Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 89, Issue 2
Displaying 1-5 of 5 articles from this issue
  • Tadayuki SAITO, Noriyasu NISHIMURA, Shigeru TAJIMA, Toshikazu FUKUDA, ...
    1987 Volume 89 Issue 2 Pages 55-62
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    The effects of KB-2413 on four types of allergic reactions classified by Coombs and Gell were investigated. KB-2413 inhibited homologous passive cutaneous anaphylaxis and passive anaphylactic bronchoconstriction in guinea pigs mediated by IgE-like antibody, and ED50 values were 0.0017 mg/kg, p.o., and 0.022 mg/kg, p.o., respectively. KB-2413 also inhibited IgG-mediated anaphylactic bronchoconstriction in guinea pigs actively sensitized with egg albumin. Both complement-dependent immune hemolysis and complement-independent hypotonic hemolysis were inhibited by KB-2413 in a concentration-dependent manner. KB-2413 had no effect on the Forssman systemic reaction. The passive Arthus reaction in guinea pigs sensitized with anti-egg albumin rabbit serum was unaffected by KB-2413. However, the early stage of the active Arthus reaction in rabbits sensitized with egg albumin was inhibited. KB-2413 had an inhibitory effect on the efferent phase of delayedtype hypersensitivity induced by picryl chloride (PC-DTH) in mice. On the other hand, the afferent phase of PC-DTH in mice was unaffected. These results suggest that KB-2413 strongly suppresses type I allergic reactions, and it slightly suppresses type II, III and IV allergic reactions.
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  • Hideaki TAGUCHI
    1987 Volume 89 Issue 2 Pages 63-72
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Five mg/kg of imipramine (IMI) or desipramine (DMI) was injected s.c. to Wistar-Imamichi male and female rats daily from 7 ?? 19 days of age. Control pups received saline. The body temperature of IMI-females showed a significant rise at 7, 8 and 12 weeks of age. Thermic responses to thyrotropin-releasing hormone (TRH, 10 mg/kg, i.p.) at 5 weeks of prepubertal age showed no marked changes. At 9 weeks of age, IMI-males showed a significant hyperthermia 15 ?? 30 min after TRH. Control and IMI-males were castrated at 9 weeks of age. At 11 weeks of age, castrated IMI-males showed a significant decrease in the TRH-induced hyperthermia compared to sham-operated or intact IMI-males. These castrated male rats were treated with a single dose of 20 mg/kg of testosterone enanthate (s.c.) at 11 weeks of age. There was no significant difference in the TRH-induced hyperthermia between the groups when tested at 13 weeks of age. Results suggest that the exposure of the infantile rats to imipramine induces sex-related functional alterations in the thermoregulatory system after puberty and that sex hormones may play a modulatory role for these changes.
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  • Toyoyuki TAMURA, Akira FUJII, Noboru KUBOYAMA
    1987 Volume 89 Issue 2 Pages 73-80
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Antitumor effects of Royal Jelly (RJ) were investigated employing the transplantable tumors of mouse advance leukemia L1210 and P388 strains and Ehrlich, Sarcoma-180 ascites and solid tumor strains. RJ was administered orally in a prophylactic-therapeutic (30 days before and 30 days after the transplantations of tumor cells) or a therapeutic (30 days after the transplantations of tumor cells) manner. Tumor cells were transplanted i.p. (ascites tumor) or s.c. (solid tumor). The daily dose of RJ was 0 (control), 10, 100, or 1000 mg/kg. In the case of the therapeutic experiments employing advance leukemia L1210 and P388 strains, which gave quite a short survival period of 8 ?? 9 days, RJ did not show any antitumor effect. In the case of the therapeutic RJ application employing the Sarcoma-180 ascites tumor, which gave a moderate survival period of 16 days, the increased life span was 9.3 ?? 19.3%; and with the Ehrlich ascites tumor (survival period of 22.1 days), the increased life span was 20.4% (RJ 10 mg/kg•day) and 17.6% (RJ 1, 000 mg/kg·day), but no antitumor effect was observed at the dose of 100 mg/kg. day. In the case of the therapeutic experiment employing Ehrlich solid tumor, tumor growth inhibition was 25.3 ?? 54.8%, where as the use of the prophylactic-therapeutic regimen gave a tumor growth inhibition of 38.3 ?? 45.7%. In the case of the therapeutic RJ application employing Sarcoma-180 solid tumor, tumor growth inhibition was 45.1 ?? 59.7%, where as the prophylactictherapeutic regimen gave a tumor growth inhibition of 49.1 ?? 56.1%. There results indicate that RJ is not effective against rapidly growing tumors; however, it is effective against slowly growing tumors such as solid tumor.
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  • Kazuhiro WAKAYAMA
    1987 Volume 89 Issue 2 Pages 81-90
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    Effects of pretreatment with hydrocortisone or prednisolone on the pharmacological effects of baclofen, particularly on the muscle relaxant action, were studied in young adult rats. 1) Muscle relaxation was determined using an inclined board (50°). A single injection of hydrocortisone (10 mg/kg, s.c.) 15 min prior to the administration of baclofen (5 mg/kg, i.p.) increased significantly the muscle relaxant time by baclofen. Prednisolone pretreatment (2 mg/kg, s.c.) also prolonged baclofen-induced muscle relaxation. Muscle relaxation due to tolperisone (50 mg/kg, i.p.) and mephenesin (80 mg/kg, i.p.) administration was enhanced by the pretreatment of hydrocortisone. Hydrocortisone pretreatment enhanced the muscle relaxant time of diazepam (2 mg/kg, i.p.) but at a lesser extent and only in males. No synergistic effect of hydrocortisone on the muscle relaxation time by suxamethonium (0.01 mg/kg, i.p.) was observed. 2) Seven daily injections of 2 mg/kg hydrocortisone as well as of 0.4 mg/kg prednisolone did not enhance the muscle relaxation by baclofen when tested 24 hr after the last injection of the two steroids. 3) Fifteen min priming with hydrocortisone had no effect on the antinociceptive and hypothermic effects of baclofen. 4) 3H-Baclofen was injected i.v. as a tracer of 1 mg/kg unlabeled baclofen. In hydrocortisone-treated rats, the uptake of 3H-baclofen into the hippocampus, medulla oblongata and cerebellum was significantly higher than that in the vehicle-treated rats, whereas the radioactivity in the cervical, thoratic and lumber spinal cord tended to decrease. The results indicate that acute priming with hydrocortisone enhances rather selectively the muscle relaxant action of the centrally acting muscle relaxant drugs. It is suggested that the primary site of the synergistic action of hydrocortisone to baclofen could be at the supraspinal level of the CNS.
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  • Hitoshi KONTANI, Akihiro MANO, Ryozo KOSHIURA, Mitsuo YAMAZAKI, Yasuji ...
    1987 Volume 89 Issue 2 Pages 91-101
    Published: 1987
    Released on J-STAGE: February 23, 2007
    JOURNAL FREE ACCESS
    In this experiment, we synthetized new 2-methyl-3-aminopropiophenone (MP) derivatives, whose structure is known to have central muscle relaxant activities, and quinolizidine and indan•tetralin derivatives derived from MP by cyclization, and we investigated the central muscle relaxant activity. Among the quinolizidine derivatives, there was a very strong central depressant agent, trans (3H, 9aH)-3-(p-chloro) benzoyl-quinolizidine (HSR-740), and among the indan•tetralin derivatives, there was an excitant agent, trans (1H, 2H)-5-methoxy-3, 3-dimethyl-2-piperidinomethyl indan-1-o1 (HSR-719). From the results, these derivatives were not considered to be adequate for central muscle relaxant. Among the MP derivatives, (4'-chloro-2'-methoxy-3-piperidino) propiophenone HCl (HSR-733) and (4'-ethyl-2-methyl-3-pyrrolidino) propiophenone HCl (HSR-770) strongly inhibited the cooperative movement in the rotating rod method using mice, and it exerted almost the same depressant activity on the cross extensor reflex using α-chloralose anesthetized rats. However, the inhibitory effects of HSR-733 on the anemic decerebrate rigidity and the rigidity induced by intracollicular decerebration in rats were weaker than those of HSR-770 and eperisone. In spinal cats, at a low dose (5 mg/kg, i.v.), HSR-733 depressed monosynaptic and dorsal root reflex potentials as compared with polysynaptic reflex potentials, and inhibitory effects of HSR-733 on these three reflex potentials were more potent than those of eperisone and HSR-770. Although HSR-770 acts on the spinal cord and supraspinal level on.which eperisone has been reported to act, HSR-733 may mainly act on the spinal cord. These results indicate that the MP derivative with a 2-methyl group may be suitable as a central muscle relaxant. HSR-770, which has equipotent muscle relaxant activity to eperisone, exerted strong inhibitory effects on oxotremorine-induced tremor and weak inhibitory effects on spontaneous motor activity in the Animex method using mice, as compared with eperisone.
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