The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Volume 36, Issue 1
Displaying 1-19 of 19 articles from this issue
  • Akira NISHIO, Shigeru ISHIGURO, Shugi MATSUMOTO, Noboru MIYAO
    1984 Volume 36 Issue 1 Pages 1-6
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    In young rats, some effects of magnesium (Mg) depletion in the diet on histamine content and histidine decarboxylase (HDC) activity in spleen were studied in comparison with those in the skin and peritoneal mast cells. In the case of the young rats fed a Mg-deficient diet (0.001 % Mg), the splenic histamine contents increased to levels about 1.3, 2.8 and 23 times as high as those in the rats fed a control diet (0.07% Mg) on the 4th, 6th and 8th day, respectively; histamine contents in the peritoneal mast cells also increased to about 1.2 and 1.8 times the control levels on the 6th and 8th day, respectively; no change was observed in histamine contents in the skin during 8 days of Mg depletion. HDC activities in the spleen of Mg-deficient rats on the 4th, 6th and 8th day increased to levels about 5.5, 15.5 and 35 times as high as the respective control values; the activities in the skin increased to about 37, 7 and 10 times the control values on the 4th, 6th and 8th day, respectively; while in the peritoneal mast cells, the activities increased to about 1.2 and 2.2 times the control values on the 6th and 8th day, respectively. On the 8th day of the Mg deficiency, some studies were made on the effects of histamine releasers on histamine contents in the spleen and peritoneal mast cells. Compound 48/80 (0.5 μg/ml) or polymyxin B (5 μg/ml) induced a release of histamine from the peritoneal mast cells, but not from the spleen cells isolated from the Mg-deficient rat in vitro. These results suggest that the effects of Mg deficiency on the spleen cells and on the mast cells were different.
    Download PDF (461K)
  • Michio KURACHI, Hironaka AIHARA
    1984 Volume 36 Issue 1 Pages 7-13
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The effects of chlorphenesin carbamate (CPC) and mephenesin on spinal neurons were investigated in spinal rats. CPC (50 mg/kg i.v.) inhibited the mono-(MSR) and poly-synaptic reflex (PSR), the latter being more susceptible than the former to CPC depression. Mephenesin also inhibited MSR and PSR, though the effects were short in duration. CPC had no effect on the dorsal root potential evoked by the stimulation of the dorsal root, while mephenesin reduced the dorsal root-dorsal root reflex. The excitability of motoneuron was reduced by the administration of CPC or mephenesin. The excitability of primary afferent terminal was unchanged by CPC, while it was inhibited by mephenesin. Neither CPC nor mephenesin influenced the field potential evoked by the dorsal root stimulation. Both CPC and mephenesin had no effect on the synaptic recovery. These results suggest that both CPC and mephenesin inhibit the firing of motoneurons by stabilizing the neuronal membrane, while mephenesin additionally suppresses the dorsal root reflex and the excitability of the primary afferent terminal. These inhibitory actions of CPC on spinal activities may contribute, at least partly, to its muscle relaxing action.
    Download PDF (466K)
  • Harlan F. HILL, Yasuo WATANABE, Takeshi SHIBUYA
    1984 Volume 36 Issue 1 Pages 15-21
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The postnatal development of 3[H] ethylketocyclazocine (EKC) binding characteristics was examined using membranes from the cerebral cortex of rats at various ages. Binding site affinity did not vary significantly between postnatal days 1 and 90. However, the apparent density of cortical binding sites increased fivefold between birth and adulthood. These results were similar to another ontogenic study of brain opiate receptor binding. Whereas EKC was equally potent as a competitor for 3[H] EKC binding in cortex from neonatal and adult rats, tifluadom was three times more potent in neonatal cortex than in adult cortex as a displacer of specific EKC binding. Brotizolam, a new thienodiazepine and a potent sedative hypnotic, also was distinctly more potent as an inhibitor of 3H-diazepam binding in neonatal rat brain cortex than in adult rat brain cortex. These results suggest that subtypes of benzodiazepine receptors, as well as some opiate receptor subtypes, exhibit different rates of postnatal development.
    Download PDF (507K)
  • Kuniko SHIMIZU
    1984 Volume 36 Issue 1 Pages 23-33
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The effect of systemically injected α1- and α2-adrenoceptor agonists and antagonists on ACTH secretion was studied in rats. Epinephrine, norepinephrine, phenylephrine, clonidine, B-HT933, and B-HT920 caused a significant and dose-related increase of the ACTH concentration in the serum. The order of median effective dose (ED50) of these drugs on ACTH secretion was as follows: epinephrine ≈ norepinephrine < B-HT920 < clonidine < phenylephrine << B-HT933. Isoproterenol, a β-adrenoceptor agonist, had no effect on ACTH secretion. ACTH secretion induced by epinephrine or phenylephrine was significantly inhibited by α-adrenoceptor antagonists, phentolamine and phenoxybenzamine. However, propranolol, a β-adrenoceptor antagonist, had no effect on ACTH secretion induced by epinephrine. Prazosin, an α1-antagonist, and yohimbine, an α2-antagonist, significantly blocked ACTH secretion induced by phenylephrine, an α1-agonist, and B-HT933, an α2-agonist, respectively. ACTH secretion induced by norepinephrine or a low dose of clonidine was inhibited by both prazosin and yohimbine. However, ACTH secretion induced by a high dose of clonidine was blocked only by prazosin. In rats with complete deafferentation of the medial basal hypothalamus (MBH), ACTH secretion induced by epinephrine, norepinephrine, and clonidine was significantly blocked, as compared with intact rats. These results suggest that both peripheral α1- and α2-adrenoceptors are involved in ACTH secretion induced by systemically injected adrenergic drugs in rats, and intact neural pathways entering the MBH are necessary for this ACTH releasing action.
    Download PDF (820K)
  • Masahiro KAWAMURA, Noboru NAKAMICHI, Nobuyuki IMAGAWA, Yoshiaki TANAKA ...
    1984 Volume 36 Issue 1 Pages 35-41
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    In primary 2-day cultured bovine adrenocortical cells, adrenaline stimulated the steroidogenesis, while the effect of adrenaline did not appear in the freshly isolated cells. Thus the primary 2-day cultured cells were used to study the effect of adrenaline on steroidogenesis. Adrenaline showed the steroidogenesis-stimulating effect at concentrations higher than 10-9 M, and the maximum effect was obtained between 10-6 M and 10-5 M in the primary 2-day cultured cells. The maximum effect of adrenaline was 50-70% of that of adrenocorticotropic hormone (ACTH). Noradrenaline, isoproterenol and phenylephrine also stimulated the steroidogenesis. However, the order of the potency was isoproterenol >> adrenaline =noradrenaline >>> phenylephrine. Propranolol and alprenolol inhibited the effect of adrenaline, but phenoxybenzamine and phentolamine did not inhibit the effect. Moreover, adrenaline stimulated the cyclic AMP production dose-dependently at concentrations higher than 10-8 M. These results suggest that there are steroidogenesis-linked adrenergic receptors in primary 2-day cultured bovine adrenocortical cell membrane and that the steroidogenesis-stimulating effect of adrenaline occurs through the β-adrenergic receptor.
    Download PDF (513K)
  • Sumio KAWATA, Yuzo MINAMI, Seiichiro TARUI, Teruyoshi MARUNAKA, Mitsuh ...
    1984 Volume 36 Issue 1 Pages 43-49
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Cytochrome P-450-dependent oxidative cleavage of 1-(tetrahydro-2-furanyl)-5-fluorouracil (FT) was investigated in a reconstituted system containing purified phenobarbital-inducible cytochrome P-450 (P-4501) or 3-methylcholanthrene-inducible cytochrome P-450 (P-4481). FT was converted into 5-fluorouracil (5-FU) in the reconstituted system, and its rate was 71 pmol 5-FU formed/min/nmol P-4501 and 45 pmol 5-FU/min/nmol P-4481. Cytochrome P-450, NADPH-cytochrome P-450 reductase and NADPH were required for 5-FU production. Inhibitors of cytochrome P-450 such as carbon monoxide and metyrapone markedly decreased the rate. FT was found to interact with the purified cytochrome P-450, causing a reverse type I spectral change. From these observations, we concluded that the hepatic microsomal cytochrome P-450-dependent mixed function oxidase system participates in the oxidative cleavage of FT.
    Download PDF (512K)
  • Kenichi MIYAMOTO, Ryozo KOSHIURA, Takaaki HASEGAWA, Nobuo KATO
    1984 Volume 36 Issue 1 Pages 51-57
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The antitumor activity of Klebsiella 03 lipopolysaccharide (KO3 LPS) isolated from the culture supernatant against S180 sarcoma, Ehrlich carcinoma, MM2 mammary carcinoma and Meth A fibrosarcoma in mice was investigated. KO3 LPS significantly prolonged the lifespan of S180-bearing ddY mice and MM2-bearing C3H/He mice by intraperitoneal pre- or postmedication at doses ranging from 0.1 to 1.0 mg/kg. The LPS also inhibited the growth of subcutaneously inoculated Ehrlich carcinoma in ddY mice and Meth A sarcoma in BALB/c mice by intraperitoneal, intravenous or intratumoral administration. The intratumoral injection of KO3 LPS was most effective and results by the intravenous and the intraperitoneal administrations followed in effectiveness, but the administration through the subcutaneous route was hardly effective. Thus, KO3 LPS was shown to have antitumor activity on both allogeneic tumors and syngeneic tumors. It was also indicated in this study that the lifeprolonging effect of KO3 LPS on S180 ascites type tumor-bearing mice was significantly minimized by pretreatment of cyclophosphamide and that the LPS did not influence the cell viability of HeLa cells, Ehrlich cells and MM2 cells in vitro. These results suggest that the antitumor activity of KO3 LPS is provided by host-mediated actions.
    Download PDF (466K)
  • Kazuko AOKI, Midori KAJIWARA, Tetsuo OKA
    1984 Volume 36 Issue 1 Pages 59-65
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The role of each enkephalin-hydrolyzing peptidase in the inhibitory potency of exogenously added enkephalins in the myenteric plexus-longitudinal muscle preparation of guinea-pig ileum was studied by using the relatively specific inhibitor of each enzyme. Results showed that three distinct enzymes, bestatin-sensitive aminopeptidase(s), angiotensin converting enzyme, and thiorphan-sensitive "enkephalinase", played a critical role in the inactivation of enkephalins. Additionally, these enzymes are likely to be located close to opioid receptors, since they produce a significant concentration difference of enkephalin between the surrounding organ bath and the vicinity of opioid receptors. In contrast to these three enzymes, both L-tyrosyl-L-tyrosine-sensitive dipeptidyl aminopeptidase and D-phenylalanine-sensitive carboxypeptidase are indicated not to be involved significantly in the degradation of exogenously added enkephalins in the guinea-pig ileum.
    Download PDF (487K)
  • Mineo KUNIHARA, Miyuki KANBAYASHI, Takao OHSHIMA
    1984 Volume 36 Issue 1 Pages 67-75
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The present study was undertaken to investigate the relationships between morphine-induced feeding and the adrenal functions. Morphine (5 mg/kg) was intraperitoneally administered at 10:45 (light period) or 18:45 (dark period). The orectic effects of morphine during the light period in normal rats were not influenced by adrenalectomy; however, the anorectic effects during the dark period in normal rats were attenuated by both adrenalectomy and adrenodemedullation. Corticosterone (10 mg/kg) itself had no effects on feeding during the light and dark period. Morphine did not alter blood insulin levels during the light period, but markedly decreased it during the dark period independently of feeding. These results show that morphine has two different effects on feeding by administration time, and they suggest that the adrenal affects morphine-induced feeding only during the dark period (hungry state), presumably through insulin release, but not during the light period (satiated state).
    Download PDF (647K)
  • Takayoshi HIDAKA, Kazunori HOSOE, Yutaka ARIKI, Kazuyuki TAKEO, Toshia ...
    1984 Volume 36 Issue 1 Pages 77-85
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    The pharmacological effects of a new anti-inflammatory compound, α-(3, 5-di-tert-butyl-4-hydroxybenzylidene)-γ-butyrolactone (KME-4), and its inhibitory effects on arachidonate prostaglandin synthetase and 5-lipoxygenase activities were examined. KME-4 showed anti-inflammatory activity. It was less active than indomethacin, but more active than naproxen and ibuprofen in carrageenin-induced paw edema in rats; and it was less active than indomethacin, equipotent as naproxen, but more active than ibuprofen in granuloma formation in rats. The ulcerogenic activity of KME-4 was weaker than indomethacin and naproxen, but stronger than ibuprofen in starved rats. The ratio of UD50 stomach to ED30 carrageenin edema or to ED25 granuloma for KME-4 showed higher values than those of the reference drugs. KME-4 showed antipyretic activity in yeast-induced fever in rats. It also inhibited platelet aggregation induced by arachidonic acid and protected rabbits from arachidonic acid-induced death. Furthermore, KME-4 was found to be equipotent in inhibiting both prostaglandin synthetase and 5-lipoxygenase activities of rat basophilic leukemia cells, unlike indomethacin, naproxen and ibuprofen. It also inhibited the prostaglandin synthetase activity of bovine seminal vesicle. The present findings indicate that KME-4 may be a new type of anti-inflammatory drug with dual prostaglandin synthetase and 5-lipoxygenase inhibition.
    Download PDF (635K)
  • Makoto MURAMATSU, Makoto TANAKA, Atsuko FUJITA, Susumu OTOMO, Hironaka ...
    1984 Volume 36 Issue 1 Pages 87-95
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Glucocorticoid binding to cytoplasmic and nuclear fractions and glucocorticoid-receptor complex binding to the nuclear fraction were investigated using rat liver. The glucocorticoid-receptor complex binding to the nuclear fraction was temperature-dependent, saturable, small in amount and of high affinity. The affinity and number of the glucocorticoid-receptor complex binding to the nuclear fraction were altered according to the glucocorticoid. Both the Bmax of nuclear glucocorticoid-receptor complex binding and the affinity of glucocorticoid to the cytoplasmic fraction were correlated with the relative anti-inflammatory potencies of glucocorticoids reported by Hynes and Murad (1980) and Fried et al. (1958). These results suggest that the number of nuclear binding sites of the glucocorticoid-receptor complex depends on the ligand steroid which is bound to the receptor of the cytoplasmic fraction and may be involved in physiological and pharmacological potencies of the glucocorticoid in addition to the affinity of the glucocorticoid to the receptor.
    Download PDF (663K)
  • Hitoshi HOUCHI, Hideyuki NAKAGAWA, Motoo OKA, Joe WATANABE, Minoru ISO ...
    1984 Volume 36 Issue 1 Pages 97-99
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (182K)
  • Atsushi MIYAMOTO, Hideyo OHSHIKA
    1984 Volume 36 Issue 1 Pages 100-103
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (264K)
  • Yasuo IMAI, Kihachi SAITO, Sadaaki MAEDA, Reizo INOKI, Hiroshi TAKAHAS ...
    1984 Volume 36 Issue 1 Pages 104-106
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (175K)
  • Haruo TAKEMURA
    1984 Volume 36 Issue 1 Pages 107-109
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (251K)
  • Hiroaki FURUTA, Takako YAMANE, Katsumi SUGIYAMA
    1984 Volume 36 Issue 1 Pages 110-113
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (235K)
  • Minoru HIRATA, Hiroshi FUKUI, Norio SHIMAMOTO
    1984 Volume 36 Issue 1 Pages 114-117
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (307K)
  • Takao KUBO, Yoshimi MISU
    1984 Volume 36 Issue 1 Pages 118-120
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (212K)
  • Youichi KUREBAYASHI, Masahide ASANO, Takeshi HASHIZUME, Akira AKASHI
    1984 Volume 36 Issue 1 Pages 121-123
    Published: 1984
    Released on J-STAGE: November 07, 2006
    JOURNAL FREE ACCESS
    Download PDF (203K)
feedback
Top