巻号一覧
34 巻 (1984)
- 4 号 p. 367-
- 3 号 p. 269-
- 2 号 p. 131-
- 1 号 p. 1-
34 巻, 4 号
選択された号の論文の17件中1～17を表示しています
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A.K. CHATTERJEE, U. SADHU, B.B. DALAL, T. CHATTERJEE1984 年 34 巻 4 号 p. 367-373
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーThe effect of deoxypyridoxine on the activities of drug-metabolizing enzymes was investigated in male rats. Phenylbutazone oxidase and aminopyrine N-demethylase decreased in both liver and kidney of deoxypyridoxine-treated rats that received either an 18% or 8% casein diet. However, the magnitude of decrease in activities was more when the rats received an 8% casein diet. The NADPH oxidase activity remained unchanged following deoxypyridoxine treatment. The diminished activities of phenylbutazone oxidase and aminopyrine N-demethylase noted after deoxypyridoxine treatment were restored by pyridoxine supplementation. The decreased activities of drug-metabolizing enzymes in deoxypyridoxine treated rats were not reversed by thyroxine supplementation. It is suggested that pyridoxine in the form of pyridoxal phosphate might be involved in the regulation of drug-metabolizing activities.抄録全体を表示PDF形式でダウンロード (489K) -
Hirokuni TAMATSU, Mikio NAKAZAWA, Shoichi IMAI, Hiroshi WATARI1984 年 34 巻 4 号 p. 375-379
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーUsing the 31P-topical nuclear magnetic resonance method (TMR), an attempt was made to determine the myocardial high-energy phosphate compounds (HEP) contents under in situ conditions in closed-chest animals, and the effects of opening the thorax on the myocardial energy metabolism were studied comparing the cardiotoxic effects of 5-fluorouracil (5-FU) in closed-chest and open-chest animals. It was found that the depletion of myocardial HEP produced by 5-FU was much more marked in open-chest animals than in closed-chest ones, indicating the necessity of conducting the experiments in closed-chest animals for the proper evaluation of the cardiotoxicity of certain types of compounds. Therefore, the cardiotoxicity of a prodrug of 5-FU was assessed in closed-chest animals, and it was found to be less cardiotoxic than 5-FU.抄録全体を表示PDF形式でダウンロード (326K) -
Keiichiro HAGA, Kunio OSUGA, Akira NAKANISHI, Tatsumi TSUMAGARI1984 年 34 巻 4 号 p. 381-387
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーEffect of the anti-anxiety drug clotiazepam on the experimental gastric ulceration induced by restraint and water-immersion stress or aspirin was studied in rats. Clotiazepam prevented the development of each gastric ulcer. From the effect of clotiazepam on aspirin-induced ulceration, we presumed that clotiazepam should have some other antiulcer mechanism in addition to its action on the central nervous system. There was an appreciable correlation between the decrease in the hexosamine level of gastric tissue and associated ulceration. After treatment with aspirin, the hexosamine level was abruptly reduced and was maintained at a low level for several hours. In the clotiazepam-pretreated group, the hexosamine level reduced by aspirin was progressively restored to the intact level. By histological examination with periodic acid-Schiff (PAS)/alcian-blue (AB) staining, clotiazepam increased the amount of gastric mucopolysaccharides decreased by aspirin. Clotiazepam did not affect gastric secretion in pylorus-ligated rats. Atropine and cimetidine inhibited ulceration induced by stress or aspirin and gastric secretion, but did not affect the hexosamine level reduced by aspirin. These results indicate that the antiulcer efficacy of clotiazepam may be attributed to its action not only on the central nervous system, but also on the mucus in gastric mucosa.抄録全体を表示PDF形式でダウンロード (750K) -
Kazumi IWAKI, Yukio YONETANI1984 年 34 巻 4 号 p. 389-396
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーIn order to evaluate the cause of diuretic-induced hyperuricemia which has been well documented in clinical studies, clearance experiments were performed in rats using furosemide and trichlormethiazide. The net flux in the tubular transport of uric acid was reabsorptive, and the fractional excretion of uric acid responded sensitively to the transtubular transport inhibitors, sodium probenecid and pyrazinoic acid. When the hemoconcentration was induced by highly potent doses of test diuretics, the inulin clearance and the fractional excretion of uric acid clearly decreased. The contraction of body fluid produced by intraperitoneal administration of polyethylene glycol resulted in marked decrease of inulin clearance and fractional excretion of uric acid. The decrease of uric acid excretory capacity under the treatment with trichlormethiazide was completely corrected by saline loading. Moreover, no significant change was found in the pyrazinoic acid-suppressible fractional excretion of uric acid between the diuretic-treated rats and the control animals. These studies suggest that furosemide and trichlormethiazide-induced changes in the renal handling of uric acid are mediated by the fluid volume contraction and that the decrease in fractional excretion of uric acid by test diuretics is the result of reabsorptive enhancement of uric acid.抄録全体を表示PDF形式でダウンロード (562K) -
Yoshinobu TAKATA, Hitoshi KATO1984 年 34 巻 4 号 p. 397-409
発行日: 1984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 transmural nerve stimulation (TNS) were evaluated using canine saphenous vein strips preincubated with [3H]norepinephrine. External Ca2+ was required for both tritium overflow and contraction evoked by TNS. All the Ca antagonists tested significantly increased the spontaneous overflow of tritium in a concentration-dependent manner with no changes in basal tension. Verapamil in concentrations lower than 10-5 M significantly enhanced the TNS-evoked tritium overflow, but reduced it at 3×10-5 M, while this drug at 3×10-6-3×10-5 M concentration-dependently inhibited the TNS-evoked contraction. Verapamil, 3×10-5 M, inhibited the TNS-evoked contraction more strongly than the evoked tritium overflow. On the other hand, diltiazem and nicardipine in concentrations higher than 10-5 M significantly inhibited both tritium overflow and contraction evoked by TNS. There was no significant difference between inhibitions of the TNS-evoked tritium overflow and contraction by either diltiazem or nicardipine. Neither increase in the spontaneous tritium overflow nor inhibitions of the TNS-evoked tritium overflow and contraction by nicardipine appeared to be related to its phosphodiesterase inhibiting activity. These results suggest that diltiazem and nicardipine may inhibit the TNS-evoked contraction mainly by inhibiting Ca2+-dependent transmitter release from the adrenergic nerve endings, whereas verapamil may inhibit it by restricting the availability of Ca2+ at the postsynaptic sites and in the highest concentration used, by additional inhibition of transmitter release.抄録全体を表示PDF形式でダウンロード (1023K) -
Hiroyasu SATOH, Keitaro HASHIMOTO1984 年 34 巻 4 号 p. 411-415
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーThe effects of nicorandil (SG-75) (3-500 μg/ml) on the membrane potential and currents of the rabbit sino-atrial node were studied using the voltage clamp technique. Low concentrations of nicorandil (3-10 μg/ml) increased the action potential duration (APD) and depolarized the maximum diastolic potential (DMP), but higher concentrations had no such effects and even decreased APD and tended to hyperpolarize MDP. Regardless of these effects, nicorandil decreased the heart rate concentration-dependently. On the current systems of the sinoatrial node, 3 μg/ml of nicorandil decreased the outward current (ik), but concentrations of over 10 μg/ml increased it. The voltage dependency of the steadystate activation of ik was unchanged. Nicorandil did not affect the inward current activated by hyperpolarization (Ih) and the slow inward current (is). These results suggest that the cardiac effects induced by nicorandil must have been produced by selective change in the conductance of ik.抄録全体を表示PDF形式でダウンロード (337K) -
Yasuhiko SASAKI, Takashi MORITA, Shigeyuki TAKEYAMA1984 年 34 巻 4 号 p. 417-427
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーIn vitro effects of the coronary vasodilator diltiazem on rat erythrocytes and liposomes were studied in comparison with propranolol and pentoxifylline. Diltiazem improved the deformability of rat erythrocytes, reduced the viscosity of rat erythrocyte suspensions, and protected the erythrocyte against hypotonic hemolysis at concentrations above 10-4 M, 10-5 M and 5×10-7 M, respectively. Diltiazem at 5×10-4 M also improved the impaired deformability of ATP-depleted erythrocytes, whereas it affected neither the adenine nucleotide level nor the phosphorylation of spectrin in the erythrocytes. Diltiazem enhanced the interaction of 1-anilino-naphthalene-8-sulfonate, a fluorescent probe, with erythrocyte ghosts at concentrations above 5×10-6 M and, above 5×10-5 M, inhibited the (Na++K+)-ATPase activity of the erythrocyte ghosts. Diltiazem reduced the microviscosity of both erythrocyte ghosts and liposomes prepared from rat erythrocyte lipids. Diltiazem induced aggregation of the liposomes prepared from rat erythrocyte lipids, phosphatidylserine or phosphatidylinositol, but it did not affect the liposomes prepared from a mixture of phosphatidylethanolamine and phosphatidylcholine (1:1). l-Diltiazem, a stereo-isomer of diltiazem, exhibited equipotent effects, compared with diltiazem, on these parameters. Propranolol showed similiar properties, but pentoxifylline shared none of the above properties, except that it improved the deformability of erythrocytes. From these results, it is suggested that diltiazem may affect the erythrocyte membrane by interacting with acidic phospholipids and thus reduce the microviscosity of the membrane, improve erythrocyte deformability and protects the erythrocyte against hypotonic hemolysis.抄録全体を表示PDF形式でダウンロード (877K) -
Haruyoshi IGARASHI, Yoko SATO, Setsuo HAMADA, Tohru KAWASAKI1984 年 34 巻 4 号 p. 429-434
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーTo elucidate the pharmacokinetics of local anesthetics with respect to corneal permeability in the rabbit, we examined the relationship between the corneal permeability velocities of three agents, cocaine·HCl, procaine·HCl and tetracaine· HCl and corneal hydration. The corneal permeability velocity constants (k) of these three ester-type local anesthetics were approximately 0.5-6.0×10-6 cm/sec and the membrane permeability constants of these agents were approximately 0.5-4.0×10-7 cm2/sec, whereas the rabbit corneal hydration values were 3.2-4.2. Tetracaine·HCl with the strongest topical anesthetic action showed the greatest corneal hydration and the smallest corneal permeability velocity constant among these local anesthetics. Rabbit corneal permeability decreased with increasing molecular length of the agents. Permeability of these local anesthetics in the rabbit cornea appears to result from passive transport. As corneal hydration values and the corneal permeability constant increased with greater topical anesthetic activity, it appears that the degree of inhibition of Na+-K+ ATPase activity is associated with the order of topical anesthetic activity in a similar manner as general anesthetics.抄録全体を表示PDF形式でダウンロード (383K) -
Takeshi SHIBUYA, Richard FIELD, Yasuo WATANABE, Katsuhiko SATO, Bernar ...1984 年 34 巻 4 号 p. 435-440
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーSeveral new benzodiazepines were studied with respect to their ability to bind specifically to benzodiazepine receptor sites in rat cerebral cortex membrane fraction. The IC50 values of new benzodiazepines were compared to that of diazepam. A group of triazolo-[1, 4] benzodiazepines displaced 3H-diazepam very effectively. The most potent of this group was brotizolam. Its potency was about ten times higher than that of diazepam. In this study, camazepam, which differs from diazepam in its C-3 substitution, had the lowest affinity to the benzodiazepine receptor site. This potency was about 0.006 that of diazepam. CM 7116 bound with the highest affinity to the benzodiazepine receptor site among the metabolites of CM 6912. The length of the side chain at the C-3 position of this compound is shorter than that of the other metabolites of CM 6912. These results indicated that the long side chain at the C-3 position might inhibit a close interaction between the receptor site and the substrate molecule, thereby leading to low-affinity binding.抄録全体を表示PDF形式でダウンロード (393K) -
Tsutomu SUZUKI, Mitsuya SHIMADA, Toshio YOSHII, Saizo YANAURA1984 年 34 巻 4 号 p. 441-446
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーThe developmental process of physical dependence on codeine has been explored in rats treated with codeine-admixed food (0.5 mg/g food) during 1 to 7 days. In rats treated with codeine for more than 2 days, body weight loss was markedly observed after the abrupt codeine withdrawal. The intensity and time course of body weight loss increased according to the duration of codeine treatment. After the codeine withdrawal, behavioral signs such as diarrhea, ptosis and vocalization were observed. In the naloxone-precipitated withdrawal test, rats treated with codeine for 1 day manifested a loss of body weight after naloxone challenge, and the intensity of body weight loss increased according to the duration of codeine treatment. After naloxone injection, the codeine-treated rats showed abnormal behaviors such as diarrhea, ptosis, teeth chattering, salivation, body shakes, vocalization, nose bleed, irritability, lacrimation and writhing. The total score, evaluated by the ranking system for precipitated withdrawal behaviors, was correlated with the duration of codeine treatment. These results suggest that naloxone-precipitated withdrawal signs are powerful in comparison with that after codeine withdrawal, and the weight loss is a common index for quantitative assessment of physical dependence on narcotics in the natural and naloxone-precipitated withdrawal tests. It is concluded that the drug-admixed food ingestion method has the advantage of rapidly inducing a high degree of physical dependence on codeine.抄録全体を表示PDF形式でダウンロード (415K) -
Kyozo YAMANAKA, Shizuo YAMADA, Satoru HAYASHI, Eiichi HAYASHI1984 年 34 巻 4 号 p. 447-455
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーEffects of chlorpromazine, metals and I-ascorbic acid (AA) on Ca2+-ATPase and Mg2+-ATPase in microsomal and granular fractions obtained from the bovine adrenal medulla were studied. Marker enzyme analysis on microsomal subfractions in a discontinuous sucrose density gradient showed a correlation of distribution between ATPase activities and plasma membrane. The two ATPase activities in such plasma membrane-rich microsomes were reduced by chlorpromazine, Hg2+ and Cu2+ (0.3 mM of each), and their effects were greater on the Mg2+-ATPase activity. Zn2+(0.3 mM) also reduced only the Mg2+-ATPase activity. AA (3 mM) reduced the two ATPase activities to an equal extent. Nevertheless, the inhibitions of ATPases by Hg2+, Cu2+ and Zn2+ were decreased, unaltered and additively enhanced in combination with AA, respectively. We also observed high Mg2+-ATPase activity in the granule-rich fraction, but this ATPase activity was unaffected by all of the above agents. These results indicate that Mg2+-ATPase in the plasma membrane-rich microsome of adrenal medulla is inhibited by chlorpromazine, Hg2+, Cu2+ and Zn2+ more significantly than Ca2+-ATPase, but Mg2+-ATPase in the granular fraction is unaffected, and that AA changes the potency of inhibition by some metals of ATPases diversely.抄録全体を表示PDF形式でダウンロード (660K) -
Che SU, Takao KUBO1984 年 34 巻 4 号 p. 457-463
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーThe modulation of vascular adrenergic neurotransmission in the spontaneously hypertensive rat (SHR) and Wistar-Kyoto rat (WKY) mediated by alpha-adrenoceptor and prostaglandin E2 (PGE2) were evaluated. The pressor responses of the perfused mesenteric vascular bed to perivascular adrenergic nerve stimulation (NS) and infusion of norepinephrine (NE) and the NS-induced 3H-efflux in preparations pretreated with 3H-norepinephrine were determined. In both SHR and WKY, a selective alpha2 agonist, B-HT 920 (30-300 nM), inhibited neurogenic vasoconstriction, and B-HT 920 (100-300 nM) potentiated the pressor response to NE in a dose-dependent manner. The effects of B-HT 920 did not significantly differ in SHR and WKY. Another alpha2 agonist, clonidine (100 nM), decreased the 3H-efflux approximately by 30% both in SHR and WKY. A selective alpha2 blocking agent, yohimbine (3-300 nM), potentiated the neurogenic vasoconstriction and inhibited the pressor response to NE equally in SHR and WKY. No difference in enhancement of 3H-efflux by yohimbine (30-300 nM) was seen between SHR and WKY either in the absence or presence of cocaine (10 μM) and metanephrine (20 μM). PGE2 (0.1-1 μM) potentiated pressor responses to NS and NE in SHR and WKY, but this compound (1 μM) did not affect the NS-induced 3H-efflux in either group of rats. It appears that adrenergic neurotransmission is inhibited presynaptically via an alpha2 receptor mechanism and facilitated postsynaptically by PGE2 in the rat mesenteric vascular bed. The hypertensive state in SHR can not be accounted for by alteration of these modulator mechanisms.抄録全体を表示PDF形式でダウンロード (514K) -
Shigetoshi CHIBA, Miyoko TSUKADA1984 年 34 巻 4 号 p. 465-467
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (217K) -
Yasushi WADA, Masaki NAKAMURA, Hiroshi KOGO, Yoshio AIZAWA1984 年 34 巻 4 号 p. 468-470
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (206K) -
Takeki TSUTSUI, Nobuko SUZUKI, Heiji MAIZUMI1984 年 34 巻 4 号 p. 471-474
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (341K) -
Seitaro OHKUMA, Jun-ichi TAMURA, Kinya KURIYAMA1984 年 34 巻 4 号 p. 475-479
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (407K) -
Toshio SUWA, Kiyomi FUKUSHIMA, Kazuaki KYOGOKU, Yo MORI1984 年 34 巻 4 号 p. 480-482
発行日: 1984年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (187K)
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