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Volume 80, Issue 1
Displaying 1-8 of 8 articles from this issue
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Kimio HARA, Yukihiro IKOMA, Nozomu OSHINO1982 Volume 80 Issue 1 Pages 1-13
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe central dopaminergic (DA) activity of lisuride hydrogen maleate (lisuride) was investigated from the view point of behavioral pharmacology in rats and mice. Lisuride exhibited a biphasic action on locomotor activity in mice and rats; with low doses lisuride caused hypomotility, whereas higher doses produced locomotor stimulation. The hypomotility induced by lisuride (0.00625 mg/kg, s.c.) was antagonized by a low dose of sulpiride (10 mg/kg, i.p.) in rats, and the lisuride (0.05 mg/kg)-induced hyperactivity was inhibited with haloperidol (0.1 mg/kg, i.p.). The stimulatory effect of lisuride on locomotion was not affected by the combined pretreatment with reserpine and α-methyl-p-tyrosine. The hyperactivity of mice induced by methamphetamine was inhibited by pretreatment with lisuride. In the rat lesioned unilaterally in the nigro striatal pathway by a local injection of 6-hydroxydopamine, a low dose of lisuride induced rotational behavior contralateral to the side of the lesion, and the rotational behavior was inhibited by pretreatment with haloperidol. These results indicate that lisuride at low doses effectively stimulates pre-synaptic DA receptors and the post-synaptic DA receptor under supersensitization in the mesolymbic and nigro striatal systems.View full abstractDownload PDF (5448K) -
Showa UEKI, Shigenori WATANABE, Tsuneyuki YAMAMOTO, Yasufumi KATAOKA, ...1982 Volume 80 Issue 1 Pages 15-30
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe behavioral effects of KB-509 and its metabolites were investigated and compared with those of diazepam in mice and rats. The locomotor activity of mice measured by an Animex test was decreased with relatively large doses of KB-509 and diazepam. The anticonflict effect of KB-509 in rats was approximately as potent as that of diazepam. The lever pressing responses in the unpunished period were reduced by diazepam at a dose of 50 mg/kg p.o., while they were not affected by KB-509 even at a large dose such as 100 mg/kg p.o. KB-509 inhibited conditioned avoidance responses of the rat in a shuttle box at an extremely large dose such as 1000 mg/kg p.o. This effect of KB-509 was much less potent than that of diazepam. KB-509 was more potent than diazepam in inhibiting footshock-induced fighting behavior in mice. KB-509 was more potent than diazepam in suppressing hyperemotionality, but was less potent than diazepam in inhibiting muricide of olfactory bulbectomized rats. KB-509 and diazepam prevented maximal electroshock, pentetrazol, and strychnine induced convulsions in mice. KB-509 was more potent than diazepam in potentiating barbital anesthesia, in impairing rotarod performance, and in muscle relaxant activity measured by a traction test in mice. The pharmacological activity of desalkyl-KB-509 was more potent than that of KB-509 and that of desalkyl-3-OH-KB-509 was approximately as potent as that of KB-509. These results indicate that KB-509 possesses pharmacological properties similar to that of diazepam, and it is slightly greater in potency and is much longer in duration of action than diazepam.View full abstractDownload PDF (7614K) -
Akihide KODA, Takeshi NISHIYORI, Hiroichi NAGAI, Naosuke MATSUURA, Hir ...1982 Volume 80 Issue 1 Pages 31-41
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSA study was carried out to examine the effects of 23 kinds of crude drugs and 3 kinds of blended Chinese traditional medicines on Type I and Type IV allergic reactions. Forty eight-hr homologous PCA in rats as a typical model of the Type I reaction using anti-dinitrophenylated ascaris•IgE serum was significantly inhibited by the oral administration of the following drugs: Aqueous extracts: Aurantii F.i., Bupleuri R., Schizandrae F., Scutellariae R., Zizyphi F., and Shohsaiko-to and Methanolic extracts: Asiasari R., Aurantii F.i., Bupleuri R., Ginseng R., Glycyrrhizae R., Magnoliae C., Schizandrae F. and Trichosanthis S., Contact dermatitis in mice as a model of the Type IV reaction caused by picryl chloride was significantly inhibited by the oral application of aqueous extracts of Ginseng R. and Magnoliae C. as well as the powder of Hoelen. The aqueous extract of Saiboku-to also showed an inhibition of the contact dermatitis, and it significantly potentiated the inhibition of contact dermatitis by prednisolone.View full abstractDownload PDF (4404K) -
Saizo YANAURA, Harumi KITAGAWA, Tomokazu HOSOKAWA, Miwa MISAWA1982 Volume 80 Issue 1 Pages 43-50
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAntitussive and respiratory effects of three newly synthesized methanobenzazonine derivatives and their d- and l-isomers were investigated to understand the relationship between the cough and respiratory centers. Antitussive effects were evaluated with the PEC (puncture electrode-induced cough) method in conscious guinea pigs. The respiration study was carried out in anesthetized guinea pigs. Intraarterial injections of d-, dl-, and l-ST-2123; d-, dl-, and l-TS-2121; and d-ST-2121 into the right carotid artery at a dose range of 0.2-0.8 mg caused no effect on respiration. dl-ST-2121 at 0.4 to 0.8 mg and l-ST-2121 at 0.2 to 0.8 mg depressed respiration dose-dependently. Codeine (0.2-0.8 mg) depressed respiration slightly. Morphine (0.2-0.8 mg) depressed respiration more strongly. All the methanobenzazonine derivatives used, when given intraperitoneally, showed antitussive potencies that were 1/3-1/2 the potency of codeine. The antitussive potencies of the d-, dl-, and l-isomers of the three derivatives used were discussed on the bases of chemical structures and drug receptors. These results provide evidence of a discrepancy between the cough and respiratory centers in the brain stem.View full abstractDownload PDF (3347K) -
Saizo YANAURA, Harumi KITAGAWA, Tomokazu HOSOKAWA, Miwa MISAWA1982 Volume 80 Issue 1 Pages 51-59
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSIn order to understand the relationship between the cough and respiratory centers in the brain stem, we investigated the effects of respiratory stimulants, pentylenetetrazol (PTZ) and nikethamide (NK), and a respiratory depressant, pentobarbital (PB) on the cough reflex. Coughs were induced in lightly anesthetized dogs by electrical stimulation of the central sectioned end of the superior laryngeal nerve. The drugs were administered intraarterially into the vertebral artery. The rate (RR), amplitude (RA), and volume (RV) of the respiration and the number (NC) and amplitude (AC) of the cough reflex induced were used as indices. PTZ and NK, even at subthreshold doses for respiratory stimulation, enhanced the cough reflex (NC; not AC). On the other hand, PB at subthreshold doses for a respiratory depression decreased both NC and AC. The above findings suggest that respiratory stimulants generally enhance the cough reflex, and respiratory depressants reduce the cough reflex. Additionally, the thresholds for the cough responses to respiratory drugs are lower than those for the respiratory responses.View full abstractDownload PDF (3988K) -
Hirosato IMAI, Yayoi MURAMATSU, Kazumi NIU, Masakatsu NOZAKI, Hajime F ...1982 Volume 80 Issue 1 Pages 61-68
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSInhibitory effects of TN-762 (suprofen), ketoprofen, and indomethacin on rat or rabbit platelet aggregation were examined. Of these compounds tested, suprofen showed the most potent effect on platelet aggregation in vitro, especially in AA-induced rabbit platelet aggregation (IC50=0.01 μM). Suprofen showed an inhibitory effect similar to that of ketoprofen and indomethacin on rat platelet aggregation ex vivo. The lethal effect of AA in the rabbits was protected by suprofen (0.05 mg/kg p.o.) at concentrations lower than the other compounds. Similar to the other compounds, suprofen had little effect on the PG I2 synthesis in the rat aorta. In order to test the direct effects of these compounds on the platelet avoiding the effects of other plasma components, gel-filtrated rat platelets were used. All tested compounds showed similar inhibitory effect. To investigate the interaction of these compounds with the lipid bilayers, we used the liposome as a model membrane. The tested compounds inhibited liposome aggregation induced by 4 mM Ca2+. In this experiment, the interaction of suprofen with the lipid bilayers was shown.View full abstractDownload PDF (3539K) -
Haruyoshi AZUMA, Tomoaki MIYAZAWA, Nozomu OSHINO, Toshihisa ISHIKAWA1982 Volume 80 Issue 1 Pages 69-81
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of lisuride, a central dopamine and serotonin agonist of the ergot type, on local cerebral glucose utilization were studied in conscious, anesthetized, and substantia nigra-lesioned rats using the autoradiographic 2-deoxyglucose method. In the conscious rat, lisuride produced dose-dependent (0.05-0.5 mg/kg s.c.) increases of glucose utilization in the cerebellar gray structures (lobule of culmen, vermian lobule, uvula, cerebellar hemisphere) and the lateral nucleus of the thalamus. Although some other gray structures including cerebral cortex were also slightly stimulated, no change was observed in the hippocampus, hypothalamus, amygdala, mammilary body, superior colliculus, pons, and any of the white structure. The stimulatory effect of lisuride was abolished almost completely by the pretreatment with sulpiride or haloperidol. Pentobarbital and γ-butyrolactone produced marked reduction in the glucose utilization all over the brain, and these effects were not affected by the pretreatment of lisuride. A unilateral 6-hydroxydopamine lesion at the substantia nigra caused a reduction of glucose utilization in the ipsilateral auditory cortex that was reversed by the administration of lisuride. These results indicate that lisuride modulates the motion coordination function of the cerebellum through the cerebral cortex.View full abstractDownload PDF (7046K) -
Minoru KATOH, Tatsuyoshi SUGIMOTO1982 Volume 80 Issue 1 Pages 83-91
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffect of malotilate on chronic liver injury induced by carbon tetrachloride (CCl4) was studied in rats. Rats were intraperitoneally injected with CCl4 dissolved in olive oil at a rate of 0.5 ml/kg, twice a week for 10 weeks. Malotilate mixed with a laboratory chow diet at a concentration of 0.2% was fed to the rats for 10 weeks, the last 5 or 2 weeks in parallel with CCl4-injection. Significant elevations of plasma transaminase activities, increases of liver triglycerides (TG), malonedialdehyde (MA), and 4-hydroxyproline contents, and decrease of liver protein content were observed at 5, 8, and 10 weeks after initiation of CCl4-injection. In the histopathological study, vacuolation at 5 weeks, vacuolation and fibrosis at 8 weeks, and extreme fibrosis at 10 weeks were observed in rat liver with CCl4-injection. In the rats fed the diet containing malotilate for 10 weeks, these changes of biochemical parameters and histopathological findings were not observed at any time and only slight increase of liver TG and slight vacuolation at 10 weeks was observed. When rats were fed the diet containing malotilate for the last 5 or 2 weeks, these changes of biochemical parameters and histopathological findings caused by CCl4 were improved thereafter. Although the covalent bindings of the radioactivity from 14CCl4 to liver and liver microsomal phospholipids were slightly depressed by malotilate feeding, it is difficult to explain the protective effect of malotilate on the liver injury only by this phenomenon. Other probable mechanisms for this effect were discussed.View full abstractDownload PDF (5354K)
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