巻号一覧
44 巻 (1987)
- 4 号 p. 373-
- 3 号 p. 233-
- 2 号 p. 105-
- 1 号 p. 1-
44 巻, 3 号
選択された号の論文の17件中1～17を表示しています
- |<
- <
- 1
- >
- >|
-
Ryuji SUNAGAWA, Keiji MURAKAMI, Goro MIMURA, Matao SAKANASHI1987 年 44 巻 3 号 p. 233-240
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーTo examine the myocardial contractile response of the diabetic heart, effects of isoproterenol (ISO) and norepinephrine (NE) on perfused hearts isolated from streptozotocin (STZ)-induced diabetic rats and insulin-treated diabetic rats were evaluated. Male Sprague-Dawley rats, weighing 200-260 g, were divided into the control (C)-group, diabetes mellitus (DM)-group and diabetes mellitus treated with insulin (DMI)-group. The C group was injected with buffered vehicle. DM and DMI groups were injected intravenously with 60 mg/kg STZ on the first day. Three days after STZ injection, the DMI group was subsequently treated with 4 U of Lente insulin subcutaneously every day. At 45 days after injection of STZ, experiments were performed using a Langendorff perfused heart preparation. The heart was paced at 300 beats/min, and myocardial developed tension (T) was measured isometrically. Plasma glucose values (mg/dl) were 142.4±8.7 in C, 499.3±15.6 in DM and 370.6±27.6 in DMI group. The order of percent increase in T induced by ISO (3×10-9-3×10-8g) was C=DMI>>DM, and that by NE (10-7-10-6g) was C>DMI>DM. On the other hand, the percent increase in T induced by CaC12 (1.1 ×10-4-2.2×10-3g) and aminophylline (AMI, 0.31×10-3-5.00 ×10-3g) was not significantly different among three groups. These results indicate that adrenergic receptor-mediated contractile response was significantly depressed in the diabetic heart.抄録全体を表示PDF形式でダウンロード (422K) -
Yoshiki KUNO, Tetsuo OKA1987 年 44 巻 3 号 p. 241-247
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーThe relative importance of three enzymes, amastatin-sensitive aminopeptidase, captopril-sensitive peptidyl dipeptidase A and phosphoramidon-sensitive endopeptidase-24.11, to inactivate two opioid peptides, [Met5]-enkephalin and [Met5]-enkephalin-Arg6, was investigated in three in vitro isolated preparations, guinea-pig ileum, mouse vas deferens and rat vas deferens, by estimating the magnitude of the enhancement of the inhibitory potency of the opioid peptide by each peptidase inhibitor. Results showed that the relative importance of the three enzymes in the inactivation of the opioid peptide, whether it was [Met5]-enkephalin or [Met5]-enkephalin-Arg6, in guinea-pig ileum was significantly different from that in either mouse vas deferens or rat vas deferens. Additionally, the relative importance of the three enzymes in the preparation, whether it was guinea-pig ileum, mouse vas deferens or rat vas deferens, in the inactivation of [Met5]-enkephalin was significantly different from that of [Met5]-enkephalin-Arg6. The significance of the presence of plural inactivating-enzymes for opioid peptides was discussed.抄録全体を表示PDF形式でダウンロード (399K) -
Kentaro KOGI, Tetsuo SATOH1987 年 44 巻 3 号 p. 249-257
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーThis study was designed to determine the extent, to which isosorbide-5-mononitrate (5-ISMN) contributes to the hemodynamic effect of isosorbide dinitrate (ISDN) in conscious dogs. Test drugs (ISDN or 5-ISMN) were given orally. Either ISDN or 5-ISMN produced a decrease in blood pressure dose-dependently, the decrease in pulse pressure being specific; the pattern of blood pressure change induced by ISDN or 5-ISMN was different from that induced by nifedipine or prazosin. The effect of ISDN (2 mg/kg) was almost equivalent to that of 5-ISMN (4 mg/kg) and the effect of ISDN (4 mg/kg) to that of 5-ISMN (8 mg/kg). After administration of ISDN, both ISDN and 5-ISMN appeared in the plasma, and the effect of ISDN well-correlated with the increase in the plasma concentration of 5-ISMN. Contribution of 5-ISMN to the effect of ISDN was estimated to be about 30% from the value of the plasma concentration of 5-ISMN at 3 to 4 hr after administration, when the maximal response to ISDN occurred. Based on the data of the area under the plasma concentration curve of 5-ISMN (from 0 to 10 hr after administration), the fraction of biotransformation to 5-ISMN from ISDN was calculated to be 73.6 to 76.6% (based on moles). Because the ability of 5-ISMN to decrease pulse pressure was about 1 /2 (or 41% based on moles) of that of ISDN, the contribution of 5-ISMN to the effect of ISDN was estimated to be about 30% in total, the value being similar with that estimated at 3 to 4 hr after administration.抄録全体を表示PDF形式でダウンロード (508K) -
Tetsu HAYASHI, Makizo HIRABAYASHI, Sakutaro TADOKORO1987 年 44 巻 3 号 p. 259-267
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーThe effect of methamphetamine (MAP) on ambulatory activity and neurochemical changes in catecholaminergic neurons in the brain were investigated in dd and C57BL/6 strains of male mice. The mice were given repeatedly MAP at 2 mg/kg, s.c., 10 times at a fixed interval of 4 days. Single MAP markedly increased the ambulatory activity in both strains of mice. The ambulation-increasing effect was progressively enhanced without accompanying stereotyped behaviors when the drug was repeatedly given. The dd mice showed higher susceptibility not only to single MAP but also to the enhancing effect of the drug (reverse tolerance) than the C57BL/6 mice. On the other hand, non-treated dd mice exhibited lower maximum densities of 3H-spiperone binding sites in the striatum and 3H-WB4101 binding sites in the cortex and hippocampus than nontreated C57BL/6 mice. In contrast, the dd mice exhibited higher noradrenaline turnover than the C57BL/6 mice in the brain regions examined. The repeated administration of MAP produced decrease in the densities of both 3H-spiperone and 3H-WB4101 binding sites in the corresponding regions with increase in catecholamine turnover in dd mice. However, the similar changes were observed only in 3H-WB4101 binding sites and noradrenaline turnover in C57BL/6 mice. These results suggest that the ambulation-increasing effect of MAP is positively correlated with catecholamine turnover, while it was correlated negatively with the densities of catecholamine binding sites. Furthermore, the enhancing effect of MAP is supposed to have been partially elicited by changes in brain catecholaminergic systems, in particular an increase in catecholamine turnover. Strain difference in the enhancing effect of MAP may be partially caused by different regional sensitivity to the drug.抄録全体を表示PDF形式でダウンロード (515K) -
Koji TAKEUCHI, Hideyuki NISHIWAKI, Yasunobu ISHIHARA, Susumu OKABE1987 年 44 巻 3 号 p. 269-281
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーThe present study was undertaken using acetazolamide (AZ) and cysteamine (Cys) to investigate the relationship between gastric motor activity and the phenomenon of “cytoprotection” in rats. Both AZ (10-100 mg/kg) and Cys (10-100 mg/kg), given either p.o. or s.c., significantly reduced the formation of gastric mucosal injury caused by HCI-ethanol (1 ml of 60% ethanol in 150 mM HCl, p.o.). The protective effect of Cys appeared within 10 min, reached the maximal levels 30 min later, while that of AZ appeared from 30 min after administration and became potent with a latency period after treatment. Neither indomethacin (IM: 5 mg/kg, s.c.) nor N-ethylmaleimide (NEM: 5 mg/kg, s.c.) significantly affected the protective effect of Cys, whereas that of AZ was almost totally antagonized by IM. Both AZ and Cys, given either intragastrically or s.c., significantly inhibited gastric motor activity measured as intraluminal pressure recordings, but had minimal effect on acid and alkaline secretion. IM significantly attenuated the inhibitory effect of AZ on the motor activity, while NEM did not affect the inhibited motor responses caused by AZ and Cys. A significant relationship was found between the inhibitory effects of these two drugs on gastric motor activity and HCl-ethanol-induced mucosal injury, the correlation coefficient being 0.819 (P<0.01). When the mucosal folds were visualized with Gentian Violet (1 ml of 0.5% v/v, p.o.), both AZ and Cys significantly prevented the localized staining along the mucosal folds, suggesting dissolution of the folds. These results suggest that both AZ and Cys protect the gastric mucosa against injury caused by HCI-ethanol, probably through a dissolution of mucosal folds due to inhibition of gastric motor activity.抄録全体を表示PDF形式でダウンロード (679K) -
Masakatsu TAKAHASHI, Shogo TOKUYAMA, Hiroshi KANETO1987 年 44 巻 3 号 p. 283-291
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーPsychological (PSY) stress using the communication box produced a short-lasting antinociceptive effect which was less potent than that induced by physical stress such as footshock (FS) and forced swimming (SW) in mice. Naloxone completely antagonized PSY-stress induced analgesia (SIA) when the analgesia was measured by the tail pinch (TP) method; however, the antagonist did not reverse the effect in the tail flick (TF) assay. On the other hand, FS-SIA was antagonized by naloxone in both methods, while naloxone failed to reverse SW-SIA in either TF or TP assessment. Daily exposure to psychological stress developed tolerance to the analgesia. One-way cross-tolerance between PSY-SIA and morphine and the naloxone antagonism of PSY-SIA by the tail pinch method lead to the suggestion that an endogenous opioid system may be involved in the underlying mechanism for its production. On the contrary, from the findings of cross-tolerance between SW- or FS-SIA and the lack of naloxone antagonism in the TF method, the involvement of a more complicated mechanism is suggested in PSY-SIA. In both tests, U-50488H, a selective κ-agonist, produced profound analgesia; however, no appreciable antagonism of naloxone was found in the TF test, whereas the effect was completely blocked by naloxone in the TP test. From the similarity in naloxone antagonism of PSY-stress and U-50488H induced an algesia, the participation of a common mechanism which may be mediated by κ-opioid receptors, is suggested in the production of PSY-SIA.抄録全体を表示PDF形式でダウンロード (404K) -
Shigeru KIGOSHI, Mamoru KOKUBO1987 年 44 巻 3 号 p. 293-302
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーDextromethorphan and its analogues (DM 16, DM 34, DM 72, DM 75 and DM 96) were examined for their effect on Ehrlich ascites carcinoma or ascites sarcoma-180 in female mice of the ddY strain. The suspension of Ehrlich carcinoma cells or sarcoma-180 cells was prepared from mice at 10 days after i.p. inoculation of the cells, using Hanks' balanced salt solution, and the cell suspension was inoculated i.p. into mice (2×106 viable cells/mouse). The chemicals dissolved in physiological saline containing 5% HCO-60 were then injected i.p. into the mice once daily for 5 successive days (5-40 mg/kg/day). In addition, mice given the tumor cells were treated with the saline containing 5% HCO-60 alone for 5 days (untreated mice). In groups of mice bearing Ehrlich ascites carcinoma or ascites sarcoma-180, the mean survival time of mice treated with 20-40 mg/kg/day of DM 96 was more than twice that of the corresponding untreated mice. The mean survival time of mice treated with 20 mg/kg/day of DM 96 was also longer than that of mice treated with 40 mg/kg/day of the other chemicals, irrespective of the ascites tumors. Concerning these survival times, the LD50 (i.p.) of DM 96 in mice differed slightly from that of other chemicals (88 mg/kg and 77-106 mg/kg). These results indicate that DM 96 is more active than the other chemicals against the ascites tumors in mice.抄録全体を表示PDF形式でダウンロード (409K) -
Hiroyasu OKUNO, Toshihiko MURASE, Sadao NAKANISHI, Yasuko SHIOZAKI, Yo ...1987 年 44 巻 3 号 p. 303-310
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーThe effect of malotilate (diisopropyl 1, 3-dithiol-2-ylidenemalonate) on drug metabolizing activity in rat liver microsomes was examined. Malotilte (500 mg/kg/day) was administered orally to rats for 3 days. The contents of cytochrome P-450 (P-450) and cytochrome b5 (b5), the activity of NADPH-cytochrome c reductase, and the metabolization of aniline, aminopyrine, benzo(a)pyrene (B(a)P) and 7-ethoxycoumarin (7-EC) in the microsomal fraction were examined 24 hr after the final administration of malotilate. The content of b5 and the activity of NADPH-cytochrome c reductase were increased by the malotilate treatment, but the content of P-450 was not significantly affected. 7-EC O-deethylation was markedly and aminopyrine N-demethylation was moderately enhanced; in contrast, aniline hydroxylation was significantly and B(a)P hydroxylation was slightly reduced. Such different effects of malotilate among the four substrate-metabolizing activities may be due mainly to the increase in the content of b5, which participates in the transport of the second electron required for P-450 function to various extents. It is also possible that malotilate affects the population of P-450 subtypes, each having a different substrate specificity and a different affinity for b5.抄録全体を表示PDF形式でダウンロード (390K) -
Masahiko SAKURAYA, Kazuya TANIGUCHI, Kuniaki SUZUKI, Akinobu KUDO, Shi ...1987 年 44 巻 3 号 p. 311-321
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーNa+, K+-ATPase from pig kidney was sequentially modified with two different sulfhydryl fluorescent reagents, N-[p-(2-benzimidazolyl)phenyl] maleimide (BIPM) and N-[7-dimethylamino 4-coumarinyl]maleimide (DACM). The preparation thus obtained contained 3 and 2 moles of each residue in the α-chain. When the BIPM residues were excited at 313 nm, ouabain sensitive decrease and increase in the fluorescence intensity at not only 365 nm (BIPM fluorescence) but also 455 nm (DACM fluorescence) were observed, which were dependent on the amounts of reaction intermediates accumulated. When DACM residues were excited directly at 390 nm, only the decrease in the fluorescence intensity was observed irrespective of the intermediates accumulated. The data suggest that at least two DACM residues which differently change their microenvironments during ouabain sensitive Na+, K+-ATPase reaction are present. One is located close enough and the other is located too far to accept the energy from BIPM residue(s) in the three dimensional structure of Na+, K+-ATPase. Addition of sodium dodecyl sulfate (SDS) remarkably inhibited the energy transfer from BIPM to DACM residues. Limited proteolysis suggested that BIPM residues are located mainly in the peptides which are assumed to contain ATP binding sites and that DACM residues are located near the phosphorylation sites.抄録全体を表示PDF形式でダウンロード (706K) -
Yukihiko HAGIWARA, Yukiko SUZUKI1987 年 44 巻 3 号 p. 323-334
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリー1) In the experiments reported here, we investigated effects of CPZ on the amplitude of cerebellar potentials using decerebrated or spinal cat; furthermore, we also examined the effects of microinjecting CPZ, DA or NE into the precerebellar nuclei on the amplitude of the cerebellar potentials. 2) Purkinje cell spontaneous discharge was either hardly changed or was depressed by CPZ. 3) CPZ did not change the potentials evoked by peripheral stimulation on the dorsal surface of the spinal cord. 4) CPZ depressed significantly the cerebellar potentials evoked by stimulation of the nucleus reticularis lateralis (LRN) or nucleus olivaris inferior (ION) in intact, decerebrated and spinal cats. 5) The cerebellar potentials evoked by the peripheral nerve stimulation were increased by microinjection of CPZ into the bilateral LRN but not into the bilateral ION. Microinjection of NE or CPZ into the contralateral LRN hardly influenced the cerebellar evoked potentials. 6) Although electrical stimulation at high frequencies of the ipsilateral LRN depressed significantly the cerebellar evoked potentials; similar stimulation after i.v. pretreatment of CPZ failed to affect them. Microinjection of CPZ into the ipsilateral LRN enhanced the cerebellar evoked potentials, and microinjection of NE or DA depressed them significantly. Furthermore, after pretreatment with CPZ, microinjection of DA failed to depress the potentials. 7) We suggest that intravenous CPZ-induced enhancement of the cerebellar potentials may be due to depression of the descending inhibitory mechanism, resulting from CPZ-induced blockage of the catecholamine receptors of the ipsilateral LRN and of the spinal levee.抄録全体を表示PDF形式でダウンロード (590K) -
Koji TAKEUCHI, Hideyuki NISHIWAKI, Osamu FURUKAWA, Susumu OKABE1987 年 44 巻 3 号 p. 335-344
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーWe examined the effects of histamine 2HCl (a stimulator of endogenous acid production) and exogenous acid on transmucosal potential difference (PD) and pH of anesthetized rat stomachs, in order to investigate the mechanism underlying the protective action of histamine against 0.6 N HCl-induced gastric mucosal injury in conscious rats. Subcutaneously administered histamine (3-20 mg/kg) dose-dependently produced a decrease in the PD and pH, and it reduced the severity of gastric mucosal injury caused by 0.6 N HCl. Both indomethacin (5 mg/kg, s.c.) and cimetidine (100 mg/kg, s.c.) completely reversed the protection afforded by histamine (20 mg/kg), although the decreased PD and pH responses were unaffected or inhibited, respectively, by indomethacin or cimetidine. Protective action of histamine was also partially mitigated by omeprazole (30 mg/kg, s.c.) which completely abolished histamine-induced acid secretion. On the other hand, exposure of the stomach for 10 min to exogenous acid (0.1-0.35 N HCl) caused a PD reduction and an increase of pH, in a concentration-related manner. The injury caused by 0.6 N HCl was prevented by prior exposure to these low concentrations of HCl, and the degrees of inhibition were associated with the concentration of HCl and the magnitude of PD reduction caused by HCl. The pretreatment with indomethacin, but not cimetidine or omeprazole, significantly antagonized the increased pH and mucosal protection induced by 0.35 N HCl. These results suggest that histamine protected the gastric mucosa against 0.6 N HCl-induced injury by two different ways, mediated with endogenous prostaglandins, (a) mainly through stimulation of H2-receptors and (b) partly through adaptive cytoprotection induced by acid.抄録全体を表示PDF形式でダウンロード (562K) -
Kazuo HONDA, Noriko MOMOSE, Chieko NAKAGAWA1987 年 44 巻 3 号 p. 345-353
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーIn the isolated detrusor smooth muscle of the rabbit urinary bladder, acetylcholine, prostaglandin (PG) F2α, histamine and methoxamine produced dose-dependent contractions. The order of efficacy was acetylcholine>PGF2α>histamine>methoxamine. Acetylcholine and oxotremorine increased tension remarkably in the rabbit detrusor muscle; and McN-A-343 also developed tension, but with weaker sensitivity and efficacy. The contractile response to acetylcholine was competitively antagonized by atropine (pA2 9.24) and pirenzepine (pA2 6.96), respectively. Histamine and 2-pyridylethylamine caused dose-dependent contractions. On the other hand, dimaprit caused no response in this tissue. Mepyramine (pA2 8.80) competitively antagonized the contraction induced by histamine, whereas cimetidine failed to antagonize the contraction even at a high concentration of 10-5 M. Norepinephrine, phenylephrine and methoxamine have greater efficacies in the ability to contract than clonidine. R(-)- and S(+)-YM-12617 and YM-12617 (pA2 10.4, 8.31 and 9.75, respectively) and prazosin (pA2 8.13), phentolamine (pA2 7.55) and yohimbine (pA2 6.44) competitively an tagonized the contraction elicited by methoxamine. These results suggest that the contraction of rabbit detrusor muscle can be mediated by α1-adrenergic receptors as well as M2-muscarinic and H1-histaminergic receptors and suggest that the contractile force mediated by α1-adrenergic receptor agonist is smaller than those stimulated by the other receptor agonists.抄録全体を表示PDF形式でダウンロード (495K) -
Kiyoshi SAITOH, Tatsuo MANABE, Hideo HONDA, Osamu IRINO1987 年 44 巻 3 号 p. 355-357
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーIt has been supposed that ifenprodil glucuronide derivative, detectable in large amount in rabbit plasma, is related to the pharmacological actions by ifenprodil tartrate. However, a synthesized ifenprodil glucuronide derivative was found to have no effect on platelet aggregation and vasocontraction in vitro. These results indicate that ifenprodil itself rather than its glucoronide derivative manifested the pharmacological actions.抄録全体を表示PDF形式でダウンロード (132K) -
Takashi ITO, Shigetoshi CHIBA1987 年 44 巻 3 号 p. 358-360
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーUsing the cannula inserting method, vascular responses to 7 vasoconstrictor substances were investigated on isolated, perfused simian metacarpal veins. The vein was markedly constricted by an intraluminal administration of norepinephrine, phenylephrine and 5-hydroxytryptamine with a maximal increase in perfusion pressure of over 100 mmHg. Clonidine and xylazine induced only a slight vasoconstriction, but tyramine produced no significant constriction. A large dose of KCI induced a strong vasoconstriction. In this study, it was demonstrated that the simian metacarpal vein has a specific characteristic of vascular reactivity.抄録全体を表示PDF形式でダウンロード (190K) -
Seiji ICHIDA, Kazuo YOSHIOKA, Hiroaki OKA, Yasuo ODA, Shunji ARIYOSHI1987 年 44 巻 3 号 p. 361-364
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーUnder Ca-depleted conditions, the contractile responses of rat vas deferens in the presence of norepinephrine were not elicited until the addition of CaCl2. L-Methionine enhanced the contractile response of vas deferens in the presence of methylation blockers under these conditions. The enhancing effect of L-methionine on some other smooth muscles could not be determined because under Ca-depleted conditions, these muscles showed 60-80% of the maximal contractile response on addition of CaCl2 alone. Theas findings suggested that L-methionine has an enhancing effect on contraction of the rat vas deferens as it does on rat uterine muscle.抄録全体を表示PDF形式でダウンロード (221K) -
Shigetoshi CHIBA, Miyoko TSUKADA1987 年 44 巻 3 号 p. 365-368
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーThe stainless steel cannula inserting method was used to investigate the effects of acetaldehyde on isolated and perfused dog mesenteric arteries. Acetaldehyde when intraluminally administered induced a marked vasoconstriction, but repetitive injections of acetaldehyde caused tachyphylaxis. Acetaldehyde-induced vasoconstrictions were blocked by bunazosin, an alpha-1 adrenoceptor antagonist. After tyramine treatment, the acetaldehyde-induced constriction was consistently restored temporarily. It is suggested that tyramine may induce a release of norepinephrine mostly from the vesicle to the neuronal cytosol, and acetaldehyde may cause a release of norepinephrine from the cytosol to the extracellular space in the isolated canine mesenteric artery.抄録全体を表示PDF形式でダウンロード (177K) -
Tadashi NAGAMATSU, Yoshio SUZUKI1987 年 44 巻 3 号 p. 369-372
発行日: 1987年
公開日: 2006/09/15
ジャーナル フリーFunction of the reticulo-endothelial system (RES) was determined by the carbon clearance technique in rats. Rats in the previous phase of nephritis showed reduced function of the RES with circulating immune complexes compared with normal rats. Prostaglandin E1 (PGE1) at 1.0 mg/kg, s.c., resulted in significant recovery in the impaired RES activity of the rats in the previous state of nephritis. Dipyridamole, 400 mg/kg, p.o., slightly enhanced function of the RES, but 20 mg/kg azathioprine, p.o., did not. Thus, the enhanced RES activity with PGE1 can explain part of the antinephritic effect of PGE1.抄録全体を表示PDF形式でダウンロード (224K)
- |<
- <
- 1
- >
- >|