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Volume 49 (1989)
- Issue 4 Pages 441-
- Issue 3 Pages 301-
- Issue 2 Pages 155-
- Issue 1 Pages 1-
Volume 49, Issue 2
Displaying 1-17 of 17 articles from this issue
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Yukihiro OZAKI, Soekeni SOEDIGDO, Yoke Rosina WATTIMENA, Asep Gana SUG ...1989 Volume 49 Issue 2 Pages 155-163
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSMace which is the aril of the fruit of Myristica fragrans HOUTT. has been used in Indonesian folk medicine as aromatic stomachics, analgesics, a medicine for rheumatism, etc. The present study was carried out to elucidate the antiinflammatory effect of methanol extract obtained from Mace and its active principles. The methanol extract was extracted with ether, and then the ether soluble fraction was extracted with n-hexane. The n-hexane soluble fraction was fractionated by silica gel column chromatography (Fr-I-Fr-V), and the active principle was isolated from Fr-II by thin layer chromatography (Fr-VI-Fr-VII). The antiinflammatory activity of these fractions was investigated on carrageenin-induced edema in rats and acetic acid-induced vascular permeability in mice. All fractions and indomethacin were suspended in 2% C.M.C. solution and administered p.o. The methanol extract (1.5 g/kg), ether fraction (0.9 g/kg), n-hexane fraction (0.5 g/kg), Fr-II (0.19 g/kg) and Fr-VI (0.17 g/kg) showed a lasting antiinflammatory activity, and the potencies of these fractions were approximately the same as that of indomethacin (10 mg/kg). Fr-VI was determined to be myristicin. These results suggest that the antiinflammatory action of Mace is due to the myristicin that it contains.View full abstractDownload PDF (575K) -
Katsumi SUGIYAMA, Takako OGINO, Ken-ichiro OGATA1989 Volume 49 Issue 2 Pages 165-171
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSTreatment of human serum albumin with a proteolytic enzyme such as pepsin, α-chymotrypsin, cathepsin D or trypsin generated histamine releasing peptides. A low-molecular weight peptide (P-1) responsible for releasing histamine was isolated from peptic digests of human serum albumin by affinity chromatography on heparin-Ultrogel and reversed-phase high performance liquid chromatography. The amino acid sequence of the P-1 was estimated to be V-R-Y-T-K-K-V-P-Q-V-S-T-P-T-L by Edman degradation. The sequence determined appears to correspond to residues 409-423 of human serum albumin. Peptide P-1 produced dose-related histamine release from isolated rat mast cells in the concentration range of 1-50 μM. The intradermal injection of the P-1 (0.5 μg) increased capillary permeability in rats. This response was blocked by the antihistamine diphenhydramine.View full abstractDownload PDF (558K) -
Masao KOZUKA, Nobuyoshi IWATA1989 Volume 49 Issue 2 Pages 173-179
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSEffects of S-adenosyl-L-methionine (SAM) on the metabolism in ischemic brain were investigated. The ischemic model employed was an incomplete cerebral ischemia of the spontaneously hypertensive rat (SHR) produced by the occlusion of both common carotid arteries. One hundred mg/kg of SAM was administered (i.p.) 6 times from the beginning of occlusion at 30 min intervals. At 3 hr after the onset of occlusion, animals were killed by microwave irradiation and creatine phosphate (CrP), ATP, glucose, lactate and γ-aminobutyric acid (GABA) contents in the brain were measured. SAM significantly mitigated both the reductions in CrP, ATP and glucose levels and the increase in GABA level due to the cerebral ischemia. In another set of experiments with the same experimental schedule, water content in the brain was examined. SAM significantly suppressed the increase in water content due to the cerebral ischemia. These results indicate ameliorating effects of SAM on the metabolism in ischemic brain.View full abstractDownload PDF (596K) -
Huei-Yann TSAI, Jaung-Geng LIN, Reizo INOKI1989 Volume 49 Issue 2 Pages 181-185
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSThe possible mechanism of electroacupuncture (EAc) in reference to the effects of neuropeptides on serotonergic neurons in rat spinal cord was studied. The tested drugs were administered by intrathecal injection or spinal push-pull perfusion. The results showed that baclofen, substance P (SP) and naloxone administered intrathecally could reduce the tail pressure pain threshold. The pain threshold was increased by met-enkephalin (EK) and EAc. The action of EAc was antagonized by naloxone. The release of 5-HT in the spinal cord evoked by tail pressure pain stimulation (TP) was inhibited by EK, baclofen and EAc. However, naloxone could potentiate the 5-HT release evoked by TP. EAc reversed the naloxone potentiation of TP-evoked 5-HT release. The 5-HT release evoked by exogenous SP, however, was potentiated by EK and EAc. From these results, it is suggested that the influence of EAc on 5-HT release may be due to activation of enkephalin-interneurons, which presynaptically inhibit the primary sensory neurons in the spinal cord.View full abstractDownload PDF (380K) -
Masatoshi TANAKA, Yoshishige IDA, Akira TSUDA, Shusaku TSUJIMARU1989 Volume 49 Issue 2 Pages 187-196
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSBy measuring levels of noradrenaline (NA) and its major metabolite, 3-methoxy-4-hydroxyphenylethyleneglycol sulfate (MHPG-SO4), in various rat brain regions, we investigated the effects of an extract isolated from vaccinia virus-inoculated and inflamed skin or tissue of rabbits (Neurotropin, NSP), administered acutely or chronically, on regional NA metabolism in stressed and nonstressed rats. An acute administration of NSP at 50 mg/kg significantly elevated MHPG-SO4 levels in the amygdala and cerebral cortex; and 100 mg/kg of the drug significantly increased the metabolite levels in the hypothalamus, amygdala, thalamus, midbrain, cerebral cortex and pons plus medulla oblongata without affecting NA levels. This suggests that acutely injected NSP slightly increases NA release in these brain regions. One hour immobilization stress caused significant increases in MHPG-SO4 levels, which were not affected by pretreatment with either 50 mg/kg or 100 mg/kg of NSP. Chronic injection with NSP daily at either 50 mg/kg or 100 mg/kg for 7 days was without effect on NA metabolism in all brain regions examined. However, increases in MHPG-SO4 levels caused by stress were significantly attenuated in some regions including the hypothalamus, amygdala and midbrain in chronic NSP-treated rats. This indicates that although an acute administration of NSP slightly increases brain NA release, a chronic treatment with NSP rather attenuates increases in NA release caused by immobilization stress in brain regions such as the hypothalamus, amygdala and midbrain. This suggests a possibility that these attenuating effects on stress-induced increases in brain NA release caused by chronic administration of NSP might be related to the stress-reducing or anti-stress properties of NSP.View full abstractDownload PDF (873K) -
Hisashi KURIBARA, Sakutaro TADOKORO1989 Volume 49 Issue 2 Pages 197-203
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSEffects of single administration of methamphetamine (1, 2 and 4 mg/kg, s.c.) and morphine (5, 10 and 20 mg/kg, s.c.) and repeated administration of methamphetamine (2 mg/kg, s.c.) and morphine (10 mg/kg, s.c.) on ambulatory activity were investigated in 6 mouse strains: dd, ICR, BALB/c, C57BL/6, C3H/He and DBA/2. Although there were differences in the drug sensitivities among mouse strains, methamphetamine and morphine increased the ambulatory activity in all the strains except for the DBA/2 strain that showed an increase only after morphine. Repeated 5 times administration of methamphetamine at intervals of 3-4 days induced a reverse tolerance (an enhancement in the sensitivity) to the ambulation-increasing effect in all the strains with a marked degree in dd, ICR, C3H/He and DBA/2 strains and a slight degree in BALB/c and C57BL/6 strains. The same treatment with morphine induced reverse tolerance to the effect of morphine markedly in C57BL/6 and C3H/He strains and moderately in dd, ICR and BALB/c strains, but the DBA/2 strain showed no significant change in the ambulatory activity throughout the repeated 5 times administration of morphine. There was positive correlation between the initial drug sensitivities of animals and the degrees of the reverse tolerance in either methamphetamine or morphine. Furthermore, the reverse tolerance to methamphetamine and morphine was sometimes transferable, although such cross interaction varied among mouse strains.View full abstractDownload PDF (518K) -
Shigeyuki NAKAJIMA, Kenji KUROKAWA, Nobuhiko IMAMURA, Motohiko UEDA1989 Volume 49 Issue 2 Pages 205-213
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSThe direct effect of pinacidil on contractile protein systems and the relationship between its vasodilating effects and intracellular Ca2+ concentration were studied in isolated smooth muscle of guinea pigs. Pinacidil, nifedipine and hydralazine did not inhibit Ca2+-induced contracture in saponin-treated taenia caecum of guinea pig, while trifluoperazine and W-7 markedly suppressed it. Simultaneous determination of the intracellular Ca2+ concentration (fura 2 method) and tension development of the isolated femoral artery of guinea pigs showed that the intracellular Ca2+ level always decreased before vasorelaxation after pinacidil or nifedipine administration. Pinacidil showed no effect on cyclic AMP or cyclic GMP contents in rabbit aortic strips. These results indicate that pinacidil, like nifedipine and hydralazine, do not seem to directly act on the process from the formation of Ca2+-calmodulin to the actinmyosin interaction in the contracting mechanism of vascular smooth muscle, and that pinacidil relaxes the vascular smooth muscle by decreasing intracellular Ca2+-levels without elevating cyclic nucleotides.View full abstractDownload PDF (665K) -
Hirohumi KODA, Tsuneichi HASHIMOTO, Kinya KURIYAMA1989 Volume 49 Issue 2 Pages 215-223
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSEffect of buflomedil (4-(1-pyrrolidinyl)-1-(2, 4, 6-trimethoxy phenyl)-1-butanone hydrochloride) on the release and uptake of dopamine (DA) and the function of DA receptors in the striatum was investigated using male Wistar rats. In vitro addition of buflomedil (10-5-10-8M) had no effect on the uptake of [3H]-DA in striatal slices. On the other hand, buflomedil (10-5-10-7 M) increased the spontaneous as well as high K+ (30 mM)-evoked releases of [3H]DA from striatal slices. Buflomedil inhibited the bindings of [3H]SCH23390, [3H]spiperone and [3H]apomorphine to striatal D1, D2 and D3 receptors only at a high concentration. On the other hand, buflomedil inhibited [3H]quinuclidinyl benzilate (QNB) binding to striatal muscarinic cholinergic receptors, which was similar to the action of carbachol. Pretreatment with scopolamine (0.5 mg/kg) in vivo inhibited the facilitation of striatal DA turnover induced by oral administration of buflomedil (300 mg/kg). In contrast, continuous oral administration of buflomedil (30 mg/kg×7 days) to rats had no significant effect on the specific bindings of [3H]SCH23390, [3H]spiperone, [3H]apomorphine and [3H]QNB to synaptic membrane preparations obtained from the striatum. These results suggest that buflomedil may enhance striatal DA release by stimulating muscarinic cholinergic receptor and that DA receptors may not be involved in the enhancing effect of buflomedil on DA release.View full abstractDownload PDF (735K) -
Hiroyuki WAKABAYASHI, Kenji SHIMADA, Yoshio AIZAWA, Tetsuo SATOH1989 Volume 49 Issue 2 Pages 225-234
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSIn the dark phase, the effects of the psychotropic drugs on the contents of melatonin, serotonin (5-HT) and N-acetylserotonin (NAS) in rat pineal gland were examined. The pineal gland was removed at a certain period of time after subcutaneous injection of the drugs. 5-HT, NAS and melatonin contents in the pineal gland were determined by high performance liquid chromatography with fluorometric detection. A dose-dependent decrease was observed for melatonin content in the administration of diazepam (DZP), hydroxyzine (HYZ), chlorpromazine (CPZ) or haloperidol (HPD). When imipramine (IPM) or amitriptyline (APL) was given to rats, pineal 5-HT content was significantly decreased. On the other hand, the administration of IPM or APL caused increases in pineal NAS and melatonin. Furthermore, the administration of phenytoin (PYT) revealed no changes in the content of pineal indoleamines. These results suggest that the psychotropic drugs widely used in clinical applications could cause significant changes in pineal indoleamine content.View full abstractDownload PDF (772K) -
Koji TAKEUCHI, Yasunobu ISHIHARA, Megumu OKADA, Hiromichi NIIDA, Susum ...1989 Volume 49 Issue 2 Pages 235-244
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSWe assembled a new system using a lucite chamber and rat stomach for simultaneous measurement of transmucosal potential difference (PD) and luminal pH as indicators of the mucosal integrity and the secretory activity, respectively. The biological preparation involved only the glandular mucosa and responded to a variety of mucosal damaging agents by different degrees of PD reduction, pH increases and histological damages. When the mucosa was exposed for 10 min to 1 M NaCl, the reduced PD was restored with time, reaching the baseline values within 2 hr with histological restitution. Titration of gastric effluent showed that after the exposure, acid secretion ceased and a considerable amount of HCO3- was evident in the lumen, followed by re-secretion of acid. These secretory changes corresponded with those of luminal pH; this remained elevated for 1 hr after the exposure and returned to the basal values 2 hr later. The histological restitution as well as the PD recovery after damage were significantly interfered with by indomethacin (5 mg/kg, s.c.) or vasopressin (10 unit/kg/hr, i.v.), respectively, at the dose which inhibited the increased pH responses caused by 1 M NaCl or reduced the mucosal blood flow. These results suggest that this system may be useful for studying physiological changes of gastric mucosa after acute injury and for screening drugs that may have an effect on the repair process.View full abstractDownload PDF (777K) -
Keitaro HASHIMOTO, Kentaro AKIYAMA, Harumi MITSUHASHI1989 Volume 49 Issue 2 Pages 245-254
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSUsing two-stage coronary ligation-, digitalis- and adrenaline-induced canine ventricular arrhythmias, antiarrhythmic effects of nicainoprol were examined in dogs, and the minimum effective plasma concentration for each arrhythmia model was determined. Nicainoprol suppressed the arrhythmias, and the minimum effective plasma concentrations for arrhythmias induced by 48 hr coronary ligation, digitalis and adrenaline were 8.9 μg/ml (by 5 mg/kg, i.v.), 3.0 μg/ml (by 3 mg/kg, i.v.) and 2.7 μg/ml (by 3 mg/kg, i.v.), respectively. The concentration for coronary ligation arrhythmia was higher than those for the digitalis and adrenaline arrhythmias. This pharmacological profile is similar to those of aprindine and propafenone. Nicainoprol induced some central nervous system effect including vomiting in conscious coronary ligated dogs. Though intravenous nicainoprol (5 mg/kg) was not effective on 24 hr coronary ligation arrhythmia, an oral dose of 30 to 40 mg/kg was effective. These results indicate that it may become a clinically useful antiarrhythmic drug.View full abstractDownload PDF (600K) -
Junichi KURIHARA, Hiroyuki NISHIMURA, Nobuyuki ODA, Hitoshi KATO1989 Volume 49 Issue 2 Pages 255-265
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSInfluence of transient global cerebral ischemia on baroreceptor reflex sensitivity (BRS) was investigated in anesthetized dogs. Cerebral ischemia was produced by the combined occlusions of the left subclavian (LSA) and the brachiocephalic (BCA) arteries with preceding ligations of the intercostal arteries (ICA). BRS was assessed by phenylephrine-induced reflex bradycardia. Ischemia of 5-and 10-min duration produced a significant decrease in BRS during the reperfusion period of 60-120 min. On the other hand, such a change was not observed following the ischemia of less than 2-min or occlusions of LSA and BCA without preceding ligations of ICA. Heart rate response to the electrical stimulation of the vagal afferent nerve was attenuated by 10-min ischemia, while response to the vagal efferent nerve stimulation and ECG parameters were not influenced. These results indicate that some regions vulnerable to the relatively short duration of cerebral ischemia may be involved in the central pathway of the baroreflex mechanism.View full abstractDownload PDF (775K) -
Wen-Chuan LIN, Shingo YANO, Kazuo WATANABE1989 Volume 49 Issue 2 Pages 267-274
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSEffect of intravenous administration of GABA antagonists on gastric acid secretion in perfused stomachs was studied in rats anesthetized with urethane. Bethanechol (BeCh)-stimulated acid secretion was definitely inhibited by bicuculline, a GABA antagonist, and strychnine, a glycine antagonist, but not by picrotoxin and pentylenetetrazol, GABA antagonists. The inhibitory effect of bicuculline and strychnine was accompanied by vigorous convulsions. Only the bicuculline-induced inhibition was still seen in d-tubocurarine paralyzed rats, and it was abolished in spinal rats. 2-Deoxy-D-glucose (2-DG)-stimulated acid secretion was apparently depressed by all the GABA antagonists of bicuculline, picrotoxin and pentylenetetrazol. The inhibitory effect of picrotoxin, but not bicuculline, on the 2-DG stimulation was still elicited in spinal rats. Inhibition of acid secretion stimulated by pentobarbital, a centrally acting secretagogue, was produced by picrotoxin and pentylenetetrazol in spinal rats. These findings suggest that bicuculline acts centrally to inhibit acid secretion stimulated both peripherally by BeCh and centrally by 2-DG, besides nonspecific mechanisms due to convulsions, and the action would be directed to centers which are implicated in stimulation of the sympatho-adrenomedullary system; picrotoxin and pentylenetetrazol also act centrally to inhibit 2-DG- or pentobarbital-stimulated acid secretion through depression of the central vagal tone which leads to inhibition of gastric acid secretion.View full abstractDownload PDF (592K) -
Stimulation of Phagocytic Activity of Leukocytes and Macrophages by Traxanox Sodium in Mice and RatsMasao HISADOME, Michio TERASAWA, Kazuhiro GOTO, Yasushi KAWAZOE, Takek ...1989 Volume 49 Issue 2 Pages 275-284
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSPhagocytosis of yeast particles by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes was enhanced by traxanox sodium in vitro. Traxanox sodium (30 and 100 mg/kg, p.o.) enhanced phagocytosis of yeast particles by leukocytes and macrophages in vivo or ex vivo. On the other hand, prednisolone, isoproterenol and theophylline inhibited phagocytosis by leukocytes and macrophages under the same conditions. Traxanox sodium (30 mg/kg, p.o.) prevented the suppression of phagocytosis by the above drugs. Combined with theophylline, isoproterenol synergistically inhibited phagocytosis by leukocytes in vivo. Traxanox sodium (100 mg/kg, p.o.) administered alone had no influence on carbon clearance in normal mice. However, traxanox sodium (1-30 mg/kg, p.o.) prevented the suppression of carbon clearance by the treatment with carrageenan, but not by the treatment with ethyl palmitate. These results suggest that traxanox sodium stimulates the phagocytic activity of leukocytes or macrophages and prevents the drug-induced suppression of the phagocytic activity of these cells.View full abstractDownload PDF (735K) -
Shabbir M. MOOCHHALA, Edmund J.D. LEE, Gwendolene T.M. HU, O.S. KOH, G ...1989 Volume 49 Issue 2 Pages 285-291
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSWe have evaluated the in vitro effects of bromocriptine (Br), on the hepatic cytochrome P-450 monooxygenase system of rats pretreated with saline phenobarbitone (PB) and β-naphthoflavone (BNF). Br inhibited ethoxyresorufin O-dealkylase (EROD) activity in liver microsomes of rats pretreated with saline and PB but not in BNF pretreated animals. Maximum inhibition of EROD activity by Br in the microsomes of saline and PB pretreated rats were 50%-60% of the control. In contrast, a dual effect was observed on aminopyrine N-demethylase activity (APD) by Br in microsomes of saline, PB and BNF pretreated rats. At a low concentration (25 μM), Br inhibited the activity of APD to a similar extent in all pretreatment groups; however, with higher concentrations of Br (50 μM to 300 μM), enhancement of APD activity was observed. Br (300 μM) increased the APD activity to 2-3 times the control level in microsomes of rats pretreated with saline, PB or BNF. Spectral studies revealed a Type II binding of Br to cytochrome P-450 from microsomes of saline and PB pretreated rats. A reverse type I binding was observed for BNF induced microsomes. In addition, Br also enhanced NADPH cytochrome c (P-450) reductase activity to a similar extent in all pretreatment groups. These results suggest that the inhibition of EROD activity may be due to direct binding by Br to certain isozymes of cytochrome P-450 and that the enhancing effect of Br on APD activity may be in part due to the activation of the NADPH cytochrome c reductase component of the cytochrome P-450 monooxygenase system.View full abstractDownload PDF (488K) -
Taeko HATA, Eiji ITOH, Ritsuko OYAMA, Atsufumi KAWABATA, Tomitaro KITA1989 Volume 49 Issue 2 Pages 293-296
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSThe sensitivity of SART-stressed (repeated cold-stressed) mice to substance P (SP) was studied. The behavioral responses to intrathecal SP in the stressed mice were less marked than those in non-stressed mice. The 50% effective dose of SP, however, did not differ between the 2 groups. Also, the antagonistic effect of intrathecal [D-Pro2, D-Trp7, 9]-substance P against SP was not different. These results suggest that SART-stressed mice are subsensitive to exogenous SP and that the number but not the affinity of SP receptors may be altered.View full abstractDownload PDF (298K) -
Yutaka GOMITA, Katsushi FURUNO, Yasunori ARAKI1989 Volume 49 Issue 2 Pages 297-299
Published: 1989
Released on J-STAGE: August 25, 2006
JOURNAL FREE ACCESSThe influence of emotional stress on the pharmacokinetics of isosorbide dinitrate (ISDN) was studied in rats. Plasma levels of orally administered ISDN and metabolites (5-isosorbide mononitrate and 2-isosorbide mononitrate) were lower in rats emotionally stressed by foot shock than in non-stressed control rats. The decrease in the ISDN levels may be mainly due to the delay of drug absorption from the gastrointestinal tract.View full abstractDownload PDF (234K)
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