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Volume 38 (1985)
- Issue 4 Pages 337-
- Issue 3 Pages 235-
- Issue 2 Pages 121-
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Volume 38, Issue 4
Displaying 1-18 of 18 articles from this issue
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Fumiyo TAKEDA, Hisato KITAGAWA, Hiroshi KOHEI1985 Volume 38 Issue 4 Pages 337-346
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe effects of antisecretory agents, pirenzepine, atropine and cimetidine, on gastric mucosal lesions induced in rats by ethanol, HCl (0.6 N), HCl-acidified 50% ethanol and HCl-acidified 50 mM sodium taurocholate (TCA) were comparatively studied with PGE2. The involvement of gastric acid in the formation of ethanol-induced necrosis was also studied. PGE2 and pirenzepine inhibited necrosis induced by all necrotizing agents at the non-antisecretory doses, and the cytoprotective effect of pirenzepine was not abolished by indomethacin. Atropine and cimetidine did not inhibit HCl-induced necrosis even at the antisecretory dose. Atropine and cimetidine at the antisecretory dose inhibited necrosis induced by ethanol, but did not inhibit the red streaks. The ethanol-induced necrosis was also inhibited by neutralizing intragastric H+ with Tris buffer. In gastric fistula rats, alkalinization of the lumen was observed by exposure to ethanol, but necrosis was not produced. There is a close relationship between the necrosis and intragastric acid. Thus it is assumed that gastric acid is involved in the formation of ethanol-induced necrosis. It was suggested that pirenzepine possesses cytoprotective action which is not related to endogenous PGs. On the other hand, the antiulcer actions of atropine and cimetidine may be due, in a part, to antisecretory effects.View full abstractDownload PDF (551K) -
Shinya MAEDA, Shigefumi TAKEDA, Yoshimasa MIYAMOTO, Masaki ABURADA, Ma ...1985 Volume 38 Issue 4 Pages 347-353
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe effects of gomisin A, which is a lignan component of schizandra fruits, on liver functions in various experimental liver injuries and on bile secretion in CCl4-induced liver injury were studied. Gomisin A weakly accelerated the disappearance of plasma ICG by itself at a high dose (100 mg/kg, i.p.). All of the hepatotoxic chemicals used in this study inhibited the excretion of ICG from plasma. Gomisin A showed a tendency to prevent the delays of the disappearance of plasma ICG induced by CCl4, d-galactosamine and orotic acid, but not that by ANIT. Bile flow and biliary outputs of total bile acids and electrolytes (Na+, K+, Cl- and HCO3-) were decreased in CC14-treated rats. Gomisin A maintained bile flow and biliary output of each electrolyte nearly to the level of the vehicle-treated group, but did not affect biliary output of total bile acids. These findings suggest that gomisin A possesses a liver function-facilitating property in normal and liver injured rats and that its preventive action on CCl4-induced cholestasis is due to maintaining the function of the bile acids-independent fraction.View full abstractDownload PDF (291K) -
Takaaki HASEGAWA, Michio OHTA, Nobuo KIDO, Nobuo KATO, Kenichi MIYAMOT ...1985 Volume 38 Issue 4 Pages 355-360
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe antitumor activity of the polysaccharide fraction (OPS) obtained by the acid hydrolysis of Klebsiella O3 Lipopolysaccharide (KO3 LPS) isolated from the culture supernatant of the decapsulated mutant strain LEN-1 (03: K1-) against both allogeneic tumor and syngeneic tumor systems in mice was compared with that of KO3 LPS. OPS prolonged the life span of MM2-bearing C3H/He mice by intraperitoneal (i.p.) pre- and post-treatment at the doses of 100 and 1000 mg/kg. However, large amounts of OPS were needed to show the antitumor activity as compared with KO3 LPS. OPS showed no growth inhibitory activity against Meth-A sarcoma in BALB/c mice by i.p., intravenous (i.v.) or intratumoral (i.t.) administration. When 1000 mg/kg of OPS was i.p. administered once a day for 10 days, OPS significantly inhibited the tumor growth of Sarcoma-180 solid type tumor. On the other hand, KO3 LPS significantly suppressed the growth of MethA tumor by Lt. administration at the doses of 0.3 and 1.0 mg/kg and showed complete regression in 8 and 9 out of 10 mice, respectively. In MM2 tumor, KO3 LPS also showed complete regression in all mice post-treated by i.p. administration at the dose of 1 .0 mg/kg. These results suggest that OPS has antitumor activity on the tumors used in this study, but the activity was less than that of KO3 LPS.View full abstractDownload PDF (304K) -
Kazumasa SHINOZUKA, Juei-Tang CHENG, Eiichi HAYASHI1985 Volume 38 Issue 4 Pages 361-365
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe action of adenosine on the electrically induced mechanical response of circular muscle in isolated guinea-pig ileum has been investigated. Electrical stimulation (0.1 Hz) elicited the twitch response, which was completely abolished by tetrodotoxin (0.2 μM), morphine (1 μM) and atropine (0.1 μM). Adenosine (0.1-100 μM) markedly depressed the twitch response in a concentrationdependent manner, and the concentration-depression curve for adenosine was significantly shifted to the right in the presence of theophylline (30 μM). On the other hand, the contractile responses induced by acetylcholine (1-300 μM) were not effected by adenosine at all. The present investigation suggests that the twitch response is mediated through acetylcholine released from the intramural cholinergic nerves supplying the circular muscle of guinea-pig ileum, and adenosine has an inhibitory effect on the cholinergic transmission, probably via P1-purinoceptors.View full abstractDownload PDF (249K) -
Ayako SUDO1985 Volume 38 Issue 4 Pages 367-374
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSSwimming produced a marked increase in adrenaline content, but produced no change or slight decrease in noradrenaline content in the heart, spleen and submaxillary gland of the rat. Pretreatment with desmethylimipramine abolished the swimming-induced increase in adrenaline in the three organs. It was also found that the administration of 6-hydroxydopamine caused almost complete depletion of both adrenaline and noradrenaline from these organs of control and swimmingtreated rats. Furthermore, a differential centrifugation study revealed that the microsomal fraction had the highest concentrations of both adrenaline and noradrenaline in the heart and spleen of control and stress-treated rats. These findings suggest that adrenaline, like noradrenaline, exists in sympathetic nerve endings in the peripheral organs of the rats under basal conditions, and the adrenaline contents in the nerve endings are increased under stress situations.View full abstractDownload PDF (491K) -
Ken-Ichi SAITO, Sachiko HONDA, Akihiro TOBE, Iwao YANAGIYA1985 Volume 38 Issue 4 Pages 375-380
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSEffects of bifemelane hydrochloride (MCl-2016) on acetylcholine (ACh) level in the cerebral cortex and hippocampus of rats and Mongolian gerbils were examined. In normal rats, MCI-2016 (30 mg/kg, i.p.) slightly increased ACh content in the cerebral cortex. Scopolamine (1 mg/kg, i.p.) or hypoxia (95% N2 +5% O2, 9 min) decreased ACh level and pretreatment of MCl-2016 attenuated the decrement of ACh level in the rats. ACh level in the brain of Mongolian gerbils was significantly decreased following ligation of bilateral carotid arteries. In this case, MCl-201 6 also attenuated the decrement of ACh level. These results suggest that improvement by MCl-2016 of behavioral impairment observed in the animals treated with scopolamine, hypoxia or ischemia may be, at least partly, attributed to the amelioration of decreased ACh level in the brain.View full abstractDownload PDF (344K) -
Katsuaki MATSUBARA, Akira MATSUSHITA1985 Volume 38 Issue 4 Pages 381-390
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSCaerulein (CLN), which is chemically related to cholecystokinin octapeptide (CCK-8) and produces a short-lasting pharmacological effect when administered peripherally, caused a long-lasting antagonistic effect on amphetamine (AMP) hyperactivity in rats when given in combination with haloperidol (HLP). Briefly, rats were treated with a combination of CLN (0.3-40 μg/kg, s.c.) and HLP (0.1 mg/kg, s.c.) and exposed to AMP on the first day. The animals became less sensitive to AMP for 24 hr to about 2 weeks depending on the CLN dose, according to measurements of their ambulatory activities in an open field or with an Animex activity meter at low sensitivity. Examination of the properties of this long-lasting effect revealed that: 1) in animals treated with CLN and HLP, but without AMP on the first day, the susceptibility to AMP was not influenced on the next day; 2) in substitution experiments, the antagonistic effect of CLN could be reproduced by higher doses of CCK-8 (160 μg/kg) but not by nonsulfated CLN;3) in the regimen of the treatment schedule, HLP could be replaced by chlorpromazine or sulpiride, but not by α-blocking agents like phenoxybenzamine or yohimbine; 4) apomorphine, nomifensine and tranylcypromine could not substitute for AMP. Thus, injection of CLN together with HLP and AMP on the first day might be necessary to produce the long-lasting anti-AMP effect. The possible mechanism of this CLN effect is discussed.View full abstractDownload PDF (548K) -
Junichiroh WAKASUGI, Katsuhiko TAWARA, Kazuei KATAMI, Takuya IKEDA, Mu ...1985 Volume 38 Issue 4 Pages 391-401
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe mode of action of malotilate in normalizing serum cholesterol in hypocholesterolemic rats with fatty liver was examined by determination of biosynthesis, catabolism and excretion of cholesterol. Fatty liver was produced by subcutaneous injection of CCl4 at the dose of 1 ml/kg into male rats (SLC-SD) twice a week for 3 weeks. Daily administration of malotilate (100 mg/kg) in rats with hypocholesterolemia resulted in a rapid normalization of lowered serum cholesterol. Such a recovery of cholesterol level in serum coincided in time with normalization of the decreased cholesterol level of each lipoprotein fraction, VLDL-triglycerides secretion and the decreased apolipoprotein A1 value. Histopathological improvement in liver was also confirmed by a decrease in the size of fat droplets stored within the hepatocytes. The malotilate treatment gave a tendency to facilitate hepatic cholesterol synthesis in the rats with fatty liver. Malotilate at a concentration of 0.5-2 μg/ml also stimulated cholesterol biosynthesis in cultured normal hepatocytes. The drug had the action to accelerate the catabolic excretion of 3H-labeled cholesterol into feces. These results suggest that the mode of action by which serum cholesterol is normalized in rats with fatty liver is probably due to a stimulative effect of malotilate on hepatic cholesterol synthesis and cholesterol secretion from the liver.View full abstractDownload PDF (670K) -
Hiroshi TSUCHIHASHI, Takafumi NAGATOMO1985 Volume 38 Issue 4 Pages 403-409
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe significance of carbohydrate moieties containing the β-adrenoceptor molecule in the rat brain was examined using radioligand binding assay methods. Thus, this experiment was designed to assess the effects of exoglycosidase (α-D-mannosidase and neuraminidase), endoglycosidase (endoglycosidase D and endoglycosidase H), and glycopeptidase A on the affinity of β-adrenoceptor. The main reason why five kinds of enzymes were used in the present study is that they can hydrolyze different carbohydrate molecules from cell membranes. Rat brain was used and β-adrenoceptor binding assay was carried out using 3H-dihydroalprenolol (3H-DHA) as a ligand. 3H-DHA binding to β-adrenoceptors was sensitive to very low concentration of endoglycosidase H and glycopeptidase A, thus indicating that the treatments with these enzymes of rat brain membrane appear to decrease the number of β-receptor binding sites. On the other hand, the treatment with neuraminidase, endoglycosidase H, and glycopeptidase A of the membrane induced lower values of the dissociation constant (Kd) than those of the control. α-D-mannosidase and endoglycosidase D are without effect in spite of the removal of hexose contents and total carbohydrate contents with these treatments, respectively. These results imply that complex type N-linked acidic carbohydrate chains containing neuraminic acid and high mannose type N-linked carbohydrate chains, which are hydrolyzed with endoglycosidase H and glycopeptidase A, of the rat brain membrane containing β-adrenoceptor molecules play a crucial role in the drug-receptor interaction.View full abstractDownload PDF (397K) -
Akira NISHI, Akira KARASAWA, Shigeka YOSHIKAWA, Ryoichi ISHITANI1985 Volume 38 Issue 4 Pages 411-417
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSAs a first step toward the examination of the involvement of sulphatides, phosphatidylserine and phosphatidylinositol in 5-HT receptor mechanisms, we performed [3H]5-HT binding experiments on the various reconstituted fractions with these acidic lipids. A binding assay of [3H]5-HT to these fractions was carried out by Sephadex LH20 column chromatography. Among various reconstituted fractions, only the reconstitution system with the three acidic lipids exhibited a saturable [3H]5-HT binding capacity, whereas no binding was seen with [3H]-spiperone. When the binding of [3H]5-HT to this fraction was plotted as a function of the ligand concentration, a multiple binding mode with three classes of binding components (or sites) was observed. Furthermore, the double reciprocal plot indicated that this reconstitution system had three apparent KD values of 4.7, 15 and 59 nM. The displacement studies with various compounds indicated that only a few 5-HT agonists (5-methoxytryptamine and tryptamine) and neurotransmitters (DA and ACh) inhibited the[3H]5-HT binding to this fraction, but 5-HT antagonists, LSD analogues and neuroleptics had no effect. Moreover, GTP, GDP and Gpp(NH)p clearly inhibited the[3H]5-HT binding in spite of their weak potencies, while GMP did not have any effect.View full abstractDownload PDF (369K) -
Takushi X. WATANABE, Koichiro KAWASHIMA, Hirofumi SOKABE1985 Volume 38 Issue 4 Pages 419-427
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSAntihypertensive effect of enalapril (MK-421), an orally active nonsulfhydryl-containing converting enzyme inhibitor, was examined in stroke-prone spontaneously hypertensive (SHRSP) rats. The treatment was started at 14-15 weeks of age with tail blood pressure over 240 mmHg and was continued for 11 weeks. We used captopril as the reference drug. The dose of enalapril and captopril was 10 and 30 mg/kg per day, p.o., respectively. Enalapril showed a sustained antihypertensive effect from the 1st to the 11th week of the treatment. This antihypertensive effect was substantiated by the good increase in body weight; decrease in heart weight; decrease in incidences of vascular disease, nephrosclerosis, stroke and death. Enalapril treatment also prevented the increases in urine volume, and excretion of osmotically active solutes, Na, Cl and K with age. Captopril treatment showed about the same antihypertensive effect. No side effects were seen in the enalapril or captopril treated group. The antihypertensive potency of enalapril was about 3 times more than that of captopril. Enalapril and captopril slightly increased plasma renin concentration. Urinary excretion of PGE2 was not changed by enalapril or captopril treatment. These results clearly demonstrate the efficacy of long-term treatment with enalapril to prevent development of malignant hypertensive cardiovascular disease in SHRSP rats.View full abstractDownload PDF (449K) -
Hiroshi HIGUCHI, Shuji UCHIDA, Miho MURATA, Hiroshi YOSHIDA1985 Volume 38 Issue 4 Pages 429-432
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSOrgan culture of rat vas deferens produced supersensitivity to norepinephrine and acetylcholine in contractile response without change in α1-adrenergic and muscarinic acetylcholine receptors. The development of supersensitivity was inhibited by low temperature and protein synthesis inhibitors. However, protein synthesis inhibitor had no significant effect on the receptors. These findings suggested that the supersensitivity may be induced by synthesis of protein(s) which have a stimulatory effect in a process(es) after activation of receptor to contraction.View full abstractDownload PDF (207K) -
Tadahiro SHIKIMI1985 Volume 38 Issue 4 Pages 433-435
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSBoth immunochemical and kinetic evidence suggest that the increase in aprotinin activity in the presence of heparin is not due to an increase in the active form of aprotinin, but rather to a qualitative change in the aprotinin molecule which would lead to an increase in aprotinin activity.View full abstractDownload PDF (135K) -
Shigeyuki NAKAJIMA, Motohiko UEDA1985 Volume 38 Issue 4 Pages 436-438
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe increase of the ventricular fibrillation threshold (VFT) by 711389-S, a new antiarrhythmic agent, was compared with several other antiarrhythmic drugs using both in vitro (Langendorff) and in vivo preparations of guinea-pigs. The doses of antiarrhythmic drugs for increasing VFT by 10 volts in in vitro (μg) and in vivo (mg/kg, i.v.) preparations were as follows: 711389-S: 4.2, 0.15; disopyramide: 32.6, 0.86; quinidine: 32.0, 0.57; aprindine: 7.6, 0.55; propranolol: 16.6, 0.57; and lidocaine: 20.7, 1.52. The duration of the antifibrillatory effects of 711389-S almost corresponded with those of aprindine and propranolol.View full abstractDownload PDF (182K) -
Yasuyuki FURUKAWA, Kimiaki SAEGUSA, Shigetoshi CHIBA1985 Volume 38 Issue 4 Pages 439-441
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSIn the isolated, blood-perfused dog atrium, strychnine evoked dose-dependent decreases in atrial rate and contractile force, and the negative cardiac effects were not influenced by atropine. Strychnine suppressed dose-dependently the negative chronotropic and inotropic responses to intramural parasympathetic nerve stimulation, but not the response to acetylcholine. These results suggest that strychnine has direct cardiac depressant properties and inhibits the release of acetylcholine from parasympathetic nerve terminals in isolated dog atrium.View full abstractDownload PDF (175K) -
Makoto KONDO, Hiroshi FUJIWARA, Chikako TANAKA1985 Volume 38 Issue 4 Pages 442-444
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSIn studies of the localization of the dopaminergic nerve terminals in the cervical cord of guinea pig, autoradiographic analysis of the spinal cord loaded with [3H]dopamine ([3H]DA) was done under conditions that prevented the nonspecific uptake of [3H] DA. There was specific labeling in the gray matter and a high density of [3H]DA was present in the dorsal horn (DH). Moderate labeling was observed in the neuropil in the vicinity of the central canal. There were grain concentrations in close approximation to the cell bodies of numerous neurons in the DH and to the cell bodies of a few of the motoneurons in the ventral horn (VH). These dopaminergic terminals are possibly linked to sensory transmission and somatic motor function.View full abstractDownload PDF (155K) -
Mutsumi MARUYAMA1985 Volume 38 Issue 4 Pages 445-447
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSSomatostatin and substance P (10-6-3×10-5 M) inhibited dosedependently the specific binding of [3H] [D-Ala2, Met5]enkephalinamide ([3H]-DALAMID) to rat brain membranes, by decreasing the number of binding sites. [Lys]-Vasopressin also inhibited the binding, by affecting both the number of binding sites and the affinity of receptors to [3H]DALAMID. The results indicate that somatostatin and substance P may interfere with the endorphin system by an apparently competitive manner.View full abstractDownload PDF (149K) -
Yoshio OHMIYA, Susumu FUJISAWA, Kengo NAKAI1985 Volume 38 Issue 4 Pages 448-450
Published: 1985
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSOur previous studies have indicated that a phenothiazine drug, chlorpromazine, and a tricyclic antidepressant, imipramine, are metabolized by the isolated perfused rat lungs via N-oxidation from whence their N-oxides are released into the circulation. This work was undertaken to compare the pulmonary accumulation of another pneumophilic tertiary amine drug, pyrilamine, with that of its N-oxide. Approximately 10-fold greater accumulation of pyrilamine than that of its N-oxide was observed in the mouse lung after a single pass perfusion with 40 μM of the drug for a 3 min period. The largest difference between accumulation of pyrilamine and its N-oxide was noted in the lung among the various tissue slices tested, suggesting the tissue specificity of affinity.View full abstractDownload PDF (170K)
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