巻号一覧
37 巻 (1985)
- 4 号 p. 307-
- 3 号 p. 227-
- 2 号 p. 137-
- 1 号 p. 1-
37 巻, 4 号
選択された号の論文の11件中1～11を表示しています
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Krishnaswami RAMABADRAN1985 年 37 巻 4 号 p. 307-316
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーAcute dependence on a single dose of morphine was assessed in Wistar rats by observing the frequencies of occurrence of several signs of withdrawal precipitated by naloxone, diprenorphine, Mr2097, Mr1452 and Mr2266. Naloxone significantly precipitated urination, paw shakes, head shakes and chewing. Diprenorphine significantly precipitated urination and chewing. Mr2097 precipitated urination, head shakes, teeth chattering and chewing. The selective kappa antagonists Mr1452 and Mr2266 significantly precipitated only urination and teeth chattering. Signs of the precipitated withdrawal by Mr2097 were mediated by stereoselective opioid receptors, as the other diastereoisomer, Mr2097, did not precipitate them. Stereospecific opioid receptors were also involved in the induction of acute dependence, as naloxone precipitated withdrawal only in l-methadone-treated rats, but not in d-methadone treated rats. All the opioid antagonists produced at least some degree of "abstinoid". signs in morphine-free rats which might be caused by the blockade of endogenous opioids acting on μ and/or κ receptors. The signs of withdrawal precipitated by naloxone and Mr2097 might be primarily mediated by μ receptors, those of diprenorphine by both μ and κ receptors, and those by Mr1452 and Mr2266 were likely to be selectively mediated by κ receptors. The latter aspect was further supported by experiments showing that the novel κ agonist U-50488H did not precipitate withdrawal. A low degree of precipitation of withdrawal by Mr1452 and Mr2266 and the absence of precipitation of abstinence by U-50488H might be related to either a lack or an existence of a low proportion of κ receptors in rat brain. Further experiments using selective agonists and antagonists are needed to evaluate these findings.抄録全体を表示PDF形式でダウンロード (717K) -
Masako MORIKAWA, Takashi KOJIMA, Michiko INOUE, Minoru TSUBOI1985 年 37 巻 4 号 p. 317-323
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーThe rat platelet aggregation induced by collagen was stronger in males than in females. The platelet malondialdehyde (MDA) production was more in males than in females, and the platelet cyclooxygenase activity was higher in males than in females. Aspirin at a dose of 10 mg/kg inhibited the collagen-induced aggregation in males, but not in females. Aspirin at a dose of 5 mg/kg blocked the MDA production only in males, but aspirin at a dose of 10 mg/kg inhibited the MDA production in both sexes. The effect of aspirin on the cyclooxygenase activity was only in males, but aspirin at a dose of 10 mg/kg inhibited the MDA production in both sexes. The effect of aspirin on the cyclooxygenase activity was similar to that on the MDA production. In gonadectomized rats, the MDA production and the cyclooxygenase activity were decreased by castration, and they were increased by ovariectomy. Aspirin at a dose of 5 mg/kg failed to inhibit them in castrated rats. Besides, in in vitro experiments, aspirin also inhibited the MDA production and the aggregation. Nevertheless, there was no sex difference in the content of arachidonic acid, a substrate of platelet cyclooxygenase. It is suggested that there is a sex difference in rat platelet cyclooxygenase activity, and it is closely related to the sex difference in the antiplatelet effect of aspirin.抄録全体を表示PDF形式でダウンロード (504K) -
Masayuki TAKAHASHI, Nobuyuki OZAKI, Seiichi KAWAKITA, Mitsuhiro NOZAKI ...1985 年 37 巻 4 号 p. 325-334
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーThe vascular effects of 15-hydroperoxyeicosatetraenoic acid (15-HPETE) and 15-hydroxyeicosatetraenoic acid (15-HETE) were investigated on isolated helical strips of canine cerebral and coronary arteries. 15-HPETE caused strong concentration-related contraction of cerebral arteries under resting tension. After contraction with prostaglandin F2α (PGF2α), 15-HPETE caused marked relaxation of coronary arteries. The effects of 15-HETE on isolated canine arteries were similar to those of 15-HPETE. The relaxation of coronary arteries caused by both 15-HPETE and 15-HETE was completely inhibited in the presence of aspirin, but not in the presence of tranylcypromine. Preincubation of coronary and cerebral arterial strips with 15-HPETE or 15-HETE resulted in suppression of the production of 6-keto-PGF1α from exogenously added arachidonic acid; and 15-HPETE, but not 15-HETE, enhanced the production of HETE(s) significantly. Aspirin blocked 15-HPETE induced HETE(s) production in coronary arteries. On cerebral angiography, strong contraction of intracranial arteries was observed after intracisternal injection of 15-HPETE. On the other hand, 15-HETE had little effect on intracranial arteries in vivo. The mechanism of the vascular effects of 15-HPETE and 15-HETE will be discussed.抄録全体を表示PDF形式でダウンロード (980K) -
Mayumi TONOOKA, Ikuo KAWASHIMA, Mitsuaki SAKASHITA, Hajime YASUHARA, K ...1985 年 37 巻 4 号 p. 335-344
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーThe effects of propranolol on lipid metabolism were studied in spontaneously hypertensive rats (SHR). Male SHR and corresponding Wistar Kyoto rats (WKY) were used at 5 weeks of age. The SHR were given 10 mg/kg/day of dl-propranolol·HCI by gavage for 10 weeks. Body weight gain in untreated SHR and propranolol-treated SHR (SHR-P) groups were low, as compared with those of the WKY group. Total cholesterol, phospholipid and total lipid of the serum and liver in the SHR-P group were higher than in the SHR group. In the early weeks of treatment, serum triglyceride and non-esterified fatty acid levels in the SHR-P group were slightly lower than those in the SHR group. Aortic lipid levels in the SHR-P group were lower than those in the SHR group. During the later weeks of treatment, blood glucose level in the SHR-P group was higher than in the SHR group. The serum immunoreactive insulin value in the SHR-P group was slightly lower than in the SHR group. These results may suggest that propranolol inhibits hormone-sensitive lipase activity in the early weeks of treatment and influences cholesterol biosynthesis and/or catabolism.抄録全体を表示PDF形式でダウンロード (540K) -
Kazuo AISAKA, Yoshikazu HATTORI, Takafumi ISHIHARA, Minoru MORITA, Yos ...1985 年 37 巻 4 号 p. 345-353
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーPiperidine is an endogenous active amine. Intravenous or intra-arterial administration of piperidine produced vasodilation in anesthetized dogs. The vasodilative effect of piperidine was inhibited by atropine (0.3 mg/kg, i.v.). In the hind limb perfusion experiment in anesthetized dogs, piperidine produced vasodilation, while it showed no vasorelaxing action in various isolated canine arterial strip preparations. These results suggest that the vasodilation caused by piperidine may be produced through activation of muscarinic receptors and that piperidine may act on smaller resistance blood vessels but not on large conductance vessels. In addition, pipecolic acid and N-methyl piperidine, the respective precursor amino acid and metabolite of piperidine, were almost inactive, but nipecotic acid was 1/4 to 1/10 times as active as piperidine as vasodilators. It is suggested that the non-substituted amine moiety of piperidine is very important for the manifestation of vasodilative activity and that piperidine might play a role in regulation of peripheral vascular circulation.抄録全体を表示PDF形式でダウンロード (581K) -
Keitaro HASHIMOTO, Gordon K. MOE1985 年 37 巻 4 号 p. 355-363
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーIsolated long Purkinje fibers were perfused in oxygenated Tyrode's solution. The conduction velocity of action potentials driven from one end of a fiber at cycle lengths of 300 and 1000 msec was measured using silver wire surface electrodes. Action potentials were recorded using glass microelectrodes. Tyrode's solutions of different potassium concentrations were used, and preparations were equilibrated for 10 min. Prior to acetylstrophanthidin, maximum conduction velocities reaching 2.3 m/sec were recorded at (K)o=6 mM. The conduction velocity was not directly proportional to maximum dV/dt or action potential amplitude at (K)o between 2 and 6 mM; maximum dV/dt and action potential amplitude were greater although conduction velocity was decreased. In this range of (K)o, membrane excitability may be an important factor. Acetylstrophanthidin (10-7 and 5×10-8 g/ml for slowly and rapidly driven preparations, respectively) increased diastolic depolarization and slowed conduction at (K)o less than 6 mM, but it did not increase automaticity or decrease conduction at (K)o over 6 mM. The added effect of high potassium on digitalis-induced slowing of conduction, reported in whole animal experiments, was not observed.抄録全体を表示PDF形式でダウンロード (726K) -
Chihiro NISHIMURA, Kinya KURIYAMA1985 年 37 巻 4 号 p. 365-372
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーPossible involvement of lipid peroxide (LPO) in the occurrence of diabetic retinal lesion was investigated using streptozotocin-induced diabetic rats. Young male Wistar rats weighing 100-150 g were made diabetic by daily intraperitoneal injection of 30 mg/kg streptozotocin (STZ) for 5 days. Five weeks after the termination of STZ-treatment, when animals maintained typical hyperglycemia, the tissue level of LPO, estimated by the thiobarbituric acid method in the presence of 0.5 mM EDTA, was found to be augmented in the kidney. At 7 to 9 weeks after the STZ-treatment, the content of LPO in the retina also exhibited a significant increase, while those in the serum, brain and peripheral nerves showed no alteration. This increment of LPO in the kidney and retina was accompanied by the concomitant reduction of fat-soluble antioxidants determined by the ferric chloride-bipyridyl reaction, and insulin treatment (10 u/rat/day, s.c.) completely eliminated the increased formation of LPO in these organs. When diabetic rats were treated with retinol acetate, which had an inhibitory effect on LPO formation in retinal homogenate, the increase in LPO content was found to be significantly suppressed, especially in the retina. These results suggest that the STZ-induced diabetic state may elicit an increased formation of LPO in the retina and kidney, both of which are known to be main organs having typical diabetic lesions.抄録全体を表示PDF形式でダウンロード (557K) -
Yutaka SAKAI, Misako NAMIMA1985 年 37 巻 4 号 p. 373-379
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーA new benzodiazepine compound, ethyl loflazepate (ethyl-7-chloro-2, 3-dihydro-5-(2-fluorophenyl)-2-oxo-1H, 1, 4-benzodiazepine-3-carboxylate; CM-6912) was studied using in vitro experimental systems for its displacement activity on 3H-diazepam binding to the synaptosomal membrane fraction of rat cerebrum and potentiating action on GABA. CM6912 inhibited the specific binding of 3H-diazepam by 25%, 75% and 90% at concentrations of 0.01 μM, 0.1 μM and 1 μM, respectively, while its metabolites CM6913 and CM7116, at 0.1 μM, completely inhibited the binding. Concentrations for 50% inhibition (IC50) were 25 nM for CM6912, 3.2 nM for CM6913 and 1.4 nM for CM7116. These results suggest that the metabolite CM7116 is stronger than its parent compound in displacing the 3H-diazepam binding, and they also suggest that the long-lasting anti-anxietic action of CM6912 might be due to the in vivo formation of CM7116. CM6912, CM7116 and diazepam potentiated the suppressive action of GABA on spontaneous spikes of Purkinje cells in guinea pig cerebellar slices in a dose-dependent manner. Concentrations for 50% suppression (IC50) were 96.0 μM for GABA alone, 75.0 μM for GABA plus diazepam (5 μM), 78.9 μM for GABA plus CM6912 (5 μM) and 60.8 μM for GABA plus CM7116 (5 μM). These findings suggest that CM6912 and CM7116 may potentiate the postsynaptic inhibitory action of GABA in a manner similar to and probably more strongly than diazepam.抄録全体を表示PDF形式でダウンロード (491K) -
Yoshinobu TAKATA, Hitoshi KATO1985 年 37 巻 4 号 p. 381-394
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーEffects of verapamil, diltiazem and nicardipine on tritium overflow and contraction evoked by 40 mM KCl were evaluated using canine saphenous vein strips preloaded with [3H]norepinephrine. Phentolamine, 10-6 M, almost completely inhibited the contraction induced by KCl, while it significantly enhanced the evoked tritium overflow. These responses to KCl were dependent on external Ca2+. All Ca antagonists tested significantly increased the spontaneous tritium overflow in a concentration-dependent manner without any changes in basal tension. Verapamil at 10-6 M significantly inhibited the contraction with no significant effect on the evoked overflow; and at concentrations above 10-5 M, it inhibited the contraction much more strongly than the evoked tritium overflow. Diltiazem and nicardipine at concentrations above 3×10-6 M significantly inhibited both tritium overflow and contraction evoked by KCl. A significant correlation between inhibitions of both responses to KCl by the three Ca antagonists was observed, although the y-intercept and slope of the regression line for verapamil obtained by plotting the inhibition of the KCl-evoked contraction as a function of the inhibition of the evoked tritium overflow were greater than those for the other two antagonists. The inhibitory effects of verapamil and diltiazem on the tritium overflow and contraction evoked by KCl were not related to their local anesthetic activities. Neither the increase in the spontaneous tritium overflow nor inhibitions of the evoked tritium overflow and contraction by nicardipine were related to its phosphodiesterase inhibiting activity. These results suggest that diltiazem and nicardipine may inhibit the KCl-evoked contraction mainly by inhibiting Ca2+-dependent transmitter release from the nerve endings, while verapamil may inhibit it by acting on the postsynaptic sites and at the relatively higher concentrations used, by further inhibition of transmitter release.抄録全体を表示PDF形式でダウンロード (1041K) -
Masayasu KIMURA, Ikuko KIMURA, Hiroshi NOJIMA1985 年 37 巻 4 号 p. 395-399
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーTwitch tensions of indirectly stimulated diaphragm muscles of mice were blocked by a combination of paeoniflorin (PF) and glycyrrhizin (GLR). The mechanism of this effect was studied electropharmacologically. When twitch responses were completely prevented, miniature end-plate, end-plate, and muscle action potentials were still observed when PF and GLR were combined, suggesting that the mechanism is postsynaptic. Potential amplitudes induced by acetylcholine (ACh), which was injected iontophoretically, were inhibited by about 70% by PF (25 μg/ml) plus GLR (75 μg/ml), although neither agent alone caused an inhibition. The combined ratio (PF:GLR=1:3) by concentrations (g/ml) potentiated both the inhibition of ACh potential amplitudes and the depolarization of resting membrane potentials. These results indicate that the effect of combined PF and GLR is to depolarize the muscle membrane and to block ACh-receptor-linked processes. In chemically skinned (saponin-treated) muscles, the tension induced by 0.39 μM of free calcium was inhibited by PF (300 μg/ml), but it tended to be increased by GLR (300 μg/ml). Caffeine-induced contractures in the skinned muscles was not influenced by PF, and they tended to be decreased with GLR treatment. Thus, in muscles with sustained depolarization, these combined compounds seem to block intracellular Ca2+ movement.抄録全体を表示PDF形式でダウンロード (386K) -
Mikio ITO, Akira FUJII, Yoshio SUZUKI1985 年 37 巻 4 号 p. 401-404
発行日: 1985年
公開日: 2006/11/07
ジャーナル フリーThe effects of dried aluminium hydroxide gel on the healing of rat acetic acid ulcer were studied in comparison to those of propantheline bromide by the method of histological measurements. Dried aluminium hydroxide gel not only decreased the macroscopic ulcer index and the defective area in the ulcerated region but also increased the decreasing index of exposed ulcer floor and the mucosal regeneration index without affecting the thickness of the ulcer base and the development index of collagen fibers. However, propantheline bromide did not have any beneficial effects.抄録全体を表示PDF形式でダウンロード (218K)
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