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Volume 80 (1982)
- Issue 6 Pages 417-
- Issue 5 Pages 325-
- Issue 4 Pages 271-
- Issue 3 Pages 203-
- Issue 2 Pages 93-
- Issue 1 Pages 1-
Volume 80, Issue 2
Displaying 1-11 of 11 articles from this issue
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Satoru SUNANO1982 Volume 80 Issue 2 Pages 93-104
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of Mn2+ and La3+ on the excitation, contraction, ion movement, and biochemistry of smooth muscles were reviewed. Both Mn2+ and La3+ block the action potential of smooth muscles without affecting membrane resting potential. However, depolarization or hyperpolarization by these ions and slow discharges which are not affected by these ions have also been reported in some smooth muscles. Mn2+ and La3+ inhibit the spontaneous contraction and high-K-induced contracture, although these ions can also initiate slow tension development in some preparations. The drug-induced contractions are relatively insensitive to these ions. Mn2+ blocks Ca influx, and La3+ blocks both Ca influx and efflux. However, La-resistant Ca movements such as Na-Ca exchange or active Ca extrusion have also been reported. La3+ also shows effects on the movement of other ions. In biochemical experiments, La3+ shows effects on Ca movement of the membranous and microsomal fractions of smooth muscles, with variations among the smooth muscles. Thus, we should be careful of using these ions as mere Ca blockers.View full abstractDownload PDF (6962K) -
Junko MAEDA, Toshimichi TSUBOI, Buichi FUJITANI, Toshiaki KADOKAWA, Ma ...1982 Volume 80 Issue 2 Pages 105-111
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of cholesterol-loading on platelet functions were studied. Guinea-pigs were fed on a diet containing 1 % cholesterol for 1-5 months. Cholesterol-feeding caused an elevation of cholesterol content in the plasma and platelets, although the phospholipids increased only in the plasma. Enhanced platelet aggregation induced by ADP, collagen, and arachidonic acid was maintained for 5 months during cholesterol-feeding, concomitant with an increase in malondialdehyde production in platelets. Although basal levels of platelet cyclic AMP were not affected, PGE1-stimulated cyclic AMP levels were markedly decreased in platelets of cholesterol-fed animals. The same results were observed in platelets treated with theophylline. No change in the generation of PGI2-like substance by the aortic tissue occurred during 4 months of cholesterol-feeding, though a significant increase was seen after 5 months. These results suggest that the enhancement of platelet function by cholesterol-feeding is concerned with enhanced prostaglandin synthesis and suppressed adenylate cyclase activity in platelets.View full abstractDownload PDF (2839K) -
Hisashi SANO, Yoshio TOTSUKA, Taketo FURUUCHI, Kouzoh SAKAI, Noriaki K ...1982 Volume 80 Issue 2 Pages 113-124
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSIn rats given methamphetamine (MAPT, 10 mg/kg i.p.) 24 hrs-48 hrs after the long term-administration of reserpine (RE), we have previously found such “ bizarre-biting behaviour ” as persistent and bloody biting activity at their own legs and tails or those of their cage mates. The present investigation examined the effect of a blockade of the dopamine receptor in the brain on MAPT-induced “ bizarre-biting behaviour ” and hypermotility of RE-pretreated rats. Male albino Wistar rats aged 4 weeks were injected intraperitoneally with RE (1.25 mg/kg) or 0.9% saline solution (1.25 ml/kg) every two days for 13 days. Twenty-three hrs after the last injection, rats received chlorpromazine (CP, 150 μg, 250 μg, 625 μg, or 1 mg/rat) intracerebrally by Valzelli's method; and 1 hr later, MAPT (10 mg/kg i.p.) was injected. MAPT-induced hypermotility was potentiated in the RE-pretreated rats, but it was suppressed dose-dependently by CP. Stereotyped licking and biting activities of saline-pretreated rats were completely suppressed by CP at each dose given, however, the “bizarre-biting behaviour ” of RE-pretreated rats was inhibited by CP only at high doses (625 μg or 1 mg/rat). It is suggested that the MAPT-induced hypermotility of RE-pretreated rats is mediated by activation of dopamine receptor while their “bizarre-biting behaviour ” is partially related to it.View full abstractDownload PDF (6282K) -
Hideo NAKAMURA, Satoru MOTOYOSHI, Chieko IMAZU, Katsumi ISHII, Yuichi ...1982 Volume 80 Issue 2 Pages 125-135
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAnti-inflammatory, analgesic, and anti-pyretic activities of orally administered etofenamate, the diethylene glycol ester of flufenamic acid, were investigated in experimental animals. Against acetic acid-induced vascular permeability in mice and ultra-violet light-induced erythema in guinea pigs, etofenamate produced a dose related inhibition at doses of 40-320 mg/kg and 5-20 mg/kg, respectively. In rats, felt-pellet-induced granuloma formation and adjuvant-induced arthritis were significantly inhibited by repeated administration of etofenamate at doses of 20 mg/kg/day for 5 days and 40 mg/kg/day for 21 days, respectively. Etofenamate showed an inhibitory activity on the squeak response caused by flexing and extending the silver nitrate-induced arthritic joint in rats; and it produced a dose related anti-writhing activity at doses of 50-300 mg/kg and 10-80 mg/kg in mice and rats, respectively, in the acetic acid-induced writhing test. Etofenamate showed a significant anti-pyretic activity at doses of 0.2 mg/kg or more. These potencies of etofenamate were 0.5 to 1.6 times those of flufenamic acid. In particular, the anti-erythema, anti-arthritis, and anti-pyretic activities of etofenamate were approximately equivalent to or superior to those of flufenamic acid. From these results, it was suggested that etofenamate given orally, like other non-steroidal anti-inflammatory drugs, showed anti-inflammatory, analgesic, and anti-pyretic activities in experimental animals.View full abstractDownload PDF (5404K) -
Norio SHIMAMOTO, Noriko GOTO, Minoru HIRATA1982 Volume 80 Issue 2 Pages 137-145
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of CV-2619 and ubiquinone-10 (Q-10) on the energy metabolism of red blood cells (RBC) of Sprague Dawley rats were studied in the presence or absence of NaF. NaF (0.3-10 mM) dose-dependently decreased the ATP and lactate contents of the RBC. In the presence of NaF (1.5 DIM), ATP content decreased to about 30% of the control. Phosphofructokinase (PFK) was markedly activated, while glyceraldehydephosphate dehydrogenase (GAPDH) and enolase were inhibited by NaF. Thus, the decrease in ATP by NaF might be attributed to retarded glycolysis due to inhibition of the latter two enzymes. The decrease in ATP by NaF (1.5 mM) was dose-dependently inhibited by CV-2619 (0.3-30 μM). Inhibition of enolase and activation of PFK by NaF were still noted even in the presence of CV-2619. Inhibition of GAPDH by NaF, however, was released by CV-2619. Q-10 (1-100μM) did not affect the ATP levels decreased by NaF. It could be concluded that CV-2619 counteracted the NaF-induced decrease in the ATP level by accelerating the glycolytic flux through the GAPDH step, which was a rate-limiting one in the presence of NaF. Q-10, however, had no effect on the glycolytic flux.View full abstractDownload PDF (4139K) -
Mitsuru KAWAGUCHI, Shoji TSUTSUMI1982 Volume 80 Issue 2 Pages 147-154
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSIt has been reported that hypothermia induced by intravenous administration of As2O3 3 mg/kg in rabbits is due to a decrease of noradrenaline (NA) in the hypothalamus. In this paper, the roles of NA or dopamine (DA) on As2O3-induced hypothermia in rabbits were investigated. As2O3-induced hypothermia was not inhibited by pretreatment with FLA-63, a potent dopamine-β-hydroxylase inhibitor, which produces an increase of DA and a decrease of NA in rabbit brain; and it was also inhibited by pretreatment with haloperidol or pimozide, potent DA-receptor blocking agents. On the contrary, pretreatment with phenoxybenzamine or dibenamine, α-receptor blocking agents, completely inhibited these hypothermia. These findings indicated that NA took an important part in thermoregulation in rabbits and certified that DA or DA-receptors were not involved As2O3-induced hypothermia.View full abstractDownload PDF (3085K) -
Hiroko ABE, Machiko SAKAGUCHI, Shigeru ARICHI1982 Volume 80 Issue 2 Pages 155-161
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of saikosaponin d extracted from Bupleuri Radix on the antigranulomatous action of glucocorticoid were investigated in rats by the cotton pellet method. Saikosaponin d (0.1 mg/kg/day × 4 days) and dexamethasone (0.1 mg/kg/day × 4 days) reduced the weight of cotton-induced granuloma to 89.58% and 88.54% of the control, respectively. These antigranulomatous actions failed to show a significant difference from the control. However, the combined administration of saikosaponin d and dexamethasone produced a significant antigranulomatous action, namely, the decrease in the weight of granuloma to 62.5% of the control. While the combination of saikosaponin d and dexamethasone showed an inhibitory trend against the increase in serum triglyceride as induced by dexamethasone, the cholesterol level was elevated by the combination. The body weight was significantly reduced by the combined administration as compared with the group treated with dexamethasone alone, but no apparent difference existed in the adrenal and thymus weights between them.View full abstractDownload PDF (2898K) -
Hideyuki TAKENAGA, Tetsuo MAGARIBUCHI, Hajime TAMAKI1982 Volume 80 Issue 2 Pages 163-168
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of trimebutine maleate (TM-906) on the spontaneous contraction were investigated in the isolated circular smooth muscle of the antrum region of the guinea pig stomach. TM-906 dose-dependently reduced the amplitude of the regular spontaneous contraction without any marked change in its frequency and basal tension. This effect of TM-906 was also observed in the presence of phentolamine, propranolol, atropine, and tetrodotoxin. However, the inhibitory effect of TM-906 was overcome by increasing the extracellular concentration of CaCl2. On the other hand, in preparations which exhibited irregular spontaneous contraction, TM-906 regularized it, and spontaneous contraction with regular frequency and amplitude was elicited. In addition, this regularizing effect of TM-906 was also observed in the presence of atropine and tetrodotoxin. It was concluded that TM-906 has dual effects on the spontaneous contraction, reducing the amplitude of regular contraction and regularizing the irregular contraction. These effects of TM-906 may be attributed to the direct action on the smooth muscle.View full abstractDownload PDF (2793K) -
Hideo NAKAMURA, Satoru MOTOYOSHI, Yuichi YOKOYAMA, Toshiaki KADOKAWA, ...1982 Volume 80 Issue 2 Pages 169-182
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSLocal anti-inflammatory activity of etofenamate gel (5% etofenamate) was investigated in rats. Etofenamate gel (5-50 mg/paw) produced a dose related inhibition in the hind paw edema caused by carrageenin with a topical application to the inflamed paw, and its ED50-value was 33.0 mg/paw. A weak but significant inhibition was seen with an application of 50 mg/paw to the non-inflamed paw, but not with 10 mg/paw. Anti-edema activity of oral etofenamate (ED50=8.49 mg/kg) was comparable to flufenamic acid. Against the hind paw edema caused by a mixture of kaolin and carrageenin, etofenamate gel showed a significant therapeutic activity with repeated application of 10-50 mg/paw to the inflamed paw, but not with 10 mg/paw to the non-inflamed paw. Etofenamate gel (50 mg/paw/day), applied topically to the inflamed hind paw of adjuvant rats, showed a significant therapeutic activity. The potency of oral etofenamate (4-8 mg/kg/day) in adjuvant rats was comparable to flufenamic acid. No gastrointestinal ulcer was produced by a topical application of etofenamate gel (up to 1, 000 mg/rat) to the clipped skin, though oral etofenamate (40 mg/kg) produced the ulcer. From these results, it was suggested that etofenamate gel, applied to the skin of rats, showed local anti-edema activity approximately comparable to oral etofenamate, and the ratio of ulcerogenic effective to anti-edema dose of etofenamate gel was larger than that of oral etofenamate.View full abstractDownload PDF (6700K) -
Hideo NAKAMURA, Yuichi YOKOYAMA, Satoru MOTOYOSHI, Yasuhiro SETO, Kats ...1982 Volume 80 Issue 2 Pages 183-194
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAnti-inflammatory and analgesic activities of topically applied etofenamate gel (5% etofenamate) were investigated in experimental animals. Etofenamate gel showed a dose related inhibition against vascular permeability caused by histamine in mice and ultra violet light-induced erythema in guinea pigs at doses of 10-100 mg/site and 25-200 (ED50=26.6) mg/site, respectively. The erythema was not inhibited with its topical application of 100 mg/site to the skin distant from the erythema. Granuloma formation, caused by felt-pellet implantation, was inhibited in a dose dependent manner by repeated application of etofenamate gel (10-100 mg/site/day). Etofenamate gel inhibited the pain-like responses in both the arthritic joint and the edematous hind paw of rats with 50-200 mg/joint and 100 mg/paw, respectively. In these tests, the vehicle gel did not show any significant activity. The potency of etofenamate gel was stronger than that of adrenal-extracts ointment (Mobilat) and approximately comparable to indomethacin ointment (1% indomethacin) in a weight basis of formulations. Topical application of etofenamate (0.5-2 mg/ear) resulted in a dose related decrease of contact hypersensitivity to oxazolone in mice, and its activity was nearly equipotent to flufenamic acid and about one-fourth that of indomethacin. From these results, it was suggested that etofenamate gel, applied topically to the inflamed tissue, showed a certain inhibitory activity against acute and subacute-chronic inflammation and inflammatory pain-like responses.View full abstractDownload PDF (6299K) -
Tsutomu SUZUKI, Mitsuya SHIMADA, Toshio YOSHII, Isamu AKIBA, Saizo YAN ...1982 Volume 80 Issue 2 Pages 195-202
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe effects of morphine on plasma corticosterone concentration in rats were studied using the drug-admixed food method. Morphine was mixed with the powder form of rat food in concentrations of 0.5 mg/g, 1 mg/g, and 2 mg/g of food. Plasma corticosterone concentration in rats treated with morphine-admixed food increased significantly, and the increment depended on the morphine concentration of drug-admixed food. The time course change of plasma corticosterone concentration in rats treated with morphine-admixed food (1 mg/g food) for 1 week was similar to that of non-treated rats without the concentration at 9:00. The plasma corticosterone concentration of morphine-treated rats at 9:00 was significantly increased in comparison with that of non-treated rats. Furthermore, the plasma corticosterone concentration after withdrawal in morphine-treated rats increased with time, and a significant increment in corticosterone was observed at 24 hr after the withdrawal. Naloxone, injected subcutaneously into morphine-dependent rats, significantly increased plasma corticosterone concentration. Increment of plasma corticosterone concentration in rats treated with morphine-admixed food for 3 or 4 weeks was significantly different from the non-treated group. The increment of plasma corticosterone concentration after the withdrawal was in a morphine treatment period-related manner. By these results, we suggest that tolerance to the increment action in plasma corticosterone concentration of morphine does not develop for at least 4 weeks using the drug-admixed food method, and the drug-admixed food method could induce morphine dependence without disturbance of the circadian rhythm in plasma corticosterone.View full abstractDownload PDF (4150K)
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