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Volume 76, Issue 1
Displaying 1-9 of 9 articles from this issue
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Susumu OTOMO, Michitada SASAJIMA, Masahiro OHZEKI, Ichiro TANAKA1980 Volume 76 Issue 1 Pages 1-13
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSD-penicillamine, an antirheumatic drug having chelating ability, was investigated for the effects on vitamin B6 and metals at doses ranging from 25 to 600 mg per kg, p.o., or in case of the highest dosing of D-penicillamine, together with s.c. administration of cupric sulfate or pyridoxine hydrochloride for 28 days in rats. The effects were compared with the actions of L and DL-penicillamine. D-Penicillamine increased urinary vitamin B6 excretion and lowered vitamin B6 levels extensively in serum and slightly in the liver. Those changes were also seen with L- and DL-penicillamine. On the other hand, D-penicillamine had no effects on the activities of serum transaminases and alkaline phosphatase and on the urinary excretion of xanthurenic acid after a tryptophan loading. D-Penicillamine, like L- and DL-penicillamine increased the urinary excretion of Cu and Zn and reduced Cu contents both in serum and liver. When Cu was given s.c. concomitantly with D-penicillamine p.o., an enhancement was seen in the effects of D-penicillamine on the urinary excretion of xanthurenic acid and body weight gain, as well as on the serum level of vitamin B6 and serum transaminase activities. Simultaneous injection of vitamin B6 With D-penicillamine produced a recovery in the lowering vitamin B6 levels induced by D-penicillamine in serum and liver and enhanced the urinary excretion of Cu, but did not influence the serum content of Cu. Thus, although the antivitamin B6 activity of D-penicillamine was demonstrated in rats, the degree was slight and was less than that seen with L- or DL-penicillamine. Moreover, the enhancing effect of Cu on the antivitamin B6 activity of D-penicillamine might be explained by the chelate formation between D-penicillamine-pyridoxal complex and Cu.View full abstractDownload PDF (13530K) -
Eiichi HAYASHI, Akihiro HARUNO, Takeshi SHIMIZU, Mamoru TERADA1980 Volume 76 Issue 1 Pages 15-24
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSTo investigate the pharmacological properties of Ascaris muscle, comparative studies were undertaken on the actions of various drugs on Ascaris muscle, guinea pig isolated ileum and frog isolated rectus preparations. In Ascaris muscle and frog isolated rectus preparations, the contractile activities with acetylcholine (ACh, 10-5 g/ml in Ascaris and 10-6 g/ml in frog rectus) and 1, 1-dimethyl-4-phenylpiperazinium (DMPP, 10-6 g/ml) were inhibited significantly and reversely by d-tubocurarine (d-Tc, 10-5 g/ml) and mecamylamine (Meca, 10-5 g/ml), and slightly by atropine (Atr, 10-4 g/ml) and hexamethonium (C6, 10-4 g/ml), In guinea pig isolated ileum preparation, the contractile activity with ACh (10-6 g/ml) was inhibited markedly and reversely by Atr (10-6 g/ml), while the activity with DMPP (10-6 g/ml) was similarly inhibited by Meca(10-6 g/ml), C6 (10-6 g/ml) and Atr (10-6 g/ml). Although frog isolated rectus preparation was contracted with 4-(m-chlorophenylcarbamoyloxy)-2-butynyltrimethylammonium (McN-A-343, 10-5 g/ml) but not with pilocarpine (10-4 g/ml), Ascaris muscle preparation was not affected by these agonists. Frog isolated rectus preparation was contracted with 5-hydroxytryptamine (5-HT, 10-4 g/ml) but was not affected by histamine (His, 10-3 g/ml) and γ-aminobutyric acid (GABA, 10-4 g/ml), whereas Ascaris muscle was contracted with His (10-3 g/ml) and relaxed with 5-HT (10-4 g/ml) and GABA (10-5 g/ml). These results suggest that Ascaris muscle as well as skeletal muscle have nicotinic receptors and that the Ascaris muscle has properties which differ specifically from skeletal muscle.View full abstractDownload PDF (11386K) -
Shigeru ISHIKAWA, Akira IIZUKA, Saizo YANAURA1980 Volume 76 Issue 1 Pages 25-32
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSMechanisms of hepatic bile secretion were studied in unanesthetized bile fistula rats. After implantation of bile fistula, bile flow and bile acids secretion were significantly decreased and secondary bile acids were greatly decreased. After cholic acid (CA) 30μM/100 g/hr infusion, bile juice was greatly increased, and CA was dramatically increased in bile. Biliary bile flow and bile acid were not increased after infusion of CDCA 30 μM/100 g/hr. CDCA was slightly increased in bile, but the amount of bile acids tended to decrease. DHCA dramatically increased the amount of bile juice, while DHCA was not detected in the bile. After DHCA infusion, 3α, 7α-dihydroxy-12-keto-5β-cholanic acid dramatically increased and slightly increased in CA. Regarding the relationship between the bile flow rate and the secretion rate of the total bile acids, bile acid-dependent bile secretion varied with the bile acid value. On the other hand, Na+ and K+ concentrations of bile were not related to bile acid concentration. These studies show that canalicular bile secretion mechanisms varied with the compositions of bile acids and bile acid secretion rate.View full abstractDownload PDF (12109K) -
Hiroo OGURA, Takashi MIKAMI, Naoko TAKAMURA, Yoshikazu SUZUKI, Tanetak ...1980 Volume 76 Issue 1 Pages 33-44
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSCytosine arabinoside (ara-C), an antiproliferative agent, was given subcutaneously to Sprauge-Dawley rats on the 2-4th postnatal day in doses of 12.5 and 25 mg/kg/day. Body weight and viability were found to be dose-dependently inhibited. The appearance of audio-startle response was delayed in the group on the high dose and up to 21 days of age, the ambulatory behavior resembled that seen in geriatric rats. The free-fall righting reflex failed to appear in the treated groups. The open field test revealed that only the treated females were hypoactive. The treated group showed a poor neuro-muscular ability in the rotarod performance and impairment of acquiring conditioned and unconditioned avoidance response in pole climbing. Histopathological and biochemical studies revealed a hypoplasia of the cerebellum. These findings are suggestive of behavioral dysfunction caused by ara-C-induced cerebellar disorders.View full abstractDownload PDF (13905K) -
Shunsuke YAMAMOTO, Yasunori HIGUCHI1980 Volume 76 Issue 1 Pages 45-49
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffect of 2-(2-fluoro-4-biphenylyl) propionic acid(Flurbiprofen, FP-70) on increased vascular permeability was studied using the potentiation of bradykinin-induced vascular permeability by prostaglandin in the guinea pig skin, as the test system. Prostaglandin E1 or E2 (1 μg/site) alone did not show increased vascular permeability but did enhance the effect of various concentrations of bradykinin when concomitantly applied, whereas prostaglandin F2α did not potentiate the effect of bradykinin on vascular permeability. Arachidonic acid (100 μg/site) had no effect on vascular permeability when injected alone or in combination with bradykinin. However, arachidonic acid enhanced the effect of bradykinin when given 30 min before bradykinin. FP-70 had no inhibitory effect on prostaglandin E1 potentiation of bradykinin-induced vascular permeability. On the other hand, FP-70 completely abolished the enhancement of the effect of bradykinin by arachidonic acid. These results strongly suggest that anti-vascular permeability action of FP-70 may be due to inhibition of prostaglandin synthetase. Indomethacin and acetylsalicylic acid also exhibit similar effects. However, the inhibitory effect of FP-70 was 12.5 and 166.7 times as potent as indomethacin and acetylsalicylic acid, respectively.View full abstractDownload PDF (5379K) -
Hideyo IMANISHI, Kozo TOMATSU, Yuji NISHIYAMA, Shinji MURATA, Hideo KA ...1980 Volume 76 Issue 1 Pages 51-58
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESS1, 1'-Heptamethylene-bis-6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline (HBDT) and 1, 1'-tetramethylene-bis-6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline (bisobrin) produced an edema when given subcutaneously into the hind paws of rats. The inhibitory effects of various antagonists on the paw edema and fibrinolysis induced by HBDT were examined in rats to determine whether chemical mediators other than histamine were involved. The relation of histamine to the fibrinolytic activity of these bis-tetrahydroisoquinoline derivatives has already been reported. Both the edema and fibrinolysis were significantly inhibited by pretreatment with promethazine, cyproheptadine or phentolamine, but not by dibenamine, propranolol, atropine, indomethacin or pyridinolcarbamate. ε-Aminocaproic acid inhibited the fibrinolytic activity completely without any effect on the paw edema. HBDT released 5-hydroxytryptamine (5-HT) along with histamine from rat peritoneal mast cells. However, the amount of released 5-HT was considerably smaller than that of histamine. These results suggested that bis-tetrahydroisoquinolines released both histamine and 5-HT and that these mediators produced paw edema and induced fibrinolysis by enhancement of plasmin production.View full abstractDownload PDF (9417K) -
Chizuko KOSEKI, Hitoshi ENDOU, Jun-ichi SUDO, Hajime SHIMADA, Fuminori ...1980 Volume 76 Issue 1 Pages 59-69
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSIntrarenal distributions of three enzymes, γ-glutamyl transpeptidase (γ-GTP), alkaline phosphatase (Al-p) and leucine aminopeptidase (LAP) were determined using six segments of nephrons. These enzymes were localized only in the proximal tubule. Intra-proximal distributions of the enzymes, however, were not uniform. The order of each enzyme activity in three segments of the proximal tubule, S1, S2 and S3 was as follows;
γ-GTP and LAP:=S2≈S3>S1
Al-p: S1≈S2≈S3
With subcutaneous administration of HgCl2 (1.0 mg/kg/day), urinary excretions of all three enzymes were increased from the 1st to the 2nd day and then decreased to the control level. However, after intraperitoneal administration of gentamicin sulfate (40 mg/kg/day), only Al-p activity in urine was significantly increased on the 1st day. Because of the lack of increasing blood levels of these enzymes after treatment, increased urinary excretions of the enzymes probably originate from the kidney, particularly the proximal tubule. The prominently increased excretion of γ-GTP and LAP after HgCl2 treatment means that HgCl2 might damage S2 and S3, because the excretory patterns of the three enzymes were similar to their distribution profiles in S2 and S3. On the other hand, the toxic action of GM may be localized in S1 portion, in which Al-p activity proved to be highest among the three enzymes.View full abstractDownload PDF (13400K) -
Shizuka HIGASHI, Hiroshi KOGO, Yoshio AIZAWA1980 Volume 76 Issue 1 Pages 71-76
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSInfluence of CD-3400, which has been developed as a new antihypertensive agent in the class of rauwolfia alkaloids, was studied and effects were compared to those seen with reserpine. A single, oral administration of CD-3400 in a dose of 50 mg/kg to female rats had no effects on ovarian estradiol levels in contrast to the significant decrease at 6 and 18 hr seen after reserpine administration. CD-3400 given in a dose of 50 mg/kg to female rats increased to a lesser degree the adrenal corticosterone level at 1 hour than did reserpine. While the serum corticosterone level in the female rats was not changed with CD-3400 administration, a large increase was detected in the case of reserpine. Administration of CD-3400 or reserpine in a dose of 100 mg/kg to male rats produced no change in the testicular testosterone level, but in both cases induced a significant decrease in the testicular estradiol levels. This inhibition was higher in the case of reserpine treatment. In addition, the serum corticosterone level in male rats treated with reserpine was higher than levels after administration of CD-3400. Our results indicate that CD-3400 exerts a weaker effect than does reserpine on gonadal and adrenal functions of boths sexes of rats.View full abstractDownload PDF (6539K) -
Mitsuru KAWAGUCHI1980 Volume 76 Issue 1 Pages 77-92
Published: 1980
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSIt has been suggested that hypothermia induced in rabbits by As2O3 3 mg/kg (i.v.) depends mostly on the blocking of the thermo-regulatory center. The relationship between hypothermia induced by As2O3 and brain monoamine levels in rabbits was investigated. To clarify the mechanism of the hypothermia, the influence of pretreatment with several agents on As2O3-induced hypothermia and on monoamine levels in the hypothalamus was examined. The core temperature was measured by inserting the thermister probe into the rectum and noradrenaline(NA), 5-hydroxytryptamine(5-HT) and 5-hydroxyindoleacetic acid(5-HIAA) levels in the hypothalamus were estimated fluorometrically. Pretreatment with p-chlorophenylalanine(PCPA), α-methyl-p-tyrosine(α-MPT) or 5-hydroxytryptophan(5-HTP) did not inhibit the hypothermia induced by As2O3 but did decrease NA levels in the hypothalamus. On the contrary, pretreatment with barbital sodium, pheniprazine, 1-DOPA and 1-tyrosine significantly inhibited the hypothermia or exhibited the hyperthermia. As2O3-induced hypothermia in rabbits was followed by a decrease in NA levels and an increase in 5-HT levels in the hypothalamus. On the other hand, when the hypothermia induced by As2O3 was inhibited by pretreatment with barbital sodium, pheniprazine, 1-DOPA and 1-tyrosine, both NA and 5-HT levels in the hypothalamus were significantly increased. These results suggest that As2O3-induced hypothermia is due to a decrease in NA levels and inhibition of the hypothermia is due to an increase in NA levels, in the rabbit hypothalamus.View full abstractDownload PDF (19856K)
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