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Volume 100, Issue 4
Displaying 1-17 of 17 articles from this issue
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ZENZO TAMURA1980 Volume 100 Issue 4 Pages 359-374
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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.View full abstractDownload PDF (1142K) -
KEIJI MURAOKA, MASATAKA ICHIKAWA, TAKUZO HISANO1980 Volume 100 Issue 4 Pages 375-385
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS2-(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.View full abstractDownload PDF (1038K) -
TEIITI HATTORI, NAOKI ASAKAWA, MASAAKI UEYAMA, AISHIN SHINODA, YASUO M ...1980 Volume 100 Issue 4 Pages 386-388
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSGood 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.View full abstractDownload PDF (341K) -
SHIGEYOSHI SAIJO, MASAO WADA, KATSUYUKI NOGUCHI, MASAYOSHI MURAKI, AKI ...1980 Volume 100 Issue 4 Pages 389-395
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSynthesis 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.View full abstractDownload PDF (864K) -
NOBUSHIGE NISHIMOTO, REIKO KATO, SHINICHI HAYASHI1980 Volume 100 Issue 4 Pages 396-401
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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.View full abstractDownload PDF (568K) -
SHUZO IWATA, YOSHIRO OHTANI, EIZABURO OSADA, HISASHI OGINO1980 Volume 100 Issue 4 Pages 402-406
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBecause 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.View full abstractDownload PDF (667K) -
YUKI NOGAMI, YASUKO MIYAMURA, AKIRA KUROBE, MICHITAKA OGAWA, SHIGEO MI ...1980 Volume 100 Issue 4 Pages 407-414
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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.View full abstractDownload PDF (680K) -
SHOJI INAGAKI, KATSUMI SUMITA, SHIKIFUMI KITAZAWA, SHINGO HIROSE1980 Volume 100 Issue 4 Pages 415-419
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSComplementary 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.View full abstractDownload PDF (574K) -
MIEKO TAGAWA, MASAYUKI NAKAGAKI, AKIRA WATANABE1980 Volume 100 Issue 4 Pages 420-426
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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.View full abstractDownload PDF (701K) -
SEIJI NAGUMO, KAZUO IZAWA, KIMIO HIGASHIYAMA, MASAHIRO NAGAI1980 Volume 100 Issue 4 Pages 427-433
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA 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.View full abstractDownload PDF (772K) -
SHINYA SHIBUTANI, TETSURO NAGASAWA, TAKAKO YOKOZAWA, HIKOKICHI OURA1980 Volume 100 Issue 4 Pages 434-442
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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%.View full abstractDownload PDF (918K) -
MASAO TOHNO, TADASHI YAMAMOTO, NORIO KAJIKAWA, TATSUYA OFUJI1980 Volume 100 Issue 4 Pages 443-451
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBefunolol 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.View full abstractDownload PDF (957K) -
YUTAKA GOMITA, AKIHISA UCHIKADO, MINEHIRO MORIYAMA, YASUYUKI ICHIMARU, ...1980 Volume 100 Issue 4 Pages 452-456
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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.View full abstractDownload PDF (613K) -
YOSHINORI TOMINAGA, SHOZO HIDAKI, YOSHIRO MATSUDA, GORO KOBAYASHI, KAN ...1980 Volume 100 Issue 4 Pages 456-459
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTreatment 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).View full abstractDownload PDF (504K) -
MITSUYOSHI OKAMOTO, FUJIZO YAMADA1980 Volume 100 Issue 4 Pages 460-465
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe 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.View full abstractDownload PDF (604K) -
SHUZO TAKAGI, MASAE YAMAKI, KYOKO MASUDA1980 Volume 100 Issue 4 Pages 466-467
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSLipophilic 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.View full abstractDownload PDF (356K) -
YOSHITERU TSUCHIYA, ATSUHIKO MATSUMOTO, KOICHI SHUDO, TOSHIHIKO OKAMOT ...1980 Volume 100 Issue 4 Pages 468-471
Published: April 25, 1980
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTen 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.View full abstractDownload PDF (448K)
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