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Volume 93 (1989)
- Issue 6 Pages 315-
- Issue 5 Pages 271-
- Issue 4 Pages 203-
- Issue 3 Pages 89-
- Issue 2 Pages 29-
- Issue 1 Pages 7-
Volume 93, Issue 2
Displaying 1-6 of 6 articles from this issue
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Keitaro HASHIMOTO1989 Volume 93 Issue 2 Pages 29-39
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSIn order to compare and clarify the effects of various antiarrhythmic drugs, we examined drug effects on several canine arrhythmia models, simultaneously determining the minimum effective plasma concentrations. We used 1) two-stage coronary ligation arrhythmia, 2) digitalis arrhythmia, and 3) halothane-adrenaline arrhythmia. The following are, a summary of our results : Antiarrhythmic drugs of class 1 all suppressed digitalis arrhythmia, and except for lidocaine, also suppressed coronary ligation arrhythmia. Class 2 antiarrhythmic drugs, β blockers, and class 4 antiarrhythmic drugs, Ca channel blockers, had common features of effectiveness, where they suppressed adrenaline arrhythmia in relatively low concentrations. Some differences among the antiarrhythmic effects of class 1 drugs could not be explained by their subclassification based either on action potential duration or kinetic properties of dissociation or association with Na channels. A new arrhythmia model for triggered activity in in vivo canine heart was developed, but drug effects on it does not seem to be very different from the effects on the other three arrhythmia models.View full abstractDownload PDF (9061K) -
Akira HIROSE, Masashi SASA, Akinori AKAIKE, Shuji TAKAORI1989 Volume 93 Issue 2 Pages 41-47
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSElectroencephalographic (EEG) studies were performed to examine the effects of SM-3997 on the spontaneous EEG, EEG arousal responses, recruiting responses and hippocampal afterdischarges in rabbits and the spontaneous EEG in chronically electrode-implanted rats. In acute experiments using rabbits, SM-3997 at doses of 1 ?? 3 mg/kg, i.v., produced lowvoltage fast waves in cortical EEG and slow waves with reduction of the amplitude in hippocampal EEG. The drug at doses of 1 ?? 3 mg/kg, i.v., dose-dependently inhibited the threshold stimulus voltages in EEG arousal responses induced by stimulation of the midbrain reticular formation and slightly inhibited the threshold in recruiting responses by stimulation of the centromedian nucleus of the thalamus. However, the cortical and hippocampal afterdischarges induced by hippocampal stimulation remained unaffected by SM-3997 at doses up to 3 mg/kg, i.v., while they were inhibited by diazepam of 1 mg/kg, i.v. In the study using rats in which electrodes were chronically implanted, SM-3997 at doses of 10 ?? 30 mg/kg, i.p., also produced low voltage fast waves in cortical EEG and slow waves of reduced amplitude in hippocampal EEG; and it simultaneously caused flat body posture. These results suggest that SM-3997 acts on both the cerebral cortex and hippocampus, inducing much more pronounced inhibition on the midbrain reticular formation-hippocampal system.View full abstractDownload PDF (5324K) -
Hisato KITAGAWA, Fumiyo TAKEDA, Masayo IZUMITA, Toshihiro HAYASHI, Hir ...1989 Volume 93 Issue 2 Pages 49-54
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSAnticholinergic properties of oxitropium bromide (Ba 253) were compared with those of atropine and ipratropium bromide (Sch 1000). The metabolites of Ba 253 (Ba 941, BEA 1125), the decomposition product (Ba 250), and the impurity (Ad 187) were also studied. In rat salivary activity, gastric secretion and rabbit gastric-motility, the anticholinergic activities of parenterally administered Ba 253 were 2.3 to 11.8 times and 1 to 2 times stronger than that of atropine and Sch 1000, respectively. The mydriatic and antisecretory actions of Ba 253 (p.o. or i.d.) were 1/7 and 1/47 those of atropine, respectively. In isolated rat stomach, guinea pig gallbladder and ileum, the anticholinergic activity of Ba 253 is similar to that of atropine. Inhalation of Ba 253 aerosol prevented ACh- and histamine-induced cough in guinea pigs, and its potency was 1/5 that of atropine or as the same as that of Sch 1000. In the isolated guinea pig trachea and ileum, the potencies of the anticholinergic activities of Ba 250 and Ad 187 were the same as that of Ba 253, but those of the other metabolites were very weak. These results suggest that the anticholinergic activity of Ba 253 is stronger than that of atropine when parenterally administered, and it cannot distinguish between the subtypes of muscarinic receptors.View full abstractDownload PDF (4950K) -
Shigeru KANEKO, Akihiro HARUNO, Norihiko SUZUKI, Kenji KITAZATO, Yasuh ...1989 Volume 93 Issue 2 Pages 55-60
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSPropiverine hydrochloride (P-4) is a new derivative of benzilic acid. The effect of P-4 on the function of the bladder in anesthetized dogs was studied in comparison with flavoxate, which is clinically used for the treatment of pollakiuria. P-4 (4 mg/kg, i.v.) caused a significant increase in maximum vesical volume (Vmax), which was estimated by a cystometrogram. A similar effect was also observed following intravenous administration of verapamil (1 mg/kg), while flavoxate (4 mg/kg, i.v.) caused no significant changes in Vmax. P-4 significantly decreased the frequency of rhythmic bladder contractions at doses higher than 1 mg/kg, i.v., whereas flavoxate first revealed a significant decrease at 4 mg/kg, i.v. Thus the inhibitory effect of P-4 on the micturition movements of the bladder is more potent than that of flavoxate. These findings indicate that P-4 is a useful drug for the treatment of pollakiuria.View full abstractDownload PDF (4265K) -
Kiyoshi KURIYAMA, Yoshiyuki HIYAMA, Yukio AOYAMA, Kiyonoshin ICHIKAWA, ...1989 Volume 93 Issue 2 Pages 61-73
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSPharmacological properties of LFP83, a non-steroidal analgesic and antipyretic drug, were studied in mice, rats and rabbits. LFP83 is a prodrug of flurbiprofen (FP) which is its active major metabolite in vivo. In experimental models of acetic acid writhing, the Randall and Selitto method, arthritic pain, yeast fever, LPS fever, carrageenin edema and adjuvant arthritis, LFP83 (i.v.) showed remarkable analgesic, antipyretic and antiinflammatory activities; and it was more potent than ketoprofen (i.m.) and aspirin DL-lysine (i.v.). The analgesic activity of LFP83 was equal to or more potent than that of pentazocine, and its duration was longer than those of aspirin DL-lysine and pentazocine. In addition, the analgesic potency of LFP83 was approximately the same or more potent than that of FP (p.o.), and the onset of this analgesic effect began earlier. On the other hand, the ulcerogenic activity of LFP83 on rat gastric mucosa was less than that of FP (p.o.) in both single and consecutive (7 days) administrations. The safety index (UD50/ED50) of LFP83 was three to ten-fold higher than that of FP (p.o.). As mentioned above, LFP83 is a potent analgesic, antipyretic and antiinflammatory drug; and in comparison to oral FP, it has a more potent and immediate effect, weak gastric irritation and high safety index.View full abstractDownload PDF (9399K) -
Takayuki IZUMI1989 Volume 93 Issue 2 Pages 75-87
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSTo understand the mechanism of eruption in continuously growing teeth, the relationship between the rate of eruption and formation of dental hard tissues was examined following administration of 1-hydroxyethylidene-1, 1-bisphosphonate (HEBP), an inhibitor of hard tissue formation. Three experimental groups of rats received daily subcutaneous injections of 9, 18 or 36 mg P of HEBP/kg, respectively, for 7 days. Tetracycline was also injected to mark the dentine in some animals. To maintain an unimpeded state, all four incisors in each rat were shortened repeatedly during the experimental period. Eruption rates of the mandibular incisors were measured by a photographic method. Transverse sections of the mandibles were cut and histological, microradiographic and fluorescent micrographic examinations were done. Significant decreases of the eruption rates were found in all experimental groups following the administration of HEBP. However, differences were not marked among the three experimental groups. It was also shown that matrix formation and calcification of the dentine were markedly inhibited following the administration of HEBP. Matrix formation and calcification of the enamel were also inhibited by the drug administration. It is assumed that the eruption of the rat incisor is not closely associated with the formation of dental hard tissues and their calcification.View full abstractDownload PDF (14597K)
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