Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 79, Issue 1
Displaying 1-7 of 7 articles from this issue
  • Yushi ITO
    1982 Volume 79 Issue 1 Pages 1-14
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    In addition to the negative feedback control of transmitter release exterted by the neurotransmitter itself, there are also other substances which may play a modulatory role in autonomic neuro-effector transmissions. Prostaglandins (PGs) belong to this class of substances. This review highlights the action of PGs and indomethacin on adrenergic and cholinergic neuro-effector transmissions in the guinea-pig vas deferens and dog trachea. In the guinea-pig vas deferens, low concentrations of the PGE series markedly suppressed the amplitude of e.j.p. without affecting the membrane potential, input membrane resistance or sensitivity of the smooth muscle cells to noradrenaline. [Ca]0 appeared to counteract the inhibitory action of PGs on the amplitude of e.j.p., indicating that low concentrations of PGs interact with [Ca]0 at the activated nerve terminals. Endogenous PGs may not play, however, a physiological role in the regulation of noradrenaline release, since indomethacin had no effect on the e.j.p. On the contrary, gradual and continuous reduction in the amplitude of e.j.ps was abolished by indomethacin in the dog trachea and e.j.ps with a constant amplitude were recorded. Low concentrations of PGs markedly reduced the amplitude of e.j.ps without affecting membrane properties of the smooth muscle cells. When indomethacin in repeated doses was given, spontaneous coughing and wheezing occurred in half the number of dogs. Endogenous PGs, therefore, probably play an important role in the negative feedback regulation of transmitter release from the cholinergic nerve terminals, in the dog trachea. Topical and species differences in the modulatory role of PGs was discussed.
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  • Kimiichiro MATSUMOTO, Takeshi TSUDA, Toshitaka SAKAI, Masami TSUBOSHIM ...
    1982 Volume 79 Issue 1 Pages 15-22
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    Effects of ONO-802 on maintenance of pregnancy, luteal function and ovulation were investigated. In pregnant rats, ONO-802 given i.p. showed antinidatory, abortifacient and strong labor-inducing effects with treatment on day 2, after day 17 and on day 21 of gestation, respectively. The abortifacient effect was not apparent when treatment was given from days 4 ?? 15. PGE1 had an antinidatory effect, PGF had an abortifacient and labor-inducing effects after implantation, and PGE2 had both these effects. PGF and PGE2 showed a luteolytic effect in rats, while ONO-802, similarly to the findings with PGE1, had no such effect. In pregnant rabbits, intraperitoneal ONO-802 exhibited antinidatory and abortifacient effects after implantation. Abortifacient effects were more potent with the progression of pregnancy though relatively large doses of ONO-802 were required. A significant decrease in peripheral blood progesterone level was observed in the group on high doses but the abortifacient effect of ONO-802 did not always depend on the decreases in the levels of progesterone. In cycling, spontaneously ovulating rats, the high doses of ONO-802 suppressed spontaneous ovulation when these doses were given two at 14:30 and 15:30 on the day of proestrus. ONO-802 did not inhibit the HCG-induced ovulation and the ovulation suppressed by ONO-802 was recovered by PGE2 or HCG.
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  • Katsuhiko KOJIMA, Katsuyuki IWANO, Hideaki NISHIMURA, Akira YOSHIMURA, ...
    1982 Volume 79 Issue 1 Pages 23-32
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    Effects of TPH-3 on various experimental gastric ulcers in rats and guinea-pigs were studied and the following results were obtained. In the preventive experiments, such as the Shay's ulcer, pylorus-ligated aspirin ulcer and restraint and water immersion stress ulcer, TPH-3 (200 mg/kg i.d. or p.o.) showed a statistically significant inhibition. TPH-3 markedly inhibited the histamine-induced gastric ulcer in guinea-pigs and a dose-response relationship was obtained for doses of 12.5, 25 and 50 mg/kg p.o. TPH-3 showed the weak inhibition regarding therapy for serosa-seared gastric ulcer and the recovery process of restraint and water immersion stress ulcer in rats. TPH-3, dosing 100 mg/kg intraduodenally, significantly inhibited the gastric secretion in the pylorusligated rats. TPH-3 significantly inhibited the histamine, pentagastrin and carbachol-induced acid secretion in the stomach-perfused rats. In particular, TPH-3 showed strong sensitivity to the action of histamine. TPH-3 had no anti-ACh or anti-Hl-receptor effects.
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  • Emiko FUJII, Fujiko TSUKAHARA, Teruko NOMOTO
    1982 Volume 79 Issue 1 Pages 33-41
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    Two weeks after streptozotocin i.v. injection, changes in glucose metabolism, levels of serum and urinary calcium, magnesium and copper, and cardiovascular responses were investigated in thyroidectomized streptozotocin treated diabetic rats. These parameters were compared to those of intact rats. Serum and urinary calcium, magnesium and copper concentrations were not influenced by thyroidectomy. Glycosylated hemoglobin (HbA1) in thyroidectomized streptozotocin treated diabetic rats was higher than that in those which were thyroidectomized alone. In thyroidectomized rats that induction of hyperglycemia required a larger dose of streptozotocin than for intact rats. Norepinephrine (0.3125, 0.625, 1.25 μg/kg i.v.)-induced pressor response and ACh (0.3125, 0.625, 1.25, 2.5 μg/kg i.v.)-induced depressor responses were both reduced in streptozotocin treated diabetic rats. These reduced pressor and depressor responses tended to recover after thyroidectomy. These results suggest that hypothyroid states may partially improve glucose metabolism and cardiovascular responses in streptozotocin treated diabetic rats.
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  • Yasushi WADA, Yoshinori ETOH, Akiyoshi OHIRA, Masami TSUKAMOTO, Masaki ...
    1982 Volume 79 Issue 1 Pages 43-55
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    It has been previously reported that acemetacin (ACM), the carboxymethyl ester of indomethacin (IND), is almost completely metabolized to IND in vivo. In the present study, the anti-inflammatory effects of ACM were compared with those of IND. ACM showed inhibitory effects on vascular permeability induced by phenylquinone. ACM inhibited carrageenin, kaolin, and nystatin edema dose-dependently and the ED30 in the carrageenin edema test was 2.8 mg/kg. Inhibitory effects of ACM on carrageenin edema was not influenced by adrenalectomy or repeated administration of ACM. ACM also inhibited ultraviolet erythema at 5 mg/kg. Furthermore, ACM significantly inhibited granuloma formation at 2.5 mg/kg/day. The ED30 for the therapeutic effect on established adjuvant arthritis was 0.33 mg/kg/day. These anti-inflammatory effects of orally administered ACM were equivalent to or somewhat weaker than those of IND at an equimolar dose. Platelet aggregation was inhibited when ACM was given orally to rats and the activity of ACM was similar to that of IND. On the other hand, the effects of locally administered ACM on carrageenin and kaolin edema were markedly less potent than those of IND. In addition, inhibitory effects on prostaglandin synthesis and platelet aggregation in vitro were significantly weaker than those of IND. These results suggest that the observed anti-inflammatory effects of orally administered ACM are not due to its inherent action, but due to its metabolite, IND.
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  • Saizo YANAURA, Hiroshi TAKEDA, Miwa MISAWA
    1982 Volume 79 Issue 1 Pages 57-64
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    The effects of glyceryl guaiacolate on secretory activities of tracheal secretory cells and on behavior of mucus glycoprotein in these cells were investigated histologically and histochemically using isolated canine trachea. Following glyceryl guaiacolate treatment, the number of total glycoprotein-containing goblet cells (GC) did not change. The numbers of acid glycoprotein (AGP)-, neutral glycoprotein (NGP)-, and sulphated glycoprotein (SGP)-containing GC were also unaltered in a concentration range of 10-7 to 10-4 M. On the other hand, the acinar inner diameter of the submucosal gland (SG) and the acinar inner diameter to wall ratio significantly increased, while thickness of acinus significantly decreased with 10-6, 10-5 and 10-4M glyceryl guaiacolate. AGP and SOP contents in glandular cells markedly decreased, while the ratio of the numbers of AGP- to NGP-containing glandular cell were the same, suggesting that glyceryl guaiacolate does not change the quality of mucus glycoprotein in GC and SG. Glyceryl guaiacolate produced a marked increase in total saccharide, protein, and N-acetylhexosamine concentrations in the incubation fluid. These findings suggest that glyceryl guaiacolate has no influence on the secretory activity of GC, but markedly stimulates the activity of SG. The secretagogue effect of the agent would be ascribable to stimulation of mucus discharge, but not to stimulation of mucus synthesis.
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  • Hisamoto IKEDA
    1982 Volume 79 Issue 1 Pages 65-76
    Published: 1982
    Released on J-STAGE: March 09, 2007
    JOURNAL FREE ACCESS
    We studied the effects of prenatal treatment with phenytoin (PHT) on the functional development of the rat brain. Pregnant rats were injected with varying doses (10, 50, 100 or 200 mg/kg) of PHT on days 1-21, 1-10, 14-21 or day 15 of pregnancy. There was no significant difference in the sleeping effect of pentobarbital, ataxic effect of diazepam, or seizure effect of pentetrazol between control-F, and PHT-F1 rats. Prenatal treatment with PHT on days 1-21 of pregnancy induced a marked increase in the duration of haloperidol-induced catalepsy in the male and female F1 rats when tested once a week, beginning on the 9th week and until the 13th week after birth. Hypersensitivity to haloperidol was induced to a greater extent in females. On the other hand, prenatal treatment with PHT on days 14-21 or on day 15 of pregnancy induced a decline in the duration of haloperidol-induced catalepsy in both male and female F1 rats. There was no significant alteration in the growth of the PHT-F1 rats. However, their eye opening was accelerated. The present results suggest that prenatal exposure to phenytoin induces long-lasting alterations in the dopaminergic and/or other neurons related to the manifestation of cataleptic behavior in the rat brain.
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