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Volume 22, Issue 3
Displaying 1-39 of 39 articles from this issue
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YOSHIKI HAMADA, ISAO TAKEUCHI, MINORU HIROTA1974 Volume 22 Issue 3 Pages 485-492
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1, 9-Diazaanthracene (IV), 4-methyl-1, 9-diazaanthracene (V), 4, 6-phenanthroline (I), 1, 6-phenanthroline (III), and 5-methyl-1, 6-phenanthroline (II) were synthesized by the reaction of 2-, 3-, or 4-aminoquinolines with glycerol or methyl vinyl ketone, in the presence of sulfo-mix, ferrous sulfate, and boric acid. Methylation of I with methyl iodide afforded the monomethiodide (VI) in which methyl iodide was proved to have reacted with the nitrogen in 6-position. Chichibabin amination of I afforded 5-amino-4, 6-phenanthroline (VIII) and this amination was examined by comparison of reaction indices by the Huckel molecular orbital method.View full abstractDownload PDF (832K) -
JUTARO OKADA, YOSHINOBU FUKUMORI1974 Volume 22 Issue 3 Pages 493-499
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo compare the compaction behavior of potassium chloride and lactose powder of 42 to 65 mesh, they were compressed under the constant pressure of upper punch (about 1000 kg/cm2 in the maximum) by compaction apparatus with a cylindrical die (8.02 mm inside diameter), in which the powder of constant net volume (0.7545 cm3) was filled. During the compression continued for ten hours, the thickness of powder bed and the pressure transmitted to lower punch were measured. And then the replicated surfaces of compacts were observed by microscope so as to examine the packing structure. In the case of potassium chloride powder, under the lower pressure than the critical pressure which exists between 391 and 625 kg/cm2, particles seem to be deformed plastically in appearance. Under the higher pressure than the critical pressure, many fragments or cracks are produced and these small fragments move to fill up voids very closely, as if original particles were deformed plastically. Therefore the values of the porosity of powder bed and the ratio of lower to upper punch pressure approach to zero and 100%, respectively. In the case of lactose powder, as particles are brittle, they are fractured and small voids are filled with the fragments. The thickness and the ratio take the almost constant values after about five hours in spite of considerable amounts of void left still.View full abstractDownload PDF (1082K) -
TAKASHI HIRAOKA, JUN SERIZAWA1974 Volume 22 Issue 3 Pages 500-504
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA correlation between the ear temperature-lowering effect and blood level was investigated in rabbits and dogs after oral administration of two different dosage forms of ethylphenylephrine ; an uncoated tablet which showed a rapid dissolution rate in vitro test and a sustained release capsule that showed a gradual dissolution rate. The urinary excretion was also examined in dogs and men after the oral administration of two dosage forms. Absorption of the drug from the uncoated tablet was more rapid than that from the sustained release capsule in rabbits, dogs, and men. Absportion from the sustained release capsule extended over a long period. The ear temperature-lowering effect was well correlated with the blood level after the oral administration of two dosage forms in rabbits. No correlation was observed between the effect and the blood level in dogs ; the effect was weak in spite of the fast rise of the blood level in early stage after the administration of both dosage froms. About 70% of the dose during 48 hr period in dogs and 80% of the dose during 24 hr period in men were recovered in the urine after the administration of either the uncoated tablet or the sustained release capsule. About 60% of the total amount excreted in the urine was recovered as free ethylphenylephrine in dogs, but no free ethylphenylephrine was detected in human urine.View full abstractDownload PDF (590K) -
HIROSHI NAGASE1974 Volume 22 Issue 3 Pages 505-513
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-Cyanomethyl-2-thioxo-4-aminothiazolines (II) were prepared by the addition reaction of dithiocarbamates to fumaronitrile. In the reactions of bis (methylthio) maleonitrile (IXa), bis (benzylthio) maleonitrile (IXb), 2, 3-dicyano-5, 6-dihydro-1, 4-dithiin (IXc) and 4, 5-dicyano-2-oxo-1, 4-dithiole (IXd) with dithiocarbamates were obtained 5, 5'-bi-2-thioxo-4-aminothiazolines (X). The 4-amino groups of II and X were found to be labile and were hydrolyzed when heated with mineral acids to give 5-cyanomethyl-2-thioxo-4-thiazolidones (III) and 5, 5'-bi-2-thioxo-4-thiazolidones (XII), respectively. X was also found to be converted to Δ5, 5'-bi-2-thioxo-4-iminothiazolidine (XI) by autoxidation in the presence of catalytic amount of triethylamine. 4-Oxo-4'-imino-Δ5, 5'-bi-2-thioxo-thiazolidine (XVI) was prepared by the addition reaction of N-benzyldithiocarbamate to 5-cyanomethylidene-2-thioxo-4-thiazolidone (XIV). XI and XIV gave Δ5, 5'-bi-2-thioxo-4-thiazolidones (XIII) on hydrolysis with mineral acids.View full abstractDownload PDF (909K) -
YASUNOBU SATO, TERUO TANAKA, SEIJI KUMAKURA, HIROYUKI KOIKE, TAKESHI O ...1974 Volume 22 Issue 3 Pages 514-522
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-[p-(Aminoalkoxy) anilino] tropone derivatives were prepared from 2-(p-hydroxyanilino) tropone derivatives by established synthetic procedures and were tested for β-adrenergic blocking, coronary vasodilating, and anti-hypertensive activities. Some members of the series exhibited significant activities in one or more of the pharmacological tests, and introduction of a halogen atom into the 5-position of the tropone nucleus caused generally an increase in the pharmacological activities.View full abstractDownload PDF (831K) -
AKEMI KANEDA, KAYOKO NISHIMURA, SHOZO MURANISHI, HITOSHI SEZAKI1974 Volume 22 Issue 3 Pages 523-528
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffect of Polysorbate 80 on the intestinal absorption of nine micelle-free drugs was examined in the rat. Regardless of the ionic nature of the compounds, two levels of the effect were observed, namely an absorption enhancing effect at relatively low concentration range and a small inhibitory effect at higher concentrations of the surfactant. Pretreatment of the gut with the surfactant, mucosal uptake, and other absorption experiments revealed that the surfactant adsorbed onto the mucosal surface exerted an absorption modifying effect. Absorption promoting and inhibiting effects may be operative at the same time within the concentration range of the surfactant investigated and the observed net absorption modifying effect dependent on the relative magnitude of each. Absorption enhancing effect was dependent on the surfactant-mucosal surface contact time and increased steadily with the time after pretreatment with Polysorbate 80. Absorption studies on sulfisoxazole from the different segments of the intestine provided evidence that the enhancing effect of Polysorbate 80 could be explained by the degree of saturation of the surfactant on the mucosal surface regardless of the regions of the intestine.View full abstractDownload PDF (736K) -
SHUNSAKU NOGUCHI, SHOJI KISHIMOTO, ISAO MINAMIDA, MIKIHIKO OBAYASHI1974 Volume 22 Issue 3 Pages 529-536
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS6-Chloro-5-cyclohexylindan-1-carboxylic acid (TAI-284) and related 5-substituted indan-1-carboxylic acids were prepared for the evaluation of antiinflammatory action. Among them, TAI-284 showed the most potent activity, comparable to that of indomethacin. The replacement of the cyclohexyl moiety at C-5 by other alkyl groups such as isobutyl or isopropyl, or the removal of the chlorine atom at C-6 resulted in a considerable reduction of the activities. The resolution of TAI-284 was effected with quinine, and it was found that the antiinflammatory activity virtually resided in the dextro isomer, the absolute configuration of which was assigned the sinister series by the optical rotatory dispersion spectrum and X-ray crystarography.View full abstractDownload PDF (1003K) -
SHUNSAKU NOGUCHI, MIKIHIKO OBAYASHI, SHOJI KISHIMOTO, MASAYUKI IMANISH ...1974 Volume 22 Issue 3 Pages 537-541
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome 1-substituted 6-chloro-5-cyclohexylindans : 6-chloro-5-cyclohexyl-1-hydroxy-methylcarbonylindan (5), 1-acetyl-6-chloro-5-cyclohexyl-1-indanol (10), 5-[(6-chloro-5-cyclohexylindan)-1-yl] tetrazole (13) and 6-chloro-5-cyclohexyl-1-methylindan-1-carboxylic acid (14), were prepared as related compounds of 6-chloro-5-cyclohexylindan-1-carboxylic acid (TAI-284) (1), a potent nonsteroidal antiinflammatory agent. During this work an interesting rearrangement from the acetate (4) of 5 to 3-acetyl-5-chloro-6-cyclohexylindene (6) by acetic acid treatment was discovered and the mechanism of this reaction was proposed.View full abstractDownload PDF (609K) -
MASAHIKO TAKADA, SHIGETAKA AKUZU, AYAKO MISAWA, RYOHEI HORI, TAKAICHI ...1974 Volume 22 Issue 3 Pages 542-550
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSInteraction between 5-n-butyl-1-cyclohexyl-2, 4, 6-trioxoperhydropyrimidine (BCP), which is one of non-steroidal anti-inflammatory agents, and several sulfonamides was investigated in dogs. Decline of plasma level of sulfamethizole, sulfamethizole-N4-acetate and sulfisomezole-N4-acetate was retarded by simultaneous medication of BCP. By simultaneous medication of BCP, sulfisomezole caused a small sudden drop of plasma level, but no alteration was observed with sulfanilamide. BCP possesses strong displacing activity for binding of certain sulfonamides to dog plasma proteins. The clearance ratios of sulfamethizole, sulfamethizole-N4-acetate and sulfisomezole-N4-acetate were remarkably decreased after BCP infusion. No significant alteration of the clearance ratio of sulfisomezole and sulfanilamide was observed. The clearance ratio of BCP was very low when the urine pH is below 8, but increased in metabolic alkalosis. The renal excretion of BCP was significantly blocked by iodopyracet infusion indicating that BCP is secreted through the proximal tubular route by the PAH transport mechanism. It became clear that prolongations of plasma levels of the certain sulfonamides by BCP, are mainly due to competitive interactions between the certain sulfonamides and BCP at renal secretory level.View full abstractDownload PDF (1004K) -
MASAHIKO TAKADA, AYAKO MISAWA, KOICHI FUJIMOTO, RYOHEI HORI, TAKAICHI ...1974 Volume 22 Issue 3 Pages 551-559
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSInteractions between sulfinpyrazone and sulfonamides, and between oxyphenbutazone and sulfonamides, were investigated in dogs. The plasma level of sulfamethizole, sulfamethizole-N4-acetate and sulfisomezole-N4-acetate were prolonged by coadministration of sulfinpyrazone or oxyphenbutazone. But no alteration was observed in plasma level patterns of sulfisomezole and sulfanilamide. Sulfinpyrazone and oxyphenbutazone possess some displacing activity towards sulfonamides bound to dog plasma proteins. In renal clearance experiments, the clearance ratios of sulfamethizole, sulfamethizole-N4-acetate, and sulfisomezole-N4-acetate were markedly decreased after sulfinpyrazone infusion. The effect of oxyphenbutazone on sulfonamide excretion was relatively small compared with that of sulfinpyrazone, and oxyphenbutazone remarkably decreased the clearance ratio of sulfamethizole only. It became clear that prolongations of plasma levels of the certain sulfonamides by SPZ or OPB, are mainly caused by competitive interactions between the certain sulfonamides and the two anti-inflammatory drugs at renal secretory level.View full abstractDownload PDF (984K) -
KANETO UEKAMA, YUKARI CHIBA, KEN IKEDA1974 Volume 22 Issue 3 Pages 560-565
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe distribution behavior of the tetracyclines in the presence of haloacetic acids at acidic conditions has been markedly influenced by the addition of alcohols in organic phase through the solvation of ion pair. The influences of variables, such as pH, anions, temperature on the distribution of tetracyclines into n-hexane containing various alcohols were studied. Stability constants, Kc, for solvated ion pairs and number of alcohol molecules associated with each ion pair, n, were determined. Kc values were highly dependent on the change in substituents of tetracyclines and on the nature of the pairing anions. A linear relationship with unit slope was found between log Kc and that of apparent distribution coefficient of intact tetracyclines. Thermodynamic parameters for ion paired chlortetracycline indicated that alcohol solvation facilitates the distribution processes of ion pair. Both values of Kc and n were influenced by the structural factors of solvating alcohols such as chain length, branching located near the OH group, and cyclic alkyl group. The solvation of alcohol with ion pair was discussed in terms of hydrophobic and hydrogen bonding.View full abstractDownload PDF (663K) -
MASAZUMI WATANABE, MITSURU KAWADA, MASAO NISHIKAWA, ISUKE IMADA, HIROS ...1974 Volume 22 Issue 3 Pages 566-575
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe syntheses of the metabolites of phylloquinone, α-tocopherol and ubiquinones are described. 1. 2, 3, 5-Trimethyl-6-(3'-carboxybutyl)-1, 4-benzoquinone (VIIa), 2-methyl-3-(3'-carboxybutyl)-1, 4-naphthoquinone (VIIb) and 2, 3-dimethoxy-5-methyl-6-(3'-carboxybutyl)-1, 4-benzoquinone (VIIc) were synthesized by two routes. 2, 3, 5-Trimethylphenol (Ia) and 3-methyl-1-naphthol (Ib) were condensed with methylsuccinic anhydride (II), followed by reduction of the carbonyl groups and oxidation of the phenols to quinones (VIIa, VIIb). 2, 3, 5-Trimethyl-1, 4-benzoquinone (XVIIIa), 2-methyl-1, 4-naphthoquinone (XVIIIb) and 2, 3-dimethoxy-5-methyl-1, 4-benzoquinone (XVIIIc) were treated with γ, γ'-dimethoxy-carbonylvaleryl peroxide (XVII) on one step to give the esters (VIIIa, VIIIb, VIIIc) of these quinones. 2. 2, 3, 5-Trimethyl-6-(5'-carboxy-3'-methyl-2'-pentenyl)-1, 4-benzoquinone (XXVa), 2-methyl-3-(5'-carboxy-3'-methyl-2'-pentenyl)-1, 4-naphthoquinone (XXVb) and 2, 3-dimethoxy-5-methyl-6-(5'-carboxy-3'-methyl-2'-pentenyl)-1, 4-benzoquinone (XXVc) were synthesized by boron trifluoride-catalyzed condensation of 2, 3, 5-trimethyl-1, 4-benzohydroquinone (XXIIIa), 2-methyl-1, 4-naphthohydroquinone derivatives (XXIIIb, XXVII, XXVIII) and 2, 3-dimethoxy-5-methyl-1, 4-benzohydroquinone (XXIIIc) with methyl ε-hydroxy-γ-methyl-γ-hexenoate (XX) or methyl γ-hydroxy-γ-vinylvalerate (XXII), followed by hydrolysis of the esters to carboxylic acids and subsequent oxidation of the hydroquinones to quinones.View full abstractDownload PDF (1290K) -
KOJI YAMAKAWA, REIJI SAKAGUCHI, KUSUO OSUMI1974 Volume 22 Issue 3 Pages 576-582
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReduction of the methoiodide (IV) with NaBH4 gave predominantly endo-2'-methyl compound (Va). On the other hand, the reaction of VII with methyl magnesium iodide gave exo-2'-methyl compound (Vb). Configuration and conformation of endo-and exo-2'-methyl-tetrahydropyridoferrocene (Va and Vb) and its quaternary salt (VIa and VIb) were discussed by means of conformational analysis and nuclear magnetic resonance spectroscopy. Attempted synthesis of pyridoferrocene (X) from XIII was unsuccessful.View full abstractDownload PDF (808K) -
ZENICHI HORII, SHUJI UCHIDA, YOSHIHIKO NAKASHITA, EIKO TSUCHIDA, CHUZO ...1974 Volume 22 Issue 3 Pages 583-586
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotolysis of sodium salt of 2-bromo-N-ethyl-4'-hydroxybenzanilide in N, N-dimethyl-formamide gave 2'-ethylspiro [cyclohexa-2, 5-diene-1, 1'-isoindoline]-3', 4-dione in good yield. This reaction was utilized in the syntheses of dl-mecambrine, dl-amurine, and dl-domesticine.View full abstractDownload PDF (589K) -
SHORYO HAYASHI, HIKARU OZAWA1974 Volume 22 Issue 3 Pages 587-593
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome properties of cyclic 3', 5'-nucleotide phosphodiesterase (PDE) in the rat cerebral cortex and heart muscle and inhibitory effect of 3, 7-dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191) on PDE have been investigated by comparison with theophylline and caffeine as PDE inhibitor. 1) Cyclic adenosine monophosphate (AMP) hydrolysis in the supernate of the cerebral cortex and heart muscle is linear with respect to time (up to 30 min) and protein concentration (up to 150 μg and 400 μg in the incubation medium on the brain and heart respectively). 2) PDE activity obtained in the absence of Mg2+ could be increased up to 70 per cent by adding Mg2+ with the supernate of the cerebral cortex as the enzyme. 3) Substantial activity was present in all of the fraction although most was contained in the supernate. 4) From typical Lineweaver-Burk plots, Km values for the supernate of the cerebral cortex and heart muscle were found to be 130 μM and 74 μM respectively. 5) Inhibitory effect of BL 191 on PDE from the rat cerebral cortex supernate was similar to the action of theophylline and was slightly more potent than that of caffeine. The inhibition of BL 191, theophylline and caffeine was noncompetitive ; the Ki was calculated to be 3.0 mM, 3.1 mM and 5.1 mM respectively. The Ki values of 1.65 mM, 1.80 mM and 1.55 mM were found in the heart muscle supernate treated with BL 191, theophylline and caffeine respectively : the type of inhibition was competitive.View full abstractDownload PDF (749K) -
EIJI OWADA, KATSUYUKI TAKAHASHI, RYOHEI HORI, TAKAICHI ARITA1974 Volume 22 Issue 3 Pages 594-600
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to clarify the renal excretion mechanisms of sulfonamides in rabbits the renal clearances of four sulfonamides, which were chosen of widely differing physico-chemical properties, were measured both in control and iodopyracet (IP) infusion periods. In control periods, all of the sulfonamides clearance were lower than inulin clearance, and descending order of these clearances were sulfamethizole (SMZ), sulfanilamide (SA), sulfisoxazole (SI) and sulfamethoxypyridazine (SMP). Sulfamethizole clearance corrected for the protein binding showed net secretion in the tubules, but the other sulfonamide clearances corrected showed net reabsorption. In iodopyracet infusion periods, the clearances of sulfamethizole and sulfisoxazole were significantly depressed below the inulin clearances, suggesting the secretion by the p-aminohippurate (PAH) mechanism and the reabsorption concurrently occurred. Further, the transfer rates in each direction into and out of the renal tubules were calculated with the four sulfonamides, and the determinating factors of the urinary excretions were discussed with reference to the physicochemical properties.View full abstractDownload PDF (795K) -
YOSHIHISA YAMADA, TOYONARI OINE, ICHIZO INOUE1974 Volume 22 Issue 3 Pages 601-609
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRing expansion reaction and dehydrochlorination reaction of substituted-2-chloromethyl-3-aryl-4-oxo-1, 2, 3, 4-tetrahydroquinazolines (2a-g) were investigated. The required starting materials 2a-g were prepared from the corresponding 4 (3H) quinazolines (1a-g) by NaBH4 reduction in excellent yields. 2a-f were easily converted to dehydrochlorination products 3a-f in CHCl3 at room temperature. On the other hand, treatments of 2a-f with EtONa in EtOH afforded ring expansion products 4a-f. The mechanism of the ring expansion reaction was proved by the isolation of an intermediate, azirinoquinazoline (7). The investigation was extended to the reactions of azirinoquinazoline (7) with nucleophiles. The reactions with NaBH4, MeOH, AcOH, PhSH, and EtSH proceeded analogously to give benzodiazepines (8, 9, 10, 11, and 12).View full abstractDownload PDF (1058K) -
HIROAKI NANBA, HISATORA KURODA1974 Volume 22 Issue 3 Pages 610-616
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe biosyntheses of the main components of mycelial cell walls on Cochliobolus miyabeanus (β-glucan, β-1, 3-linked glucan having branched units connected through C-6 and C-1 ; chitin-like substance, β-1, 4-linked N-acetylglucosamine having branched units of N-acetylgalactosamine connected through C-1 by α-glycosidic linkage) were studied. The incorporation of 14C-glucose or 14C-N-acetylglucosamine from uridine diphosphate (UDP)-derivative into β-glucan or chitin-like substance was catalyzed by the particulate enzymes obtained from mycelia. The optimum conditions of these synthetic reaction were as follows : for glucan ; 0.08M Tris-HCl buffer pH 8.2 (contained 0.01M MgCl2 and 0.001M ethylenediamine tetraacetic acid (EDTA)), cell wall glucan, 0.08M UDP-14C-glucose (5 μCi/ml) and enzyme solution ; for chitin-like substance ; 0.08M Tris-HCl buffer pH 7.5 (contained 0.01M MgCl2 and 0.001M EDTA), cell wall chitodextrin, 0.08M UDP-14C-N-acetylglucosamine (5 μCi/ml) and enzyme solution.View full abstractDownload PDF (758K) -
MASAKATSU SONE, YOSHINORI TOMINAGA, REIKO NATSUKI, YOSHIRO MATSUDA, GO ...1974 Volume 22 Issue 3 Pages 617-622
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of methyl 2-cyano-3-methylthio-4-nitrocrotonate with conc. sulfuric acid gave 2-carbamoyl-3-methylthio-2-buten-4-olide (II) in a good yield. This compound (II) was formed easily by the replacement reaction between methylthio group and nucleophilic reagents such as amines or active methylene compounds. Condensation reaction of II as a nucleophilic reagent with various reagents having a formyl or ketone group gave corresponding condensation products. Reaction of II with quinoline 1-oxide gave 2-carbamoyl-3-methylthio-4, 4-bis (2-quinolyl)-2-buten-4-olide (X).View full abstractDownload PDF (704K) -
AKIRA TSUJI, TSUKINAKA YAMANA, YUZO MIZUKAMI1974 Volume 22 Issue 3 Pages 623-627
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIntramolecular catalyzed hydrolysis of amide bond by a second amide group was investigated in the acidic hydrolysis of 2-acylamidobenzamide as model compound. In the 2-arylamido series, the hydrolysis rate decreases as the substituent becomes more electron withdrawing. A Hammett reaction constant was found to be -1.05 and is consistent with the intramolecular catalyzed mechanism. The connection between the present results and penicillin stability in an acidic medium was discussed.View full abstractDownload PDF (597K) -
CHIAKI MORIWAKI, NORIKO WATANUKI, YUKIO FUJIMOTO, HIROSHI MORIYA1974 Volume 22 Issue 3 Pages 628-633
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA purified kininogenase preparation which was homogeneous in disc-electrophoresis and ultracentrifugal analysis was obtained from a guinea pig's coagulating gland by the purification methods of DEAE-cellulose chromatography and Sephadex G-200 gel filtration. The apparent molecular weight of it was estimated to be 31000 by ultracentrifugation and about 40000 by gel filtration, and its isoelectric point was found to be pH 3.4 in electrofocusing analysis with carrier ampholyte. Its amino acid composition was similar to those of the other glandular kallikreins, and it was found to be a glycoprotein containing about 14% of carbohydrates. The kininogenase hydrolyzed N-α-tosyl-L-arginine methyl ester and N-α-benzoyl-L-arginine ethyl ester, having the Km values of 7.80×10-4 and 2.13×10-4 M, respectively. the pH optimum appeared to be 9.0 in the esterolytic response. This enzyme seemed to be rather stable in heat treatment because about 60% of the esterolytic activity was retained after a treatment at 75° for 60 min.View full abstractDownload PDF (819K) -
SHUNICHI YAMADA, YOSHIO TAKEUCHI1974 Volume 22 Issue 3 Pages 634-637
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome amides and carbamates, or some esters and carbonates were synthesized by the reaction of phosphoranes Ph3P=CHCOR (R=Me, Ph, OMe, OEt) with nitrosonium ion in the presence of some amines or alcohols.View full abstractDownload PDF (567K) -
SHOZO MIYAZAKI, TAKAICHI ARITA, RYOHEI HORI, KEIJI ITO1974 Volume 22 Issue 3 Pages 638-642
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe existence of the two crystalline forms of chlortetracycline hydrochloride (CTC-HCI) was confirmed by infrared spectroscopy and X-ray diffraction. From the dissolution studies with crystalline powder and compressed disk, an appreciable difference in the dissolution behavior in water was detected between the two forms. In order to determine the effect of polymorphism on the gastrointestinal absorption of CTC-HCl, blood plasma levels obtained in rabbits after intraduodenal administration and cumulative amounts excreted in human subjects after oral administration of the two forms were compared. The results indicated that polymorphic state of CTC-HCl significantly influences bioavailability of the CTC-HCl.View full abstractDownload PDF (609K) -
MICHIYA KIMURA, KAZUYUKI AKIYAMA, TOSHIAKI MIURA1974 Volume 22 Issue 3 Pages 643-649
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBehavior of various 3-methoxylated phenolic steroids (I-VII and IX-XI) in conc. H2SO4 was studied, in particular relation to the earlier period of the Kober reaction. Alteration of the light-absorptions at the maxima of 432, 465, and 515 nm was detected to be varied with the concentrations of H2SO4 (Fig. 1). The maximum absorption at 372 nm was observed in the mixture of estradiol-3-methyl ether (II) with 97.2% H2SO4 (Fig. 2), which appeared, on the contrary, immediately after mixing III, IV, V, VI, or VII with the same acid (Fig. 3 and 4). Nuclear magnetic resonance study on the solutions of III, IV, or V in the acid (Fig. 5) suggested that the absorption at 372 nm is due to the carbocation χ-372 (VIII) produced. As for the Kober reaction of steroidal estrogens, it was postulated that χ-372 initially formed is oxidized into the characteristic chrommophores χ-465 and χ-515, through which the highly dehydrogenated steroidal olefins are finally produced.View full abstractDownload PDF (747K) -
KOTARO TAKAHASHI, SATOSHI KAWAGUCHI, KENICHI NISHIMURA, KOICHI KUBOTA, ...1974 Volume 22 Issue 3 Pages 650-653
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the pericarps of the capsules of Euscaphis japonica PAX., oleanolic, pomolic, tormentic acids and a new triterpene acid, named euscaphic acid were isolated and the structure of euscaphic acid was elucidated to be 2α, 3α, 19α-trihydroxyurs-12-en-28-oic acid by chemical and spectral evidences.View full abstractDownload PDF (615K) -
NORIKO MOTOHASHI, ITSUHIKO MORI, YUKIO SUGIURA, HISASHI TANAKA1974 Volume 22 Issue 3 Pages 654-657
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe interaction between ergothioneine and divalent metal ions has been investigated by means of potentiometric titration, visible and near-infrared spectra. The order of the relative formation constants of erogothioneine-metal complexes was Cu (II)>Hg (II)>Zn (II)>Cd (II)>Co (II)≨Ni (II). For ergothioneine-cobalt (II) complex, the crystal field parameter (Dq) and Racah interelectron repulsion parameter (B) calculated were 453 and 971 cm-1, respectively. It was indicated that ergothioneine coordinates to cobalt (II) ion through its sulfur atom and forms a distorted tetrahedral complex.View full abstractDownload PDF (554K) -
JUN ADACHI, KEIICHI NOMURA, KOWASHI SHIRAKI, KEMMOTSU MITSUHASHI1974 Volume 22 Issue 3 Pages 658-662
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of benzomorphan analog of which aromatic ring is heterocyclic was investigated. The key compounds of this synthetic route, 2-benzoyl-2-azabicyclo [3.3.1]-nonan-8-one derivatives (X, and XII), were prepared starting from ethyl 4-pyridinepropionate (I). 1, 2, 3, 4, 5, 6-Hexahydro-1, 5-methanopyrido [2, 3-c] azocine derivative (XV) was synthesized by condensation of XII with 3-aminoacrolein. Furthermore, the pyrazolone derivative (XI) was also prepared from X by treatment with hydrazine, and the pyrimidine derivative (XIV) was obtained from XII via the β-diketone (XIII).View full abstractDownload PDF (786K) -
MITSUTERU NUMAZAWA, YORIHISA TANAKA, YOKO(NOTTA) MOMONO, TOSHIO NAMBAR ...1974 Volume 22 Issue 3 Pages 663-668
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe biliary excretion of the water-soluble metabolites in the rat administered with 2-hydroxyestrone-6, 7-3H and estrone-4-14C has been investigated. A polar metabolite separated from the collected bile was characterized to be a conjugate of 2-hydroxyestrone with cysteine at C-1 or C-4 through a sulfide linkage. The in vitro experiment with the rat liver preparation also demonstrated the formation of the cysteine conjugate. Based upon the 3H/14C values of 2-hydroxyestrone and its cysteine conjugate the probable mechanism involved in conjugation has been discussed.View full abstractDownload PDF (752K) -
TOSHIMICHI TSUBOI, KOHSAKU ISHIKAWA, YOSHIKO OHSAWA, KOUICHI YOSHIDA, ...1974 Volume 22 Issue 3 Pages 669-675
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBiochemical Studies of myocardial lesions induced by isoproterenol (ISP) were performed on the changes of myocardial water content, high energy phosphate levels and plasma enzyme activities. Protective effects of propranolol and anti-inflammatory drugs on the biochemical shifts by ISP were also examined. Cardiac water content increased immediately after subcutaneous injection of ISP and reduced near the normal level after 3 days. Anaerobic glycolysis and depletion of high energy phosphates were observed immediately after an injection of ISP. These biochemical shifts returned to normal within 24 hr except adenosine triphosphate (ATP) and total adenine nucleotide levels which remained at lower levels than normal. Distinct indications of returns toward the normal values with the levels of ATP and total adenine nucleotides took place at the same time as water content reduced. Plasma creatine phosphokinase (CPK), glutamic oxaloacetic transaminase (GOT) and lactic dehydrogenase (LDH) activities were markedly elevated after the treatment of ISP and did not reach to normal after 24 hr. Pretreatment with propranolol blocked the biochemical shifts by ISP, such as cardiac edema, depletion of myocardial adenine nucleotides and elevation of plasma LDH activity. Prednisolone or indomethacin pretreatment decreased the water content and plasma LDH activity, but did not show the influence on cardiac adenine nucleotide levels.View full abstractDownload PDF (852K) -
HIROYUKI INOUYE, SHINICHI UEDA, KENICHIRO INOUE, YOSHIO TAKEDA1974 Volume 22 Issue 3 Pages 676-686
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTracer experiments revealed that (10-3H)-loganin (2) was incorporated into gentiopicroside (3) in Gentiana triflora var. japonica. (7-3H)-2 and (carbo-14C-methoxy)-secolo-ganin (10) were also found to be incorporated into morroniside (4) in Gentiana thunbergii and Cornus officinalis, respectively. The biosynthetic pathway of oleuropein-type glucosides in Olea europaea and Jasminum primulinum was further examined by employing (10-3H)-7-deoxyloganic acid (1), (10-3H)-loganin (2), (carbo-14C-methoxy)-secologanin (10), (8-3H)-and (carbo-3H-methoxy)-kingiside (11), together with (8-3H)-and (carbo-14C-methoxy)-8-epikingiside (18).View full abstractDownload PDF (1310K) -
SEIJIRO HONMA, TOSHIO NAMBARA1974 Volume 22 Issue 3 Pages 687-695
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn connection with the studies on the enterohepatic circulation of estrogen the biliary metabolites formed from estrone have been investigated in the rat. The free and conjugated metabolites were separated from the bile collected after administration of estrone. The structures of these metabolites were deduced from the physico-chemical data and definitely characterized by direct comparison with the authentic specimens. The significance of the biotransformation hereby observed has been discussed.View full abstractDownload PDF (1300K) -
MITSUJI SANO, HIDEO HAKUSUI1974 Volume 22 Issue 3 Pages 696-706
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe metabolism of methylscopolammonium methylsulfate (I) in rats was investigated. Eight metabolites were detected in urine and faeces after oral and subcutaneous administrations. The feature of metabolic pathway was characterized as follows ; i) the quarternary ammonium moiety was unchanged, ii) major pathway involved oxidation at the paraposition of benzene ring to introduce a hydroxy and a methoxy groups, iii) minor products were the apo-derivative, glucuronide of I and scopine derivative. Absorption and excretion were examined by using 14C-labeled compound, and excreted total radioactivities were 82.2% of oral dose and 93.6% of subcutaneous dose in urine and faeces. In respiratory air 14CO2 was not detectable. Comparison of the metabolic pathway with that of tertiary scopolamine are also discussed.View full abstractDownload PDF (1079K) -
SHINICHI FUJITA, YASUJI FUJITA1974 Volume 22 Issue 3 Pages 707-709
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (438K) -
KOJI YAMAKAWA, MICHIO MOROE1974 Volume 22 Issue 3 Pages 709-711
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
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TOYOSHIGE KABEYA, KAZUYA KOHASHI, YOSUKE OHKURA1974 Volume 22 Issue 3 Pages 711-714
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (550K) -
SHINICHI YOSHIHARA, HIDETOSHI YOSHIMURA1974 Volume 22 Issue 3 Pages 714-717
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (498K) -
SUSUMU SHIBUYA, AKIRA KUNINAKA, HIROSHI YOSHINO1974 Volume 22 Issue 3 Pages 719-721
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (451K) -
YUTAKA OKADA, HIROYOSHI HORIKOSHI, YOSHIHIKO BABA1974 Volume 22 Issue 3 Pages 721-723
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (459K) -
MASANORI KUROYANAGI, MASAMICHI FUKUOKA, KUNITOSHI YOSHIHIRA, SHINSAKU ...1974 Volume 22 Issue 3 Pages 723-726
Published: March 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (466K)
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