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Volume 86, Issue 1
Displaying 1-9 of 9 articles from this issue
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Motohiro KUROSAWA1985 Volume 86 Issue 1 Pages 1-7
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSEvidence is presented that RBL-1 cells, which are similar to normal rat mast cells in morphology and contain IgE receptors and histamine, contain a calcium-activated, phospholipid, diacylglycerol-dependent protein kinase. This enzyme is very similar in its activation requirements to the calcium-dependent enzyme termed protein kinase C in other tissues. The enzyme is activated by Ca2+. Diolein, but not other di, mono or triglycerides, substantially increases the enzyme activity. Among various phospholipids, phosphatidylserine is the most reactive activator; phosphatidylinositol, phosphatidic acid and phosphatidylethanolamine are less effective; and phosphatidylcholine is practically inactive. The enzyme is inhibited by chlorpromazine and local anesthetics such as dibucaine, tetracaine and procaine.View full abstractDownload PDF (4919K) -
Motohiro KUROSAWA1985 Volume 86 Issue 1 Pages 9-15
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSGranules were isolated from sonicated purified rat mast cells on a Percoll gradient. The granules were shown to contain a highly active phosphatidylinositol kinase which catalyzes the formation of diphosphoinositide (DPI) from endogenous phosphatidylinositol in the granule membrane. The enzyme requires ATP and Mg2+ or Mn2+ for activity. DPI formation is almost completely dependent on MgCl2 or MnCl2, and maximal response wasobserved at 20 mM or 2 mM, respectively. The effects of the divalent cations are competitive. Ca2+, fluoride and cyclic AMP are inhibitory. The Km for ATP is 25 μM. The initial reaction is rapid, but the response ceases within a few min. The maximal response is seen at 28°C.View full abstractDownload PDF (4492K) -
Osamu IRINO, Kiyoshi SAITOH, Kazumi OHKUBO1985 Volume 86 Issue 1 Pages 17-23
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSEffects of choline salicylate, sodium salicylate, choline chloride and acetylsalicylic acid on platelet aggregation in vivo, ex vivo and in vitro in mice were studied. These drugs all inhibited adenosine diphosphate (ADP)-induced respiratory depression, which is closely related to platelet aggregation in vivo, with choline salicylate showing the strongest inhibitory effect. Choline salicylate had a tendency to reduce the mortality of animals injected intravenously with endotoxin, but the other drugs had no such effect. The inhibitory effects of these drugs on ADP-induced platelet aggregation ex vivo were in the order of choline salicylate>acetylsalicylic acid ?? sodium salicylate>choline chlorides ?? no effect, and plasma concentrations of protein-unbound salicylic acid at 1 hr after oral administration of drugs were in the order of choline salicylate>acetylsalicylic acid ?? sodium salicylate. The in vitro effects of these drugs were in the order of choline salicylate ?? sodium salicylate>choline chloride ?? acetylsalicylic acid ?? no effect. Therefore, it was considered that salicylic acid played an important role on the in vivo, ex vivo and in vitro effects of choline salicylate and that choline increased plasma concentrations of salicylic acid and consequently enhanced the in vivo and ex vivo effects of salicylic acid. Furthermore, the ex vivo effects of choline salicylate were found when ADP-induced platelet aggregation was measured with platelet-rich plasma prepared from blood collected with heparin as anti-coagulant, but not when blood was collected with citrate. Thus, the possibility that the anti-platelet actions of salicylic acid may be due to the inhibition of metabolism of extracellular calcium in platelets during ADP-induced aggregation was suggested.View full abstractDownload PDF (5692K) -
Effects on vitamin B6, metals and skin collagen in ratsHideyasu YAMAUCHI, Kouichi MORIKAWA, Mitsuaki KUWANO, Mitsushi HIKIDA, ...1985 Volume 86 Issue 1 Pages 25-33
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSN-(2-Mercapto-2-methylpropionyl)-L-cysteine (SA96), an antirheumatic agent, and the main metabolite of SA96, N-[2-methyl-2-(methylthio)propionyl]-L-cysteine (SA679), were investigated for the effects on vitamin B6 (VB6), metals and skin collagen in rats in comparison with D-penicillamine (D-Pc). SA96 had no effect on VB6 amount in serum and liver at doses of 30 mg/kg and 150 mg/kg, p.o., for 28 days, but SA96 as well as SA679 lowered the level in the liver slightly at a dose of 600 mg/kg. On the other hand, D-Pc lowered the VB6 level markedly both in serum and liver at doses of 150 mg/kg and 600 mg/kg, p.o., for 28 days. SA96, SA679 or D-Pc had no effect on urinary VB6 excretion. The degree of complexing of SA96 as well as SA679 with pyridoxal-5-phosphate in vitro was very slight as compared with D-Pc. SA96 and D-Pc increased Cu and Zn excretion in urine, decreased Cu level both in serum and liver, and increased Zn level in serum. However, the degree of these effects of SA96 on the metals was very slight as compared with D-Pc. SA96 or SA679 had no effect on skin collagen, neither soluble nor insoluble collagen, but D-Pc increased soluble collagen markedly. In addition, at a dose of 600 mg/kg, D-Pc decreased insoluble collagen. From these results, it was suggested that SA96 did not have an effect on the levels of VB6 and metals and on the fractions of skin collagen in normal rats at doses showing an anti-adjuvant arthritic effect in rats.View full abstractDownload PDF (6653K) -
Yutaka KUROGOCHI, Toshikatsu NAKASHIMA, Taizo KITA, Yasumasa NAKANISHI1985 Volume 86 Issue 1 Pages 35-39
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSMale Wistar rats, aged 4 weeks, were kept in a temperature controlled room with a 12 hr light-dark cycle and given food and water ad libitum. The nicotine-treated group of rats was given water containing nicotine, which was estimated to be 10 mg/kg/day, for 40 days. Spontaneous motor activities, drinking activities and serum corticosterone levels showed circadian rhythms characteristic of a nocturnal animal in both the control and the nicotine-treated groups. As compared to the control group, however, the nicotine-treated group showed an increase in ambulatory activities, a decrease in drinking activities and a diminution of weight gain. In comparison with diurnal variations, serum corticosterone levels and liver nicotine oxidase activities increased in the nicotine-treated group during the dark period. However, the pattern of circadian rhythms characteristic of a nocturnal animal were not altered.View full abstractDownload PDF (4237K) -
Atsufumi MANABE, Kyoko SHIRASAKI, Ikuo KAWASHIMA, Sadao NAKAYAMA, Taka ...1985 Volume 86 Issue 1 Pages 41-49
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSThe effects of antiarrhythmic drugs, aprindine, mexiletine and lidocaine, on rat erythrocytes, isolated rat hepatocytes and DPPC-liposomes were studied at various concentrations. Maximal inhibition of aprindine on the hypotonic hemolysis was observed at a concentration of 2×10-4M. In isolated rat hepatocytes, aprindine caused an increase in GOT leakage above 4×10-4M. Mexiletine and lidocaine caused a slight decrease in GOT. Only aprindine caused an increase in LDH leakage above 2×10-4M. In the relationship between the surface tension and pH conditions (pH 5.7, 7.4 and 8.0), aprindine and mexiletine indicated a depression of surface tension at a dose of 10-4M to 10-3M under all pH conditions. Lidocaine indicated a depression of surface tension at a dose of 10-4M at pH 8.0 only. Aprindine and mexiletine depressed the phase transition temperature (Tc) of DPPC-liposomes. The depression of Tc by aprindine was greater than that by mexiletine. The rank by order of surface activity was the same as that of enzyme leakage from hepatocytes, hemolysis of erythrocytes and depression of Tc in DPPC-liposomes in vitro. These results suggest that differences in membrane damage produced by antiarrhythmic drugs may by related to surface activity, which in turn may determine the extent of adsorption onto cell membranes.View full abstractDownload PDF (6303K) -
Akihiro TOBE, Mitsuo EGAWA, Ken-ichi SAITO, Noriko HASHIMOTO1985 Volume 86 Issue 1 Pages 51-60
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSEffects of MCI-2016 on SMA changes were examined under several experimental conditions (normal conditions, hypoxia and head injury). Under normal conditions, MCI-2016 showed a significant increase of SMA after single administration of 12 mg/kg, i.p. Other doses (12.5 ?? 50 mg/kg, p.o. and 3 ?? 6 mg/kg, i.p.) of MCI-2016 were without significant effect. Under the same condition, MCI-2016 produced a dose-dependent increase of SMA after repeated doses of 12.5 to 50 mg/kg, p.o. (9 ?? 10 days administrations). After 5 days repeated administration, MCI-2016 significantly improved the decreased SMA due to hypoxia (rats) at 50 to 100 mg/kg, p.o. Furthermore, the drug also improved the decreased spontaneity due to head injury (mice) at 50 to 400 mg/kg, p.o. These improving effects of MCI-2016 were superior to those of Ca-hopantenate. The SMA increasing effect of MCI-2016 (12 mg/kg, i.p.) was antagonized more strongly by phenoxybenzamine than by haloperidol. In addition, the drug was shown to be rather antagonistic to the effects of anticholinergic agents. These effects may indicate the existence of qualitative differences between MCI-2016 and methamphetamine in the SMA increasing actions. It is also suggested that MCI-2016 may exhibit the above pharmacological effects through possible activation of noradrenergic and/or cholinergic mechanisms.View full abstractDownload PDF (7315K) -
Kazunaga FUKAWA, Kazuyoshi BANDO, Yoshikazu HATANAKA, Seiichi OHBA, Hi ...1985 Volume 86 Issue 1 Pages 61-69
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSThe pharmacological actions of iprazochrome (IC) on the vascular system were studied, and the following results were obtained: 1) No death nor abnormal behaviors were observed in acute toxicity tests conducted on male and female mice and rats despite the administration of large doses of IC (10, 000 mg/kg, p.o. and 80 mg/kg, i.v., respectively). 2) IC inhibited dose-dependently platelet aggregation in vitro induced by arachidonate and ADP, whereas no effect was observed on ADP-induced respiratory depression in mice, which is closely related to platelet aggregation in vivo. 3) The antiserotonergic actions of IC on the isolated external carotid arteries and femoral arteries in dogs observed in a noncompetitive manner were found to be 1/24 to 1/65 that of methysergide. On the other hand, IC showed no inhibitory effect on the paw edema of rats in vivo induced by serotonin. 4) The inhibitory effect of IC on peritoneal dye leakage in mice was less than half that of phenylbutazone. 5) IC prevented apoplexy in stroke-prone SHR (SHRSP) without lowering the blood pressure. 6) Histological changes in the cerebrum of SHRSP were ischemic changes such as swelling of the neurons and shrinkage of the nuclei, mainly in the cerebral cortex and corpus striatum area.View full abstractDownload PDF (7434K) -
Hideji MORISHITA, Kazushi KUSHIKU, Tatsuo FURUKAWA, Yoshio YAMAKI, Mas ...1985 Volume 86 Issue 1 Pages 71-85
Published: 1985
Released on J-STAGE: March 02, 2007
JOURNAL FREE ACCESSPharmacodynamic effects of ethyl 7-chloro-2, 3-dihydro-5-(2-fluorophenyl)-2-oxo-1H-1, 4-benzodiazepine-3-carboxylate (CM6912), a new benzodiazepine derivative, and its main metabolites (CM6913=M1, CM7116=M2) on the peripheral systems were investigated in several species of animals. 1) In pentobarbital-anesthetized rabbits, CM6912 and M2 (1 or 5 mg/kg, i.v.) had little effect on blood pressure, heart rate and ECG, but it slightly reduced the respiration rate. M1 decreased the heart rate without affecting respiration, blood pressure and ECG. In conscious rabbits, CM6912 and M2 (1 mg/kg, i.v.) did not affect respiration, blood pressure, heart rate and ECG, but M1 (1 mg/kg, i.v.) increased the heart rate. CM6912 (5 or 30 mg/kg), when administered orally, also increased heart rate. In pentobarbital-anesthetized dogs, CM6912 and its metabolites (5 mg/kg, i.v.) decreased respiration and heart rate without affecting blood pressure and ECG. 2) CM 6912 (5 mg/kg, i.v.) did not affect cardiovascular responses to the carotid occlusion, vagus stimulation, and pre and post-ganglionic stimulation of cardiac ganglion in anesthetized dogs. 3) CM6912 and its metabolites affected neither the spontaneous contraction nor the heart rate of isolated rabbit atria. These compounds also had no action on isolated aortic strips from rabbits. 4) CM6912 and its metabolites did not affect the muscle tone of isolated guinea pig intestine, and it had no effects on the contractile responses to acetylcholine, histamine, serotonin and barium chloride. In isolated rabbit intestine, CM 6912 and M2 slightly reduced the amplitude of contraction, while M1 had no effect. CM 6912 and its metabolites did not affect the spontaneous motility of isolated non-pregnant and pregnant rat uteri as well as in situ non-pregnant rat uterus and isolated guinea pig vas deferens, including the contractile response to adrenaline. CM6912 and M2 relaxed isolated guinea pig trachea strips only at high concentrations. 5) CM6912 and its metabolites did not affect the contractile responses of isolated rat diaphragm to electrical stimulation of the phrenic nerve. 6) CM6912 (2 or 10 mg/kg, p.o.) did not affect the rat renal and hepatic functions. 7) CM 6912 influenced neither blood coagulation in rabbits nor blood hemolysis in rats. 8) CM6912 and its metabolites did not affect the pupil size and its light reflex, and they did not produce a local anesthesia and edema. The present results suggest that CM 6912 and its main metabolites exert only slight effects on the peripheral systems in animals.View full abstractDownload PDF (10920K)
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