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Volume 72, Issue 4
Displaying 1-9 of 9 articles from this issue
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Shinobu SAKURADA, Takeshi TADANO, Kensuke KISARA1976 Volume 72 Issue 4 Pages 371-379
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESS1) Tyramine (Ty), octopamine, dopamine (DA), noradrenaline (NA) and 5-hydroxytryptamine (5-HT) were separated on a phosphorylated-cellulose column (1 × 32cm; 26m1). 2) When Ty was qualitatively analyzed by native fluorescence, Ty reached to peak 30 min after i. c. administration of Ty and disappeared 120 min after administration. 3) 30min after Ty (160 μg, i. c.) the maximum increase of DA was observed. Though DA was maintained at the significant increase level as compared with the saline-treated group, there was no significant difference in the level 120 min later. 4) 30 ?? 60 min after Ty (160 μg, i. c.), NA and 5-HT decreased significantly compared with the saline-treated group. 120 min after Ty, both amines recovered to the normal levels. 5) 30 min after Ty, the increase in DA was dependent in proportion to doses of Ty, and the decrease in NA and 5-HT was also in parallel. 6) 30 min after the pretreatment of isocarboxazide, injection of Ty produced a significant increase in the DA level as compared with the non-pretreated group and the decrease of NA level compared with control (MAOI + saline). Although the injection of Ty only reduced the 5-HT level, the administration of Ty produced an increase in the 5-HT level in mice pretreated with MAGI.View full abstractDownload PDF (3685K) -
Hiroyuki MATSUDA, Tamako KATO, Yukio YAMAMOTO, Hiroaki MIICHI, Shuntar ...1976 Volume 72 Issue 4 Pages 381-395
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSPharmacological properties and acute toxicity of 2-tolyl 1-phenyl-3-(2-methylpiperidino) propyl ether methyl bromide (R111) and 2-chlorophenyl 1-phenyl-3-(2-methylpiperidino) propyl ether methyl iodide (R97) were examined. The results obtained were as follows: (1) In the analgesic effects, RIII and R97 inhibited markedly the acetic acid-induced writhing in mice, but in reducing pain induced by heat, R111 and R97 showed negative results. The local anesthetic effect of R111 was approximately equal to that of procaine. R111 and R97 showed no effects on spontaneous locomotion, the convulsion induced by strychnine or pentetrazol, and normal body temperature. (2) R111 and R97 antagonized acetylcholine, barium chloride, nicotine and serotonine-induced spasm, but not that of histamine and bradykinin. In particular they possessed marked anti-barium chloride activity, where their effects were 20 to 30 times more active than that of papaverine. (3) R111 and R97 indicated weak mydriatic activity. (4) R111 and R97 showed inhibitory effects on the pilocarpine-induced sialic secretion and the propulsive movements of the small intestine, but their inhibitory effects on the gastric secretion were relatively weak. (5) R111 and R97 displayed protective effects in Shay's ulcer, but had no curative effects on acetic acid ulcer. (6) R111 and R97 induced temporary reduction of arterial blood pressure and blood flow immediately after the administration of the test compounds in anesthetized rabbits. However, these agents induced no change in ECG, heart rate and respiration. (7) Intraperitoneally administered R111 and R97 were effective in inhibiting the carrageenin-induced edema in the hind paw of rats. From the above results, it may be considered that R111 and R97 have together strong cholinergic blocking and muscotropic antispasmodic effects, moreover, no significant effects on the central nervous system.View full abstractDownload PDF (6792K) -
Toshie KOGA1976 Volume 72 Issue 4 Pages 397-402
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSInfluence of meclofenoxate (MF) on the 5-HT and 5-HIAA contents in the cortex, diencephalon and brain stem of the rat was studied with the following results. MF caused a dose-dependent elevation of 5-HIAA level in the three different brain regions and particularly in the brain stem. An increase of 5-HT was also noted in the brain stem, whereas 5-HT in the diencephalon tended to decrease. The increase of 5-HT after pargyline was accelerated and the pargyline-induced decrease of 5-HIAA was equally inhibited by MF and probenecid, which suggests that MF blocks the efflux of 5-HIAA from the brain. The effects of MF on the brain 5-HT and 5-HIAA contents were identical with those of its hydrolysate, p-chlorophenoxyacetic acid.View full abstractDownload PDF (2666K) -
Yutaka MARUYAMA, Yukinobu KADOBE, Hiroshi IMAMURA1976 Volume 72 Issue 4 Pages 403-416
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThis anti-inflammatory agent proved to have a therapeutic margin wider than that of indomethacin. Y-8004 exhibited little effect on the central nervous system, somatic and autonomic nervous system. On the cardiovascular system in dogs, Y-8004 induced a slight transient fall in blood pressure followed by a pressor response, increase in heart rate and coronary vasodilation at a dose of 30 mg/kg given intravenously, but no remarkable change was seen on the electrocardiogram. Y-8004 showed no effect on isolated smooth muscles such as vas deferens, ileum and atria, but inhibited gastrointestinal propulsion at a dose of 100 mg/kg given orally in mice and spontaneous contractions of the pregnant uterus of rats at a concentration of more than 10-6 M. This agent also decreased urine volume and electrolytes in rats. This property was considered to be common to other acidic nonsteroidal anti-inflammatory agents. On the other hand, in guinea pigs, Y-8004 inhibited the bradykinin-induced bronchoconstriction and the collagen-induced platelet aggregation to a greater extent than did indomethacin. These findings suggest that Y-8004 is an active compound with properties similar to acidic non-steroidal anti-inflammatory agents such as indomethacin.View full abstractDownload PDF (6334K) -
Akira AKASHI, Takeshi HASHIZUME, Makoto TANAKA, Shin-ichi NAKA, Ikuo S ...1976 Volume 72 Issue 4 Pages 417-431
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSPharmacological properties of LOP were compared with those of imipramine(IMP). LOP had little or no effect on electroconvulsive shock and chemoconvulsions in mice, conditioned avoidance response in rats, pain threshold in mice and rats and body temperature in rabbits. LOP, unlike IMP, showed relatively weak effects on general behavior in mice, spontaneous EEG in cats and spontaneous motor activity in mice. LOP prevented oxotremorine-induced hypothermia but not tremor, while IMP antagonized both the responses in mice. In anesthetized dogs, LOP caused a respiratory stimulation and a fall in blood pressure, left ventricular pressure and left ventricular dp/dt without a noticeable effect on heart rate. LOP was less potent than IMP in the depressor and cardiodepressing effects, antispasmogenic activity and in antagonizing the depressor response to acetylcholine. LOP, like IMP, potentiated pressor response to norepinephrine and reduced that to tyramine in anesthetized dogs, but neither antidepressant produced norepinephrine potentiation in isolated guinea-pig vas deferens. Both drugs inhibited spontaneous motility of the jejunum without reducing the gastric motility in anesthetized dogs. These results indicate that, compared with IMP, LOP is characterized by weak general pharmacological activities.View full abstractDownload PDF (7458K) -
Hikaru OZAWA, Takashi NOZU, Hironaka AIHARA, Fusao AKIYAMA, Michitada ...1976 Volume 72 Issue 4 Pages 433-443
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSAbsorption, distribution and excretion after oral administration of lithium carbonate (Li2CO3) and/or lithium chloride (LiCl) were studied in Wistar rats and beagle dogs. The maximum level of concentration in the blood was seen within 4 hr after administration of Li2CO3, and a greater part of the orally dosed Li2CO3 was excreted into the urine. The blood and urine Li levels after the administration of LiCI were similar to those seen with Li2CO3. In dogs, Li2CO3 was more slowly excreted into the urine than it was in rats. Li was selectively incorporated into the thyroid and pituitary a short time after administration, and was not detected in any organ 7 days after cessation of repeated dosing for 19 days. The movement of Li into the brain was slow and relatively low levels were achieved after a single administration, but high and constant levels were shown after repeated administration. Effects of Li salts on behavior of ddy mice with repeated administration were investigated. The spontaneous motor activity was suppressed with Li2CO3 more strongly than with LiCl. The high dose of Li2CO3 suppressed not only the stimulating actions of methamphetamine and cocaine, but the ptotic and hypothermic action of reserpine. From these results, it is concluded that the repeated administration of Li salts reveals higher levels of Li ion in the brain than does a single administration, and also more responsive action on the central nervous system.View full abstractDownload PDF (4238K) -
Takashi NOZU, Tatsuo FURUKAWA1976 Volume 72 Issue 4 Pages 445-451
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSSimple and sensitive methods for the separation and determination of catecholamines and their metabolites by thinlayer microcrystalline cellulose chromatography have been developed and applied to the analysis of norepinephrine (NE) and dopamine (DA) metabolism in the brain of Wistar rats given 14C-NE or 14C-DA intraventricularly. 14C-DA in the whole brain declined more rapidly than did 14C-NE. The percentage of unchanged 14C-NE in total radioactivity in the brain of rats administered 14C-NE was high, while on the other hand, the percentage of unchanged 14C-DA in cases of 14C-DA was low. In the metabolism of 14C-DA, the deaminated and O-methylated deaminated metabolites showed transient and delayed temporary rises, respectively. Drugs which affect the metabolism of catecholamines were also examined. Methamphetamine reduced NE, deaminated and O-methylated deaminated metabolites, and markedly elevated normetanephrine in the brain of rats given 14C-NE. Regarding the metabolism of DA, methamphetamine increased 3-methoxytyramine and homovanillic acid and reduced deaminated metabolites, but had no effect on DA and NE. On the other hand, a reserpine-like drug (Ro4-1284) reduced NE and increased deaminated and O-methylated deaminated metabolites in the metabolism of NE, and reduced to a great extent DA and NE and increased homovanillic acid in the metabolism of DA. From these results, it is concluded that the effect of methamphetamine was more evident in NE metabolism than DA, while the effect of Ro4-1284 was more evident in DA metabolism than NE.View full abstractDownload PDF (3337K) -
Kiyoshi KIMURA1976 Volume 72 Issue 4 Pages 453-473
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe role of 5HT and NA in the regulation of the sleep-awake cycle, especially in the triggering mechanisms of paradoxical sleep (PT), was studied in rabbits using reserpine, parachlorophenylalanine (PCPA), α-methylp-tyrosine (α-MT) and α-methyl-m-tyrosine (α-MMT). 1) Reserpine (0.5 mg/kg, i.v.) caused a diphasic action on the brain electrical activity in rabbits: an initial activation pattern in the EEG which continued for 2-3 hr, was followed gradually by a slow wave. Forty to sixty min after reserpine administration, spike waves resembling the PGO waves in cats appeared from the medial nucleus Trapezoides (Trap. m.) in rabbits. From the electrophysiological point of view, these spike waves (reserpine spike waves) were in many respects similar to those recorded during PS (TR spike waves). Later reserpine spike waves appeared almost continuously for about 8 ?? 12 hr during arousal and slow wave sleep stages. When the amplitude and grouping of spike waves became prominent, severe myoclonic jerky movements resembling “pseudo hallucinatory” behavior were observed. Polygrams of these periods were similar to those of PS except for abrupt arousal and orienting reactions. The onset of the typical PS episode was delayed by more than 8 ?? 9 hr. 2) Repeated doses of PCPA (500 mg/kg/day for 3 consecutive days, i.p.) caused only slight suppressive effect on slow wave sleep (SS), but spike waves similar to TR spike and/or reserpine spike waves developed throughout SS. When the amplitude and grouping of these spike waves were progressively increased, SS was often followed by PS. Abrupt enhancement of these spike waves was associated with “pseudo hallucinatory” behavior and aroused the animal. Usually these spike waves were not seen during arousal phase. When reserpine (0.5 mg/kg) was given i.v. to PCPA-treated rabbits, the latent period of appearance of reserpine spike waves was markedly shortened. 3) α-MMT, at a dose which had no effect on SS, markedly suppressed PS for a long period. These findings suggest that 5HT and NA in the lower brainstem play inhibitory roles on the triggering mechanism of PS.View full abstractDownload PDF (9220K) -
Kimikazu ITAYA, Jiosuke KIYONAGA1976 Volume 72 Issue 4 Pages 475-481
Published: 1976
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSIn clinical trials, it is well known that γ-oryzanol is effective against the syndromes of autonomic nervous unbalance and climacteric disorders. The authors studied the action of γ-oryzanol on restraint, waterimmersion stress ulcer under various conditions in rats. The drug, given 1 to 100 mg/kg s.c. daily for five days, reduced the ulcer index dose-dependently, and slightly prevented the rate of increase in serum level of 11-OHCS. These effects were observed in adrenalectomized as well as sham operated rats. It is likely that the antiulcerogenic action of γ-oryzanol is due to participation of the autonomic nervous system, but not the hypophyseoadrenal axis.View full abstractDownload PDF (2930K)
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