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Volume 77 (1981)
- Issue 6 Pages 559-
- Issue 5 Pages 447-
- Issue 4 Pages 337-
- Issue 3 Pages 231-
- Issue 2 Pages 99-
- Issue 1 Pages 1-
Volume 77, Issue 2
Displaying 1-13 of 13 articles from this issue
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Haruhiro HIGASHIDA, Naomasa MIKI1981 Volume 77 Issue 2 Pages 99-113
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThis review concerns neuropharmacological properties of clonal cells from tumors in the nervous system and muscle, and/or somatic hybrid cells derived from these clonal preparations. These cells grow well under conditions of culture and show neuronal characteristics identical to those seen in normal cells. Observations of these clonal cells contribute to studies on development, differentiation, synaptogenesis and cellular recognition in the nervous system. Analyzation of eukaryotic genes also enables investigations on genetic control mechanisms by which highly differentiated neuronal functions are expressed.View full abstractDownload PDF (8222K) -
Makoto MURAI1981 Volume 77 Issue 2 Pages 115-122
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSCholinesterase (ChE) hydrolyzing acetylcholine (ACh) in vivo can be classified into two groups. The ChE localizing in brain and erythrocytes is known as ChE and hydrolyzes ACh and acetyl-β-methylcholine (MeCh) but not benzoylcholine (BzCh). The ChE localizing in liver and serum is termed pseudo ChE and hydrolyzes ACh and BzCh but not MeCh. Effects of BzCh, a specific substrate of pseudo ChE on true ChE in brain mitochondria and erythrocytes of rabbit and rat were studied. The ChE activities in rabbit brain with ACh and MeCh as substrates were decreased to 1/4 and 1/3 of the control activities by addition of 10 mM BzCh, respectively. The pS curve for ChE in rabbit brain and erythrocytes with ACh and MeCh as substrates markedly decreased by addition of 3 mM of BzCh. The inhibitory effect of BzCh was reversible and competitive, as assessed by a Lineweaver-Burk plot method. BzCh protected the irreversible inactivating effect of true ChE by DEP. These results suggest that BzCh is not hydrolyzed by true ChE but does have an affinity for the active center of true ChE.View full abstractDownload PDF (3397K) -
Studies on anti-allergic agents (IV)Kazuhiro GOTO, Michio TERASAWA, Atsuo KOMORI, Yutaka MARUYAMA1981 Volume 77 Issue 2 Pages 123-129
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSY-12, 141 (0.1 ?? 0.3 mg/kg) given i.v. 1 min before the antigen challenge inhibited both the 48-hour passive cutaneous anaphylaxis (PCA) and active anaphylactic bronchoconstriction of rats mediated by IgE-like antibody. The anti-PCA activity of Y-12, 141 (0.3 mg/kg i.v.) given 1 min before the antigen challenge decreased significantly by predosing with Y-12, 141 (1 ?? 3 mg/kg i.v.) 60 min before the antigen challenge. The induction of tachyphylaxis in the PCA test appeared to depend on the doses and intervals between predosing and second dosing. The anti-PCA activity of disodium cromoglycate (DSCG) at a dose of 1 mg/kg i.v. decreased significantly by predosing with DSCG (10 mg/kg i.v.) 30 min before the antigen challenge. Cross -tachyphylaxis between Y-12, 141 and DSCG was observed in the PCA test. The tachyphylaxis to Y-12, 141 was more readily induced in the PCA than in the bronchoconstriction. The inhibitory activity of Y-12, 141 (0.3 mg/kg i.v.) given 1 min before the antigen challenge in the PCA and bronchoconstriction was not affected by predosing with Y-12, 141 (1 mg/kg p.o. or s.c.) for 7 days.View full abstractDownload PDF (3064K) -
Ken-ichi SASAKI, Shinobu FURUSAWA, Giichi TAKAYANAGI1981 Volume 77 Issue 2 Pages 131-139
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of butoctamide (N-(2-ethylhexyl)-3-hydroxybutyramide, L-2) on the antitumor activity of 6-mercaptopurine (6-MP) against Ehrlich solid tumors in mice were investigated. No change was observed in tumor growth after either oral or intraperitoneal administration of butoctamide (100 mg/kg/day × 7). This drug increased the activity of a low dose of 6-MP (2.5 ?? 10 mg/kg/day, i.p., × 7), but did not change the activity of a high dose of 6-MP (40 ?? 80 mg/kg/day, i.p., × 7). The antitumor activity of thioinosine (6-MP riboside) was similarly increased by administration of butoctamide (100 mg/kg/day, i.p., × 7). On the other hand, concomitant administration of butoctamide with cyclophosphamide, methotrexate, mitomycin C or adriamycin had no effect on the activity of these anticancer drugs. In butoctamide (100 mg/kg/day, i.p., × 7)-treated mice, the antitumor activities of a single administration of 6-MP and cyclophosphamide were not increased. Butoctamide stimulated the hypoxanthine-guanine phosphoribosyltransferase activity and inhibited the xanthine oxidase activity of mouse liver, to a certain degree as compared to controls. Butoctamide may promote conversion from 6-MP to thioinosinic acid monophosphate to a biologically active state, rather than to thiouric acid or hypoxanthine which would be inactive.View full abstractDownload PDF (4500K) -
Minoru YAMAMOTO, Kenichi TOMIOKA, Shiro TACHIKAWA, Hiroo MAENO1981 Volume 77 Issue 2 Pages 141-151
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSCentral pharmacological effects of YPG-209 were examined in comparison with those of PGE2(prostaglandin E2). Spontaneous motor activity and exploratory movement in mice were inhibited by oral administration of YPG-209 in a dose of 10 μg/kg. These inhibitions seemed to involve factors different from those related to the central nervous system, e.g. intestinal movement. Thiopental-induced sleeping time in mice was prolonged by oral administration of YPG-209 in a dose of 300μg/kg. On the other hand, spontaneous EEG and EEG arousal response in gallamine-immobilized cats were not affected by intravenous administration of YPG-209 in a dose of 100μg/kg. Mice taming effect, rota rod performance and drug- or electroshock-induced convulsions were not affected by oral administration of YPG-209 in a dose of 3 mg/kg. Methamphetamine-induced lethality in mice was inhibited by subcutaneous administration of YPG-209 in a dose of 5 mg/kg. Normal rectal temperature in mice was lowered by oral administration of YPG-209 in a dose of 100 μg/kg. The central pharmacological actions of PDE2 were qualitatively similar to those of YPG-209, but the potencies of central actions of PGE2 were less than those of YPG-209.View full abstractDownload PDF (5254K) -
Masako OKAZAKI, Tadashi KURIMOTO, Keiko OZAWA, Koji SAKAMOTO1981 Volume 77 Issue 2 Pages 153-164
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffect of M3, an anticancer agent, on the phagocytic activity of the mouse reticuloendothelial system was studied by the carbon clearance method. Lysosomal enzyme activities of peritoneal exudate cells solution (PECs) and peritoneal macrophage (Mp), and morphological changes of Mp were also examined. The K index (phagocytic index) was significantly increased 24 hr after the administration of M3 (250, 300 mg/kg, i.p.×3) as well as that of zymosan (Z: 50 mg/kg, i.p.×3). The time course on phagocytic activity of M3 (300 mg/kg) was also investigated. The index was increased 2, 4, and 96 hr after i.p. administration, but on i.v. administration the index was decreased at 2 and 4 hr, although increased at 72 hr. Microscopically, carbon particles were internalized by Mp of marginal zones between white and red pulp in the spleen, and in the liver, mainly by Kupffer cells. Lysosomal enzyme activities (acid phosphatase and β-glucuronidase) and cell numbers of PECs were increased as follows: Z>M3>Na2HPO4. These enzyme activities in Mp were also increased significantly 72 and 96 hr after i.p. administration. Observing of morphology by Giemsa staining, saline and Na2HPO4 groups showed round monocytes, but in the M3 and Z groups there were enlarged cells with many projections. These results suggest that M3 promotes the phagocytic activity on the reticuloendothelial system in mice and has a stimulatory effect on Mp because of the increase in the lysosomal enzyme activities and morphological changes in the cells.View full abstractDownload PDF (6901K) -
Masayuki NAKANO, Akira TAKASHIMA, Masanori NISHIUCHI, Masaharu TAKEUCH ...1981 Volume 77 Issue 2 Pages 165-176
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAs betamethasone 17, 21-dipropionate induces adrenal atrophy in rat dams and adrenal hypertrophy in the fetus, we investigated the placental transfer of this compound using autoradiography and liquid scintillation counting in animals in the late stages of pregnancy. In these two species, 3H-betamethasone 17, 21-dipropionate and/or its metabolites transferred across the placental barrier into fetal tissues and were distributed at levels lower than detected in the maternal tissues. The rat fetus showed a high uptake of radioactivity in the adrenal cortex. In pregnant rats, the ratios of the radioactivity in brain tissues to the plasma in fetuses were much higher than in the dams after the administration of 3H-betamethasone 17, 21 -dipropionate or 3H-betamethasone. In the dams given 3H-betamethasone 17, 21-dipropionate, the accumulation of radioactivity in the hypothalamus and septum was significantly greater than in other regions. The present study suggests that betamethasone 17, 21 -dipropionate or its metabolites transferred across the placental barrier following administration to the mother rat may produce an adrenal hypertrophy in the fetus and that accumulation of radioactivity in the hypothalamus of the dam may be related to a suppression of the function of hypothalamo-pituitary-adrenal axis.View full abstractDownload PDF (5667K) -
Hitoshi KONTANI, Ryozo KOSHIURA1981 Volume 77 Issue 2 Pages 177-185
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAfferent activities were recorded in vagosympathetic nerves from mechanoreceptors of the isolated heart of bullfrog. The rate of discharges was increased when Ca2+ or Mg2+ (1.1 ?? 4.4 mM) was added to normal Ringer's solution containing 1.1 mM Ca2+. In terms of increase in the rate of discharges following the addition of Ca2+ an increase in the tone of cardiac muscle at diastole was observed. The rate of discharges was decreased and thereafter abolished within 5 to 10 min by lowering Ringer's solution Ca2+ concentration from 1.1 to 0.37 mM. A high firing frequency was observed with the addition of Mg2+ (0.73 mM) in the low Caz+ Ringer's solution containing 0.37 mM Ca2+ and the rate remained unchanged for at least 15 min. On the other hand, the discharges were reduced, concentration dependently, when Mn2+(0.22 ?? 1.1 mM) was added to normal Ringer's solution. When Mn2+(0.22 or 0.55 mM) was applied, the rate of discharges decreased gradually and the reduction of discharges decreased 10 to 20 min after application. It appears that increase in the rate of discharges by application of Ca2+ in mainly the result of an increase in the tone of cardiac muscle induced by Ca2+. The presence of Ca2+ in external medium seems to be necessary to maintain the generation afferent discharges and Mg2+ can act as a substitute for Ca2+ in the generation of afferent discharges. The inhibitory effect of Mn2+ seems to be the result of depression of mechanoreceptors but the receptor becomes insensitive to Mn2+ within 10 to 20 min during exposure to low concentrations of Mn2+.View full abstractDownload PDF (4626K) -
Akira YAMASHITA, Yoichiro HAMADA, Hisakazu ISHII, Takashi NOSE1981 Volume 77 Issue 2 Pages 187-194
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAfter the administration of dehydroepiandrosterone sulfate (DHAS) (0, 10, 30, 70 mg/kg, i.v.) to rabbits during late pregnancy, serum concentration of DHAS, dehydroepiandrosterone (DHA), testosterone (T), estradiol (E2) and progesterone (Prog) were determined by radioimmunoassay. Serum levels of DHAS increased dose-dependently, and were reduced biphasically to normal levels at 24 hr after the administration. Similarly, the levels of DHA, T and E2 increased, and reached the maximum at 30 min after, though the increase of DHA or T was one-thousandth that of DHAS, and that of E2 was about one-hundred-thousandth. On the other hand, Prog concentration in sera decreased to 50 ?? 60% of that before the injection at 30 min after (p<0.05). These results suggest that the changes observed in E2 and Prog levels after the injection of DHAS into pregnant rabbits corresponded to the changes of endogeneous E2 and Prog seen in early parturition in women.View full abstractDownload PDF (3388K) -
Taku NAGAO, Sakae MURATA, Katsuo IKEZAWA, Tomihiro IKEO, Hiroshi NARIT ...1981 Volume 77 Issue 2 Pages 195-203
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of diltiazem, a calcium antagonist, on the cardiovascular system in the pentobarbital anesthetized dogs were investigated. Diltiazem (100 μg/kg and 300 μg/kg, i.v.) decreased blood pressure, heart rate and total peripheral resistance, while cardiac output and stroke volume were markedly increased. The max dp/dt of left ventricular pressure tended to increase with a dose of 100 μg/kg. Left ventricular end-diastolic pressure was slightly increased with a dose of 300 μg/kg. Rate pressure product was significantly reduced. Diltiazem (30 μg/kg and 100 μg/kg) increased pulmonary arterial flow together with the increase in both systolic and diastolic pulmonary arterial pressure. Diltiazem (100 μg/kg) increased common carotid, femoral and superior mesenteric arterial blood flow by 30 to 40%, whereas vertebral blood flow was increased by over 100%. The dose dependency in the vertebral blood flow was remarkable. Response of the vertebral artery to diltiazem was similar to that reported in the case of the coronary artery. In the His bundle electrogram, diltiazem increased the AH interval by about 10% at 100 μg/kg and 25% at 200 μg/kg, without changing the HV interval. Diltiazem-induced AH prolongation was completely depressed by epinephrine but only partially so by CaCl2. Thus, the effects of diltiazem on sinus rhythm and AV conduction in the anesthetized dog were more potent than the effects on cardiac contractility, although weaker than the effects of the vasodilating action. The vasodilator effects appear to be the primary action of diltiazem on the cardiovascular system.View full abstractDownload PDF (4167K) -
Shoichi KONDO, Mitsuo KAWADA, Nobuyuki SANO1981 Volume 77 Issue 2 Pages 205-211
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSRegional cerebral blood flow (r-CBF) in anesthetized dogs was measured by the H2 clearance method. Cerebral ischemia was induced by permanent ligation of bilateral vertebral arteries (VA) and a 10 min occlusion of bilateral common carotid arteries (CCA). Under normal conditions, dilazep (100 and 300 μg/kg i.v.) increased r-CBF dose-dependently without affecting arterial PO2, PCO2 and pH. r-CBF was reduced by 40% during cerebral ischemia. Relative r-CBF rates, as compared with pre-ischemic rates, were 85%, 80%, 77% and 75% at 30, 60, 90 and 120 min after cerebral ischemia, respectively, indicating development of recirculation impairment. Dilazep (100 and 300 μg/kg i.v. 30 min before CCA occlusion) did not affect r-CBF reduction during the state of cerebral ischemia, whereas it prevented re-circulation impairment after cerebral ischemia. Papaverine (300 μg/kg i.v. 30 min before CCA occlusion) exerted similar effects. These results suggest that dilazep is a potentially effective drug for treating cerebrovascular disorders.View full abstractDownload PDF (2900K) -
Fumio KIMURA, Junko SHIMOZAWA, Fumiko SAITO, Mari MORIKUBO, Setsuya TA ...1981 Volume 77 Issue 2 Pages 213-220
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSA new perfusion technique was applied to the rat pancreas to elucidate neural mechanisms related to insulin secretion. The pancreas and a part of the gastroduodenal tract were perfused in situ with an artificial perfusion fluid consisting of 5% of rat red blood cells, 4% bovine serum albumin and 0.1 % of glucose and Krebs-Ringer bicarbonate buffer. Stimulation (5-10V, 5 msec, 50 Hz for 5 min) to the right or bilateral cervical vagal nerves produced a significant increase in insulin activity in the perfusate. Acetylcholine (5-10 μg/0.1 ml) added to the perfusion fluid produced a dose-dependent increase in insulin activity in the perfusate, and the responses disappeared after pretreatment with atropine (100 μg/ml in perfusion fluid). After adding noradrenaline or isoproterenol (each 0.1 μg/0.1 ml) to the perfusion fluid, appreciable changes were not apparent.View full abstractDownload PDF (3835K) -
Takayuki TANI1981 Volume 77 Issue 2 Pages 221-230
Published: 1981
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSUsing spiral strips of male rabbit thoracic aortae, we examined the effect of formaldehyde (HCHO) on vascular smooth muscle. HCHO (6.6×10-4M) did not inhibit the tonic contraction induced by 25 mM K+, while inhibition was apparent with a pretreatment of HCHO in the same dose. HCHO markedly inhibited Ca2+ -induced contraction in the preparation depolarized by excess K+ in Ca2+-free media, but did not inhibit 50 mM K+-induced contraction in the preparation exposed to Ca2+-free media (EGTA deleted). In addition, HCHO did not inhibit the contraction induced by 2.2 mM Ba2+ in the preparation exposed to Ca2+-free media (added EGTA). These results suggest that HCHO inhibits the transmembrane influx of Ca2+. The contraction induced by norepinephrine (NE) was also inhibited by HCHO. High performance liquid chromatography revealed that NE was rapidly inactivated by HCHO in Krebs-bicarbonate solution at 37°C. This finding suggests that the inhibitory effect of HCHO on the contraction induced by NE is mainly due to inactivation of NE. Therefore, the relaxation of the vascular smooth muscle induced by HCHO is probably mainly related to both the inactivation of catecholamines and the inhibitory effect on transmembrane influx of Ca2+.View full abstractDownload PDF (5374K)
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