at an oral dose level of 2 mg/kg or more. β-Blocking action in these preparations was found to be tiprenolol>Kö 1400>propranolol. Pharmacological half life of tiprenolol was longer than that of propranolol, whereas that of Kö 1400 was shorter. No selectivity of β-blocking actions was observed with all three β-blockers. These findings are in agreement with the results obtained in isolated atrial and tracheal preparations of the guinea pig.View full abstractDownload PDF (4262K) -
Yoshito NAKAGAWA, Keisuke TAKEDA, Yumi KATANO, Tokumasa TSUKADA, Issei ...1977 Volume 73 Issue 4 Pages 411-421
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSUsing the canine heart-lung preparation supported by a donor, effects of a new adrenergic β-blocking agent, dl-1-(tert. butylamino)-3-[(2-propinyloxy) phenoxy]-2-propanol hydrochloride (Kö 1400), on cardiac function, myocardial metabolism, and coronary circulation were studied and compared with those of propranolol. Effects of this substance on the peripheral vascular bed were also studied in the perfused hindlimb preparation of the dog. Kö 1400 produced a positive inotropic and chronotropic effect. Mechanical efficiency of the heart improved after Kö 1400, while it lessened after propranolol. A decrease in the coronary flow was observed in association with a slight increase in myocardial O2 consumption, indicating that the substance exerted a direct constrictive effect on the coronary vasculature. As a β-blocker, Kö 1400 was found to be 2-3 times more effective than propranolol. The uptake of the free fatty acid (FFA) by the heart was increased by Kö 1400 and the myocardial redox potential improved. In the perfused hindlimb preparation, intraarterial injection of Kö 1400 resulted in a transient increase of the femcral blood flow for a decrease in the flow followed by a sustained decrease. With repeated administration a marked tachyphylaxis was observed.View full abstractDownload PDF (4692K) -
Akira NOMURA1977 Volume 73 Issue 4 Pages 423-435
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSSulfhemoglobin (SHb) and methemoglobin (MHb) formations by various aniline derivatives were examined by a single and three consecutive intraperitoneal administrations to mice. It was found that with a single administration, methemoglobinemia was induced by aniline, 2-methylaniline, 3-methylaniline, 4-methylaniline, 3-trifluoromethylaniline (3-TFMA), 4-trifluoromethylaniline (4-TFMA), 2, 3-dichloroaniline, 2-aminophenol, acetanilide (AA), 2-hydroxyacetanilide, N-methylaniline (NMA), N, N-dimethylaniline (NDMA), N-ethylaniline (NEA) and N, N-diethylaniline, and was not observed with 2, 3-dimethylanilnie, 2-trifluoromethylaniline, 3-aminophenol, 4-aminophenol, 2, 6-dichloroaniline, 3-hydroxyacetanilide (3-HAA), 4-hydroxyacetanilide (4-HAA), 2-aminobenzoic acid, 3-aminobenzoic acid, 4-aminobenzoic acid and 4-chloro-2-aminobenzoic acid. On the other hand, sulfhemoglobinemia which appeared much more delayed than MHb, with a single administration, was found to be induced by 3-TFMA, 4-TFMA and NMA. Furthermore, with three consecutive administrations, such was induced by AA, 3-HAA, NDMA and NEA even though SHb was not demonstrated with a single administration. Structure-SHb and MHb forming property relationships were discussed.View full abstractDownload PDF (5554K) -
Toshiro TSUCHIYA, Hideaki FUKUSHIMA1977 Volume 73 Issue 4 Pages 437-447
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSID-690 was given at doses over 0.3 mg/kg, and increase in state of arousal and decrease in state of slow wave sleep were observed. Nitrazepam at doses over 1.0 mg/kg revealed similar effects. These agents increased incidences of paradoxical sleep at a low dose of 0.03 mg/kg. When ID-690 was given at doses over 0.3 mg/kg, the number and duration of incidences of paradoxical sleep decreased. Nitrazepam at doses over 0.1 mg/kg had a similar depressive effect on paradoxical sleep. These results suggest that these benzodiazepines have, dose-dependently, both facilitative and depressive actions on paradoxical sleep, and that the dose of these agents which affects arousal is not always the same as that which affects paradoxical sleep.View full abstractDownload PDF (4173K) -
Shuji AMAN1977 Volume 73 Issue 4 Pages 449-456
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSMAO activity decreased with increase in the concentration of sodium cholate when either tyramine or benzylamine was used as substrate and this activity was inhibited completely with 50 mM sodium cholate. Sodium cholate had no effect on MAO activity in rabbit serum. The pH optimum and pS maximum for tyramine were not changed when 10mM sodium cholate was added, while when benzylamine served as substrate inhibition with an excess of the substrate concentration occurred. Addition of 50 mM sodium cholate caused a complete inhibition of MAO activities with tyramine and benzylamine as substrates before dialysis and 45% and 75% after dialysis, respectively. Sodium cholate acted as an uncompetitive inhibitor for tyramine and benzylamine oxidation. After addition of various concentrations of sodium cholate to the mitochondria, the mixtures were centrifuged and MAO activities were measured in the supernatant and precipitate fractions. With increase in the concentration of sodium cholate, MAO activities in the supernatant increased and those in the precipitate decreased. When 50 mM sodium cholate was added, 50% of the activities were found in each fraction with tyramine as substrate, while when benzylamine was used as substrate, a 35% activity in the supernatant and a 65 % activity in the precipitate fractions were noted. Substrate specificities for MAO activity in the supernatant and precipitate treated with 50 mM sodium cholate were quite similar to specificities in the mitochondria. However, when 2.5 mM sodium cholate was used to treat the mitochondria, MAO activities in the precipitate with serotonin and tryptamine as substrates were increased to over control values.View full abstractDownload PDF (3440K) -
Kimikazu ITAYA, Jiosuke KIYONAGA, Muneyoshi ISHIKAWA, Kazutaka MIZUTA1977 Volume 73 Issue 4 Pages 457-463
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSIn the course of investigations of γ-oryzanol in rats, circadian rhythms in antiulcerogenic action on γ-oryzanol were observed. Circadian rhythms in several other parameters were investigated and correlated with the antiulcerogenic action. Pretreatment of rats with γ-oryzanol 100 mg/kg, s.c., for 5 days tended to decrease serum gastrin levels and gastric secretion, and to increase serum 11-OHCS. Suppresive patterns of serum gastrin and gastric secretion following the pretreatment with γ-oryzanol corresponded to the circadian rhythms in antiulcerogenic action of r-oryzanol. A compilation of our results suggests that increment of catecholamines in rat brain after γ-oryzanol plays a role in the abovementioned actions.View full abstractDownload PDF (3468K) -
Michitada SASAJIMA, Yasuo TARUMOTO, Hironaka AIHARA, Yoshiharu TANAKA, ...1977 Volume 73 Issue 4 Pages 465-477
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSPhysical dependence liability of chlorphenesin carbamate (CPC) was studied in parallel with phenobarbital-Na (PB). Beagle dogs were used and the overall duration of the experiment was 85 days, i.e. the first dosing period was 42 days (6 weeks) in which drugs were repeatedly administered orally once daily, followed by a withdrawal period (7 days), the second dosing period was continued from the 50th-78th day in which the form and schedule of drug administration was as in the first dosing period. The last 79th to 85th days were used for substitution experiments. In both dosing periods, PB but not CPC showed signs of tolerance formation. Severe withdrawal syndrome was observed in PB administered dogs whereas there were no changes of behavior observed in CPC-dogs by withdrawal and substitution procedures, respectively. CPC apparently does not have a physical dependence liability.View full abstractDownload PDF (4966K) -
Shigenori WATANABE, Hiroaki ARAKI, Hiromu KAWASAKI, Showa UEKI1977 Volume 73 Issue 4 Pages 479-496
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSElectroencephalographic (EEG) effects of chlorphenesin carbamate were investigated in rabbits with chronic electrode implants, and compared with those of chlormezanone and methocarbamol. Chlorphenesin carbamate (50 mg/kg i.v., 100 mg/kg i.d.) induced a drowsy pattern of spontaneous EEG consisting of high voltage slow waves in the cortex and amygdala, and desynchronization of hippocampal theta waves. Chlormezanone also elicited similar EEG changes but such were much more potent than chlorphenesin carbamate. Methocarbamol showed no effect on spontaneous EEG. Chlorphenesin carbamate caused sedation in this period and muscle relaxation was more potent than that of chlormezanone. The EEG arousal response to auditory stimulation and to electric stimulation of the posterior hypothalamus, centromedian thalamus and mesencephalic reticular formation was slightly depressed by chlorphenesin carbamate. Chlorphenesin carbamate, as with chlormezanone, markedly depressed the limbic afterdischarges elicited by hippocampal stimulation. These EEG effects of chlorphenesin carbamate were qualitatively similar to but much weaker than those of chlormezanone, whereas the muscle relaxant effect of chlorphenesin carbamate was more potent than that of chlormezanone.View full abstractDownload PDF (8189K) -
Kenji YAMADA, Yoshio AIZAWA1977 Volume 73 Issue 4 Pages 497-500
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffects of prostaglandin(PG)s on phospholipid metabolism in cotton pellet granuloma were studied. Fifty ng of PGE2 or PGF2α was injected twice a day for 3 days into cotton pellet which was implanted into the interscapular region of rats. Phospholipid content in granuloma tissue treated with PGE2 was about 3 times that of control. The incorporation of 32P-orthophosphate into phosphatidylcholine in granuloma treated with PGE2 was about 6 times that of control. The incorporation of 32P-orthophosphate into phosphatidylethanolamine was increased by PGF2α but not by PGE2. These results suggest that PGE2 and PGF2α have a different site of action in the proliferative inflammatory process.View full abstractDownload PDF (1748K) -
Motohiko UEDA, Shoichi MATSUMURA, Saburo MATSUDA, Masaru KAWAKAMI, Eii ...1977 Volume 73 Issue 4 Pages 501-516
Published: 1977
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSDobutamine (DOB) showed a dose dependent positive intropic effect on the right ventricular muscle of vagotomized Beagle dogs under pentobarbital anesthesia. Positive inotropic effects of other catecholamines (CA) decreased in the following order; isoproterenol (Iso, 115)>norepinephrine (NE, 15)>DOB (1)> dopamine (DA, 0.36). Brachiocephalic arterial flow was also increased by DOB with a positive inotropic effect in the right ventricular muscle. Though the positive inotropic effect of DOB was slightly decreased by pretreatment with phenoxybenzamine, such was almost completely antagonized by propranolol. Contractions of isolated cat papillary muscle driven by electrical stimulation (12 beats/min) were increased by CA in the following order; Iso (17)>NE (3)>epinephrine (2.5) >DOB (1)>DA (1>). Activity of DOB to induce spontaneous contractions of papillary muscle was weakest among these CA. To determine the arrhythmogenic effect of these CA, coronary ligated Beagle dogs were employed, in which the anterior descending branch of the left coronary artery was ligated. Arrhythmogenic activity of DOB was weaker than other CA employed both in early stages and 48 hr after coronary ligation. DOB shows good potential for treating acute cardiac insufficiency and cardiogenic shock, as effects on heart rate and blood pressure are weaker.View full abstractDownload PDF (6596K)
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