巻号一覧
100 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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田村 善蔵1980 年 100 巻 4 号 p. 359-374
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe development and clinical use of methods for the determination of catecholamines, their metabolites and dopa in biological materials, by use of gas chromatography, high performance liquid chromatography and immunoassay, were summarized.抄録全体を表示PDF形式でダウンロード (1142K) -
村岡 敬治, 市川 正孝, 久野 拓造1980 年 100 巻 4 号 p. 375-385
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリー2-(1-Oxido-2-pyridinio)-3-phenyl-4 (3H)-quinazolinone (1), 2-(1-oxido-2-pyridinio)-3-phenyl-4 (3H)-quinazolinone 1-oxide (4) and their control compounds, 3-phenyl-2-(2-pyridyl)-4 (3H)-quinazolinone (6) were nitrated under appropriate conditions, to give 3-(3-nitrophenyl)-2-(1-oxido-2-pyridinio)-4 (3H)-quinazolinone (2), 3-(3-nitrophenyl)-2-(1-oxido-2-pyridinio)-4 (3H)-quinazolinone 1-oxide (5) and 3-(3-nitrophenyl)-2-(2-pyridyl)-4 (3H)-quinazolinone (7) as mononitro-derivatives or 6-nitro-3-(3-nitrophenyl)-2-(1-oxido-2-pyridinio)-4 (3H)-quinazolinone (3) and 6-nitro-3-(3-nitrophenyl)-2-(2-pyridyl)-4 (3H)-quinazolinone (8) as dinitro-derivatives, selectively and in comparatively higher yield. Next, compound (6) was halogenated with bromine, NBS and NCS by varying reaction temperature and concentration of sulfuric acid, and by adding silver sulfate as an activator, to give 3-(3-bromophenyl)-2-(2-pyridyl)-4 (3H)-quinazolinone (10) and 6-bromo-3-phenyl-2-(2-pyridyl)-4 (3H)-quinazolinone (12) as monohalogenides and 3-(3, 4-dibromophenyl)-2-(2-pyridyl)-4 (3H)-quinazolinone (11), or 6-bromo-3-(3-bromophenyl)-2-(2-pyridyl)-4 (3H)-quinazolinone (13) as dihalogenides, and further to give a derivative which was presumed to be a trihalogenide.抄録全体を表示PDF形式でダウンロード (1038K) -
服部 禎一, 浅川 直樹, 上山 政晤, 篠田 愛信, 三宅 康夫1980 年 100 巻 4 号 p. 386-388
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーGood separation of Vitamin B12 analogues (mecobalamin, cobamide, cyanocobalamin and hydroxocobalamin) by reversed phase high performance liquid chromatography was studied using a 37% methanol-0.04M tartaric acid-Na2HPO4 buffer (pH 3.0) mixture as mobile phase.抄録全体を表示PDF形式でダウンロード (341K) -
西條 成良, 和田 征夫, 野口 勝通, 村木 正義, 石田 昭彦, 日水 順一1980 年 100 巻 4 号 p. 389-395
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーSynthesis of 8-azaprostanoids (1a-e and 15a-e) from 5-hydroxymethyl-2-pyrrolidinone (3) was described. Acetylation of 3 and subsequent alkylation with methyl 7-iodoheptanoate yielded N-alkylated compound (7), which was converted into 5-hydro-xymethyl derivative (10) after selective hydrolysis. The same compound (10) was also conveniently prepared from 3 after ethoxyethylation and alkylation followed by treatment with acidic methanol. The Collins oxidation of 10 provided an aldehyde (11) which served as a key intermediate. The wittig reaction of 11 with various dimethyl 2-oxo-phosphonates yielded the corresponding enones (12a-e), which were reduced by sodium borohydride, followed by the separation of C15-epimers and alkaline hydrolysis, to give moderate yields of 1a-e, and 15a-e.抄録全体を表示PDF形式でダウンロード (864K) -
西本 喜重, 加藤 礼子, 林 信一1980 年 100 巻 4 号 p. 396-401
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe determination of tropane alkaloids (atropine and scopolamine), contained in gastrointestinal drugs and scopolia roots, was studied using a gas chromatograph equipped with a flame thermoionic detector with specific sensitivity to nitrogenous compounds. Dexil 300 GC, Silicone OV-17 and Thermon 1000 were used for the stationary phase. Homatropine to Dexil 300 GC and Silicone OV-17, and diphenhydramine to Thermon 1000 gave good results as an internal standard substance. Between the peak height ratio of alkaloids to the internal standard substance and the alkaloid contents, a linear response at the range 25 to 75 ng atropine and 2.5 to 7.5 ng scopolamine was recognized. The determination of atropine and scopolamine in gastrointestinal drugs and scopolia roots was easily carried out by this method without any interference.抄録全体を表示PDF形式でダウンロード (568K) -
岩田 修造, 大谷 淑郎, 長田 永三郎, 荻野 尚1980 年 100 巻 4 号 p. 402-406
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーBecause the cornea forms an important boundary tissue in the anterior eye portion, the corneal permeability of ophthalmic drugs is of great importance in drugs administered topically. To evaluate the intraocular penetration of bupranolol, an antiglaucoma ophthalmic solution, its in vitro corneal permeability was examined, using excised rabbit cornea mounted on the methacrylate chamber. Permeation time was carried out within 10-30 minutes at 35°. Permeability constants were calculated from measuring the initial amount of bupranolol (C0), the residual amount of bupranolol in the tear-side chamber (C1), the concentration in the aqueous-side chamber (C2), thickness of the cornea (Δχ) and corneal permeation area (A) after each permeation time. In both, tissue culture medium and ophthalmic solution, the constant of corneal permeable velocity (K) and permeability constant of the membrane (P) of bupranolol increased with permeation time, and those values did not depend on bupranolol concentration. The present results suggest that the bupranolol compound at the precorneal pocket penetrates into the intraocular area through the cornea.抄録全体を表示PDF形式でダウンロード (667K) -
野上 祐喜, 宮村 靖子, 黒部 明, 小川 貫山, 宮本 重夫, 小泉 保1980 年 100 巻 4 号 p. 407-414
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe metabolism of ST-2121 was investigated in rat urine after subcutaneous administration of 14C-labeled and non-labeled compounds. The metabolites were characterized by radio-thin-layer chromatography and gas chromatography-mass spectrometry. ST-2121 (M-I), 9, 10-dihydroxy-1, 4-dimethyl-2, 3, 4, 5, 6, 7-hexahydro-1, 6-methano-1H-4-benzazonine (M-II), 9-hydroxy-10-methoxy (or 9-methoxy-10-hydroxy)-1, 4-dimethyl-2, 3, 4, 5, 6, 7-hexahydro-1, 6-methano-1H-4-benzazonine (M-III), 10-hydroxy-1-methyl-2, 3, 4, 5, 6, 7-hexahydro-1, 6-methano-1H-4-benzazonine (M-IV) and their glucuronides were identified. d-, l- or dl-ST-2121 was administered to rats and M-I, M-II, M-III and M-IV excreted in the urine were determined by mass fragmentography. Remarkable differences were observed between d- and l-isomers with respect to the excretion rate of M-I, M-II and M-III, however, the excretion rate of M-IV was the same among the optical isomers.抄録全体を表示PDF形式でダウンロード (680K) -
稲垣 承二, 住田 克己, 北澤 式文, 広瀬 信吾1980 年 100 巻 4 号 p. 415-419
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーComplementary Tristimulus Colorimetry (CTS) was applied in dissolution tests of multi-ingredient tablets. In the test, internal standards were used for improved accuracy. Two kinds of internal standard situations were studied, in one, the absorption spectra of tablet components and the internal standard overlapped, and in the other, they did not. In the latter situation, carbazochrome sodium sulfonate, and in the former, chloperastine hydrochloride was used as the internal standard for the dissolution test of EA tablets which contained aspirin and ascorbic acid. Our results indicate that the internal standard method is useful in the dissolution test.抄録全体を表示PDF形式でダウンロード (574K) -
田川 美恵子, 中垣 正幸, 渡辺 昌1980 年 100 巻 4 号 p. 420-426
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe effect of L-alanine on dispersion and coagulation of ferric hydroxide sol was investigated by optical measurement of the coagulation rate. Ferric hydroxide sol was prepared by pouring a ferric chloride solution into boiling water. A small quantity of sodium hydroxide solution was added to the sol, and the coagulation rate was monitored based on the change in turbidity with time. The turbidity change vs. pH showed a maximum at the point of zero charge, which was obtained by electrophoretic mobility measurements of the ferric hydroxide sol particles. The maximum of the turbidity cnange vs. pH curve shifted towards the iso-electric point of L-alanine by the addition of this agent. The change of the point of zero charge was also observed by electrophoresis when L-alanine was added to the sol. L-Alanine was found to be an effective dispersing agent for ferric hydroxide particles at pH 2-8, and its effectiveness was enhanced by the presence of sodium chloride.抄録全体を表示PDF形式でダウンロード (701K) -
南雲 清二, 伊沢 一男, 東山 公男, 永井 正博1980 年 100 巻 4 号 p. 427-433
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーA bitter principle glucozaluzanin C (I) of Pertya robusta (Compositae) was isolated together with β-sitosterol, oleanolic acid, ursolic acid, chlorogenic acid and β-sitosteryl glucoside. The chemical structure of I was determined to be 3β-hydroxy-1αH, 5αH, 6βH, 7αH-guaian-4 (5), 10 (14), 11 (13)-triene-6, 12-olide-3β-D-glucopyranoside on the basis of chemical and spectral evidence.抄録全体を表示PDF形式でダウンロード (772K) -
渋谷 眞也, 長澤 哲郎, 横澤 隆子, 大浦 彦吉1980 年 100 巻 4 号 p. 434-442
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe effect of intraperitoneal administration of rhubarb extract (5 mg/rat) on urea nitrogen and amino acid metabolism in rats was investigated. Urea nitrogen concetrations were decreased by 21% in the liver at 8 hr and by 46-51% in the kidney at 4-8 hr after treatment. The excretion of urea and ammonia in the urine was not different from the control values and ammonia nitrogen concentrations in peripheral blood, the portal vein, liver and kidney were not different. On the other hand, in rats treated with rhubarb extract, α-amino acid nitrogen concentration in serum was significantly decreased by 20-36% at 2-8 hr. Seven amino acid concentrations in the plasma were decreased Gln (31%), Ala (51%), Gly (29%), Ser (26%), Glu (31%), Met (39%), and Arg (25%) and 3 amino acid concentrations in the liver were significantly decreased Gln (31%), Glu (42%), and Asp (45%) at 2 hr after the treatment. With respect to the net balance of plasma amino acids across various organs at 2 hr after the administration, release of Gln from the liver was decreased by 40% and the uptake of Gln by non-hepatic visceral organs was decreased by 44%.抄録全体を表示PDF形式でダウンロード (918K) -
東野 正男, 山本 正, 梶川 憲雄, 尾藤 龍哉1980 年 100 巻 4 号 p. 443-451
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーBefunolol was transformed to 11 metabolites along the following three major metabolic pathways by rabbit hepatic 9000×g supernatant : (i) reduction of 2-ketone·carbonyl ; (ii) 4-hydroxylation of benzofuran ring ; (iii) oxidation of 7-side chain. Only one metabolite (reduction product of befunolol ; MI) was formed after incubating befunolol with rabbit hepatic cytosol. The same liver fraction also converted MI to befunolol in the presence of NADP+. The befunolol-reducing activity in the cytosol utilized NADPH more effectively than NADH. Optimum pH was approximately 7 and the apparent Km value was 0.81 mM. The reducing activity was competitively inhibited by the presence of microsome, including other befunolol-metabolizing activities such as 4-hydroxylating activity. In hamsters, befunolol-4-hydroxylating activity varied remarkably by treatment with SKF 525-A, CCl4 or phenobarbital, whereas the befunolol-reducing activity was little affected by the same treatment. In vivo formation of befunolol from MI was recognized in rabbits, rats and guinea pigs.抄録全体を表示PDF形式でダウンロード (957K) -
五味田 裕, 内門 昭久, 森山 峰博, 市丸 保幸, 川崎 博己, 野中 源一郎, 西岡 五夫1980 年 100 巻 4 号 p. 452-456
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe pharmacological effects of water-soluble and insoluble fractions extracted from Zingiber mioga ROSCOE were examined in mice and rats. In mice, Fr-W1, Fr-2 and Fr-W4 in water-soluble fraction significantly prolonged the sleeping time after thiopental Na administration. Intracranial self-stimulation behavior in rats was also depressed by Fr-W1 and Fr-W4. These results suggest the possible existence of some substances that exert central nervous depressive action in these fractions.抄録全体を表示PDF形式でダウンロード (613K) -
富永 義則, 肥田木 省三, 松田 芳郎, 小林 五郎, 酒見 寛郎1980 年 100 巻 4 号 p. 456-459
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーTreatment of methyl 2-(1-cyano-2-methylthio-2-p-tolylsulfonylaminoethenyl) benzoate (III), prepared from N-bis (methylthio) methylene-p-tolylsulfonamide (Ia) and o-methoxycarbonylphenylacetonitrile (II) in the presence of sodium hydride with hydrochloric acid, yielded 4-cyano-1, 2-dihydro-3-methylthioisoquinolin-1-one (V). Similarly, the reaction of II with N-bis (methylthio) methylenecyanamide (Ib) afforded a good yield of 2, 4-dicyano-1, 2-dihydro-3-methylthioisoquinolin-1-one (IV). Compound III reacted with ethanolamine, benzylamine, and hydrazine hydrate to give the corresponding 3-amino-4-cyano-1, 2-dihydroisoquinolin-1-ones (VIIa, b) and 1-amino-4, 5-dihydro-p-tolysulfonylpyrazolo [3, 4-c] isoquinolin-5-one (VIII). The reaction of III with o-phenyl-enediamine and ethylenediamine gave good yields of the corresponding benzimidazo [2, 1-b] isoquinolin-7-one (IX) and imidazo [1, 2-b] isoquinolin-5 (5H)-one (X).抄録全体を表示PDF形式でダウンロード (504K) -
岡本 光美, 山田 不二造1980 年 100 巻 4 号 p. 460-465
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーThe trace amount of β-naphthylamine (β-NA) co-existing with a large amount of α-naphthylamine (α-NA) was determined with high accuracy and sensitivity by high speed liquid chromatography after mesitylenesulfonylation (Ms-). By elution with methanol/acetonitrile/pH 4.6, 0.1M sodium acetate buffer (54 : 6 : 40 v/v) on an ODS column, the resolution between Ms-α-NA and Ms-β-NA peaks was 3.43. A more accurate detection of Ms-β-NA than of Ms-α-NA was possible at approximately 240 nm using an ultraviolet monitor. With this method, the amount of Ms-β-NA was determined within 1.1% error over the range from 0.005 to 10μg, and the limit of detection was 0.005μg.抄録全体を表示PDF形式でダウンロード (604K) -
高木 修造, 山木 正枝, 増田 京子1980 年 100 巻 4 号 p. 466-467
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーLipophilic constituents of the fruits of Rosa multiflora THUNB., a purgative drug, were investigated and β-sitosterol, 5α-stigmastan-3, 6-dione, scoparone, salicylic acid were identified.抄録全体を表示PDF形式でダウンロード (356K) -
土屋 悦輝, 松本 淳彦, 首藤 絋一, 岡本 敏彦1980 年 100 巻 4 号 p. 468-471
発行日: 1980/04/25
公開日: 2008/05/30
ジャーナル フリーTen strains of Actinomycetes producing, earthy-musty odor were isolated from the bottom sediment in Chidorigafuchi, the moat of the Imperial Palace. Their volatile metabolites were identified by gas chromatography-mass spectrometry. The Actinomycetes were cultured at 28°for 14 days on oatmeal agar and the cultured media were subjected to steam distillation to recover volatile metabolites. 2-Methylisoborneol and Geosmin were found in all cultured media, ranging from trace to 3000μg/254cm2. Newly identified Germacrene-D was found in all Actinomycetes, ranging from trace to 78μg/254cm2.抄録全体を表示PDF形式でダウンロード (448K)
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