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Volume 32, Issue 1
Displaying 1-50 of 59 articles from this issue
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BUNJI UNO, YOSHIO MATSUHISA, KENJI KANO, TANEKAZU KUBOTA1984 Volume 32 Issue 1 Pages 1-10
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe nonaqueous reduction polarograms of 4, 4'-disubstituted stilbenes exhibited two waves, the half-wave reduction potentials, Ered1/2·1 and Ered1/2·2, of which are mainly controlled at the steps of monoanion and dianion formation, respectively. The physical meanings of Ered1/2·1 and Ered1/2·2 can be clearly seen by applying the Born-Haber type thermochemical cycle and molecular orbital (MO) calculation, and theoretical equations concerning (Ered1/2·1+Ered1/2·2) and (Ered1/2·1-Ered1/2·2) were formulated. The MO calculations of the PPP-SCFMO, LP-SCFMO, and CNDO/2 levels were used for checking the formulae. The results were quite reasonable on the assumption that the contribution from the solvation energy terms is almost constant or alters in parallel with the LUMO energy in a series of similar substances. In the case of NO2 as a substituent, as in 4, 4'-dinitrostilbene, the Ered1/2·2 value is markedly shifted in a negative direction from that expected from the other substituents, so that the NO2 group does not fit well with the above theoretical treatment. High-speed cyclic voltammetric measurements were performed to investigate this phenomenon of nitro-substituted aromatics, and the results are discussed in detail.View full abstractDownload PDF (879K) -
KENICHI YAKUSHIJIN, TOMOKO TOHSHIMA, EIJI KITAGAWA, RIKA SUZUKI, JUNKO ...1984 Volume 32 Issue 1 Pages 11-22
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSChemical constituents of the leaves of Illicium tashiroi and I. arborescens (Illiciaceae) were examined. Novel phytoquinoids, (+)-illicinone-A (1a), -B (2a), -C (3a), and -D (4a), and illifunone-A (5a) and -B (5b) were isolated from I. tashiroi, and characterized. As constituents of I. arborescens, enantiomers (1b and 2b) of (+)-illicinone-A (1a) and -B (2a), and diastereoisomers (2c, 3b, 4b, and 4c) of (+)-illicinone-B (2a), -C (3a), and -D (4a) were characterized. The absolute stereochemistry of (-)-illicinone-A was established by analysis of the circular dichroism (CD) spectra of the α-hydroxy ketones (15 and 16) derived from 1b. The stereochemistries of other illicinones and illifunones deduced from the chemical and/or biogenetic correlations.View full abstractDownload PDF (1043K) -
KENICHI YAKUSHIJIN, HIROSHI FURUKAWA, ANDREW T. MCPHAIL1984 Volume 32 Issue 1 Pages 23-30
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSConversion of illicinone-A (1) to illicinole (4) and the reverse reaction (4→1) were occurred thermally and photochemically, respectively. The photochemical reaction of illicinone-A (1) led to the formation of 5 and 6, having novel carbon skeletons. The structure of 5 was established by X-ray analysis.View full abstractDownload PDF (698K) -
TETSUYA TAKEYA, YUKARI AKABANE, EIICHI KOTANI, SEISHO TOBINAGA1984 Volume 32 Issue 1 Pages 31-37
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(±)-lsopodophyllotoxone 6a and the related lactones 8a and 9a were synthesized by a biomimetic procedure from the ester 5a by oxidation with a CrO3-HBF4-MeCN reagent system in one step. 4'-Benzyl-isopodophyllotoxone 6b, 4'-benzyl-picropodophyllone 7b, and the γ-lactones 8b and 9b were also synthesized from the ester 5b by oxidation with the same reagent system.View full abstractDownload PDF (734K) -
SADAKATSU SHIMADA, MASAHARU OKI1984 Volume 32 Issue 1 Pages 38-43
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel and convenient synthesis of pyridoxine starting from N-(1-cyanoethyl) formamide is described. The reaction of N-(1-cyanoethyl) acylamides with olefins in the presence of an acid catalyst gave 3-amino-2-methylpyridines. Similar reaction of N-(1-cyanoethyl) formamide with fumaronitrile in the presence of trifluoroacetic acid afforded 5-amino-6-methylpyridine-3, 4-dicarbonitrile, which was easily converted to pyridoxine by reduction and diazotization.View full abstractDownload PDF (568K) -
TAKESHI KATO, KIYOHISA KAWAI, YOICHI SAWA1984 Volume 32 Issue 1 Pages 44-54
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn a search for synthetic non-narcotic analgesics, 1, 6-trans-N-substituted (6-benzyl-4, 4-dimethyl-2-cyclohexenyl) methylamines (5) were prepared by dehydration of the corresponding 2, 3-trans-2-aminomethyl-3-benzylcyclohexanols (2 and 3) with thionyl chloride. The (1-cyclohexenyl) methylamines (4) and the 1, 2-trans-(2-chlorocyclohexyl) methylamines (6) were also produced from the 1, 2-cis-cyclohexanols (2) as minor products, but the only isolable by-product from the 1, 2-trans-cyclohexanols (3) was the 1, 2-cis-(2-chlorocyclohexyl) methylamines (7). The 1, 6-cis-(6-benzyl-2-cyclohexenyl) methylamine (13a) was obtained by isomerization of the 2, 3-trans-3-benzyl-2-dimethylaminomethylcyclohexanone (1a) followed by reduction and dehydration. Catalytic hydrogenation of (2-benzyl-2-cyclohexenyl) methylamines (17) gave the 1, 2-trans-and 1, 2-cis-cyclohexylmethylamines (8 and 19). Among the compounds tested, 1, 6-trans-N, N-dimethyl-(6-benzyl-4, 4-dimethyl-2-cyclohexenyl) methylamine (5a) hydrochloride was as potent as codeine phosphate in analgesic activity as determined by the phenylquinone writhing method.View full abstractDownload PDF (942K) -
KAORU FUJI, TOSHIHIDE YAMADA, EIICHI FUJITA, KAORU KURIYAMA, TATSUO IW ...1984 Volume 32 Issue 1 Pages 55-62
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe circular dichroism (CD) spectra of Lythraceae alkaloids and their derivatives having a mobile biphenyl moiety were measured. The conformational chirality of the biphenyl system in these derivatives can be determined from the Cotton effects in the 200-240nm region. The biphenyl system of M helicity showed a positive Cotton effect at long wavelength coupled with a negative Cotton effect at short wavelength, and vice versa for P helicity. Single crystal X-ray analyses of O-methyllythranidine N, O, O-triformate (17) and O-methyldeacetyl-lythranine (20) provided support for this conclusion.View full abstractDownload PDF (648K) -
KAORU FUJI, TOSHIHIDE YAMADA, EIICHI FUJITA, HIROSHI NAKAI, MOTOO SHIR ...1984 Volume 32 Issue 1 Pages 63-69
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe crystal and molecular structures of three derivatives of Lythraceous alkaloids, O-methyllythranidine N, O, O-triformate (2), 22-bromolythranine N, O, O-triacetate (3), and O-methyldeacetyl lythramine (4) were determined. The conformational chiralities of the biphenyl group in the crystals of these compounds were in conformity with those proposed on the basis of circular dichroism studies as the predominant forms in solution.View full abstractDownload PDF (575K) -
KAORU FUJI, TOSHIHIDE YAMADA, EIICHI FUJITA1984 Volume 32 Issue 1 Pages 70-74
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTemperature-dependent carbon-13 nuclear magnetic resonance (13C-NMR) studies have disclosed that the mobile equilibrium in N, O-dimethyllythranidine (1) involves mainly two dynamic processes, which are rotation about the carbon-carbon bond between two phenyl rings and reversal of the piperidine ring. At ambient temperature, 13C chemical shift differences due to rotational movement were averaged, while those due to ring flip of piperidine moiety were not. This provides another example of "selective kinetic equalization of chemical shifts."View full abstractDownload PDF (423K) -
MINORU MACHIDA, KAZUAKI ODA, YUICHI KANAOKA1984 Volume 32 Issue 1 Pages 75-84
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotolysis of N-(3-alkenyl) phthalimides 2 in methanol gave tetrahydro-5H-pyrrolo [2, 1-a] isoindol-5-ones 3 and/or tetrahydropyrido [2, 1-a] isoindol-6 (2H)-ones 4 depending on the degree of substitution at the olefin carbons of 2. Electron transfer followed by the anti-Markownikoff addition of methanol is proposed as a possible pathway.View full abstractDownload PDF (793K) -
EIKO OHTSUKA, YOSHIO TANIYAMA, SHIGENORI IWAI, TADAO YOSHIDA, MORIO IK ...1984 Volume 32 Issue 1 Pages 85-93
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour dodecanucleotides dATGTTTCCCTCTpOAr (12a), dATGATGTGGTATpOAr (12b), dATGTTGCCCGTTpOAr (12c) and dATGTGTCTGCGGpOAr (12d) having the 3'-(o-chlorophenyl) phosphate moiety have been synthesized on a polymer support by elongation in the 3'-direction. The 5'-succinyl group of N-protected deoxynucleoside 3'-(o-chlorophenyl)-phosphoro-p-anisidates was reacted with the amino group of the aminomethylene derivative of 1% cross linked polystyrene and the 3'-phosphoro-p-anisidate was converted to the phosphodiester by treatment with isoamyl nitrite. The chain was elongated by condensation of the 3'-phosphodiester with 5'-deblocked dinucleotides or trinucleotides having the 3'-(o-chlrophenyl) phosphoro-p-anisidate moiety by using 1-(mesitylenesulfonyl)-3-nitro-1H-1, 2, 4-triazole as the activating reagent. The reaction was repeated and products were deblocked except for the o-chlorophenyl group on the 3'-phosphate. The overall yields of the dodecamers were 9-16%. The method can be applied to the synthesis of oligonucleotides having nucleoside derivatives at the 3'-end.View full abstractDownload PDF (766K) -
KENICHI KAWAI, KOOHEI NOZAWA, SHOICHI NAKAJIMA, YOICHI IITAKA1984 Volume 32 Issue 1 Pages 94-98
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of meleagrin (1), isolated from Penicillium meleagrinum, was determined by X-ray crystallographic analysis of 9-O-p-bromobenzoylmeleagrin (7) monohydrate. The crystal structure of 7 monohydrate was determined by the heavy atom method : the final R value without hydrogen atoms was 0.094. The structure of meleagrin was established as the 9-O-demethyl compound of oxaline (4), isolated from Penicillium oxalicum. The absolute configurations at N1, C2, and C3 are S, S, and R, respectively.View full abstractDownload PDF (563K) -
SABURO SUGAI, TAKASHI KODAMA, SANYA AKABOSHI, SHIRO IKEGAMI1984 Volume 32 Issue 1 Pages 99-105
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of aldehydic acetals with hypochlorous acid in acetic acid-acetone afforded the corresponding esters in excellent yields. From cyclic acetals, only the corresponding hydroxyalkyl esters were obtained.View full abstractDownload PDF (683K) -
MASAYUKI SATO, NORIO KANUMA, TETSUZO KATO1984 Volume 32 Issue 1 Pages 106-116
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCycloaddition of acylketenes (2) to 1, 2-and 1, 3-dipolar compounds was investigated. The thermal reaction of 1, 3-dioxin-4-ones (1) with isoquinolinium phenacylide (11) gave the aromatized pyrrolo [2, 1-a] isoquinolines (12-15). The reaction of 1 with pyridinium and isoquinolinium cyanomethylides (3-5) afforded the 1, 3-oxazinylmethylides (6-8). The intermediate 2 likewise reacted with cyanamides and benzonitriles to give the corresponding 1, 3-oxazin-4-one derivatives (19-23).View full abstractDownload PDF (797K) -
TAKASHI TANAKA, GENICHIRO NONAKA, ITSUO NISHIOKA1984 Volume 32 Issue 1 Pages 117-121
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSix methyl glucoside gallates (I-VI) were isolated, together with gallic acid 3-O-β-D-(6'-O-galloyl)-glucopyranoside (VII), from the undeground part of Sanguisorba officinalis L. On the basis of chemical and spectroscopic evidence, the structures of these compounds were established to be 6-O-gallate (1), 6-O-digallate (2), 4, 6-di-O-gallate (3), 2, 3, 6-tri-O-gallate (4), 3, 4, 6-tri-O-gallate (5) and 2, 3, 4, 6-tetra-O-gallate (6) of methyl β-D-glucopyranoside.View full abstractDownload PDF (565K) -
YOSHINORI TOMINAGA, SHINYA KOHRA, HIROTO OKUDA, ATSUYUKI USHIROGOCHI, ...1984 Volume 32 Issue 1 Pages 122-129
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of ketenethioacetals [methyl 2-cyano-3, 3-bis (methylthio) acrylate (2), 3, 3-bis-(methylthio)-2-phenylsulfonylacrylonitrile (13)] with 6-aminouracils (1a : R1=R2=Me, 1b : R1=Ph, R2=H) in the presence of potassium carbonate followed by cyclization under reflux in diphenyl ether gave the corresponding 5-amino-6-methoxycarbonyl-7-methylthiopyrido [2, 3-d]-pyrimidine-2, 4 (1H, 3H)-dione derivatives (4a, b). Reaction of other ketenethioacetals [2-cyano-3, 3-bis (methylthio) acrylonitrile (10), dimethyl bis (methylthio) methylenemalonate (18), α-oxo ketenethioacetals (21a-e)] with 1 directly afforded pyrido [2, 3-d] pyrimidine derivatives (11a, b, 20a, b, 23a-e) in good yields. 5-Amino-7-methylthiopyrimido [4, 5-d] pyrimidine-2, 4 (1H, 3H)-dione derivatives (16a-c) were also synthesized from 6-aminouracils (1a, b) and dimethyl cyanoimidodithiocarbonate (15) in a manner similar to that used for the preparation of compound 11a.View full abstractDownload PDF (823K) -
KATSUMI ITOH, AKIO MIYAKE, NORIO TADA, MINORU HIRATA, YOSHIKAZU OKA1984 Volume 32 Issue 1 Pages 130-151
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn a search for a new structural type of β-adrenergic antagonist. a series of trans-2-(N-substituted amino)-1, 2, 3, 4-tetrahydronaphthalen-1-ol derivatives (3-36) was synthesized in several steps from 3, 4-dihydro-1 (2H)-naphthalenone (37) having a variety of substituents at the 5-, 6-, 7-and 8-positions. Compounds 3-36 were tested in vitro for β-adrenergic activity. Among them, 2-benzhydrylamino-6-chloro-1, 2, 3, 4-tetrahydronaphthalen-1-ol (28c) was found to show a fairly potent β-adrenergic blocking activity.View full abstractDownload PDF (1484K) -
YASUO ISOMURA, SHUICHI SAKAMOTO, NORIKI ITO, HIROSHIGE HOMMA, TETSUSHI ...1984 Volume 32 Issue 1 Pages 152-165
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 2, 6-di-tert-butylphenols with azoles at the 4-position was synthesized and evaluated for anti-arthritic activity in adjuvant-induced arthritis (AA) assay. Some compounds were also examined for anti-inflammatory activity in carrageenin-induced rat paw edema assay (CIPE) and for analgesic activity in AcOH-induced writhing assay in mice. 4-(3, 5-Di-tert-butyl-4-hydroxyphenyl)-5-methyl-2-oxo-4-imidazoline (6b) (25mg/kg. p.o.) had about the same activity as indomethacin (2mg/kg, p.o.) in AA assay. Compound 6b (25mg/kg, p.o.) was as potent as phenylbutazone (50mg/kg, p.o.) and indomethacin (3mg/kg, p.o.) in CIPE and showed low acute toxicity (>1000mg/kg, mouse, >400mg/kg, rat). Compound 6b had radical-scavenging activity in vivo and in vitro, and showed mild inhibitory activity on delayed-type hypersensitivity. Thus 6b is a promising candidate as a new anti-arthritic agent. Detailed pharmacologic studies of 6b are under way.View full abstractDownload PDF (1087K) -
CHIENCHIH CHEN, YUHPAN CHEN, HONGYEN HSU, YUHLIN CHEN1984 Volume 32 Issue 1 Pages 166-169
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new flavones, 5, 6, 7, 5'-tetramethoxy-3', 4'-methylenedioxyflavone (1), 5, 6, 7, 3', 4', 5'-hexamethoxyflavone (II) and 5, 7, 5'-trimethoxy-3', 4'-methylenedioxyflavone (IV), together with known flavones, 5, 6, 7, 3', 4'-pentamethoxyflavone (III), 5, 7, 3', 4', 5'-pentamethoxyflavone (V). and 5, 7, 3', 4'-tetramethoxyflavone (VI), have been isolated and identified from the root of Bauhinia championii BENTH.View full abstractDownload PDF (535K) -
TAICHI OHMOTO, KAZUO KOIKE1984 Volume 32 Issue 1 Pages 170-173
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo New alkaloids, 1-(1-hydroxy-2-methoxy) ethyl-4-methoxy-β-carboline (IV) and 5-hydroxymethylcanthin-6-one (V), have been isolated from the root bark of Ailanthus altissima SWINGLE (Simaroubaceae) together with three known alkaloids, β-carboline-1-propionic acid (I), 1-carbamoyl-β-carboline (II), and 1-carbomethoxy-β-carboline (III). The structures were elucidated on the basis of spectral and chemical evidence.View full abstractDownload PDF (522K) -
KAZUO OKUMURA, TOSHIKO WADA, KIYOSHI YAMAOKA, TOYOZO UNO1984 Volume 32 Issue 1 Pages 174-178
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe rate constants for the formation and the decomposition of color products in the Fujiwara reaction using benzotrichloride (α, α, α-trichlorotoluene) as the starting material were evaluated by means of simultaneous nonlinear least-squares fitting for the time course data of three compounds. The apparent rate constants for the formation of red and yellow compounds are 0.16 (s-1) and 0.095 (s-1), respectively, and those for the decomposition of these chromophores are 10.3 (s-1) and 0.67 (s-1), respectively. These results indicate that the red compound which is the main color compound in the Fujiwara reaction is very unstable and the yellow compound is rather stable. It was found that 40.3% of benzotrichloride is converted to the red compound, 23.9% to the yellow compound and 35.8% to other compounds.View full abstractDownload PDF (466K) -
KENICHI KUSUBE, KOUICHI ABE, OSAMU HIROSHIMA, YOSHINOBU ISHIGURO, SEIJ ...1984 Volume 32 Issue 1 Pages 179-184
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple, sensitive, and specific method for the determination of phylloquinone (PK) and menaquinone-4 (MK-4) in rat plasma was developed. PK and MK-4 extracted from biological materials were separated by high performance liquid chromatography using a Nucleosil[○!R] C18 column with acetonitrile-isopropyl alcohol as a mobile phase, monitored with a fluorescence detector (ex=330nm, em=430nm) after on-line electrochemical derivatization to fluorescent naphthohydroquinones in an electrochemical reactor. This method was successfully applied to the determination of very small quantities of PK and MK-4 in rat plasma.View full abstractDownload PDF (504K) -
KAYOKO ODA, SHIGERU YOSHIDA, SHINGO HIROSE, TATSUMORI TAKEDA1984 Volume 32 Issue 1 Pages 185-192
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA photon counting method based on the detection of bioluminescence was developed for the determination of ultratrace levels of β-nicotineamide adenine dinucleotide, reduced form (NADH). A commercial bacterial luciferase (Vibrio fischeri) which contains both flavin mononucleotide (FMN) reductase and luciferase was immobilized by the diazocoupling method onto arylamine glass beads. The immobilized luciferase beads were packed in a tube and placcd in front of the photomultiplier tube of a photon counter. A flow injection system with a packed-bed reactor was used for the determination of NADH. The immobilized enzyme system is superior to soluble luciferase in that it is reusable and much more stable. In the present method. the lower limit of detection of NADH was 130 fmol. Ethanol and L-lactic acid determinations in serum were carried out by using immobilized alcohol dehydrogenase and lactic dehydrogenase, respectively. NADH produced in each enzyme reaction was assayed by using the immobilized luciferase column. The serum background emission is negligibly small. The methods are simple and suitable for routine use.View full abstractDownload PDF (789K) -
HIDEMI TODORIKI, AKIKO Y. HIRAKAWA1984 Volume 32 Issue 1 Pages 193-197
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe use of an optical fiber as a wave guide for a laser beam reduces the undesired scattered light in trace fluorometry and in Raman spectroscopy of microliter-size samples. It also permits effective sample excitation and easy optical alignment. In conjunction with high performance liquid chromatogaphy (HPLC), this excitation method has improved the detection limit by an order of magnitude without any other change in the conventional HPLC fluorometric detection system.View full abstractDownload PDF (600K) -
KAZUYUKI KIRANO, YUICHI IIIZUMI, MAMORU SUGIURA, YUKIO MORI, KAZUMI TO ...1984 Volume 32 Issue 1 Pages 198-204
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to elucidate the physiological function of intestinal alkaline phosphatase, the characteristics of alkaline phosphatases from rat and human small intestine were compared under optimal and physiological pHs. The Km values of these enzymes towards p-nitrophenylphosphate at the physiological pH were lower by two orders of magnitude than those at the optimal pH. At the physiological pH, phosphate, arsenate and vanadate competitively inhibited alkaline phosphatase activity, as they did at the optimal pHs, and the Ki values of these inhibitors at the physiological pH were also lower by two orders of magnitude than those at the optimal pHs. The effects of various inhibitors and antiserum to rat intestinal alkaline phosphatase on the transport of phosphate into everted rat intestine were investigated. The results obtained from the present study indicate that a phosphate transport system operating at physiological pH exists in the upper part of the small intestine where the alkaline phosphatase is maximally concentrated. It was also found that the phosphate transport was affected by various inhibitors and antiserum to rat intestinal alkaline phosphatase, but L-homoarginine and ouabain had no effect. From the above findings, it is suggested that alkaline phosphatase may function not only as a hydrolytic enzyme of phosphomonoesters but also as a phosphate transporter in the physiological state.View full abstractDownload PDF (705K) -
TAKAKO YOKOZAWA, PINGDONG ZHENG, HIKOKICHI OURA, ITSUO NISHIOKA1984 Volume 32 Issue 1 Pages 205-212
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of rhubarb extract on the urinary constituents was examined in rats with renal failure induced by adenine. Administration of the rhubarb extract markedly increased the urinary excretion of both urea and creatinine, indicating an improvement of renal clearance in the uremic state. Furthermore, a number of significant differences in the amino acid levels in the urine were observed. Among the essential amino acids, the urinary outputs of threonine, phenylalanine, leucine, and methionine were remarkably lower in the rhubarb extract-treated group than in the control group. Outputs of inessential amino acids (alanine, glycine, glutamic acid, serine, aspartic acid, tyrosine, and cysteine) were also strikingly reduced after the treatment. In addition. the amount of urinary Ca was significantly reduced in the rhubarb extract-treated rats. while urinary inorganic phosphate was significantly elevated. A marked decrease of 2, 8-dihydroxyadenine excretion in the urine was noticed. However, no changes were seen in the urinary excretions of protein, glucose, Na, and K throughout the experimental period.View full abstractDownload PDF (786K) -
YOSHIHIKO INAMORI, YOSHIAKI KATO, MAYURI KUBO, MASAHIDE YASUDA, KIMIYE ...1984 Volume 32 Issue 1 Pages 213-218
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3, 3', 4, 5'-Tetrahydroxystilbene (1) isolated from the heartwood of Cassia garrettiana CRAIB. showed a broad spectrum of physiological activities, including antifungal, phytogrowthinhibitory and ichthyotoxic activities. Firstly. 1 showed antifungal activity ; the minimal growthinhibitory concentration (MIC) was 25 μg/ml against Penicillium citrinum and Rhizopus nigricans. Secondly, 1 showed rather strong inhibitory activity on the growth of five plant species at a concentration of 500ppm. Thirdly. 1 had ichthyotoxic activity. The median tolerance limit (TLm) at 48h was 26.5ppm in Oryzias latipes TEMMINCK et SCHLEGEL and 31.5 ppm in Carassius auratus LINNE. Studies were made on the activities of derivatives of 1, i.e., 3, 3', 4, 5'-tetrahydroxystilbenetetraacetate (2), 3, 3', 4, 5'-tetrahydroxystilbene-tetramethyl ether (3), and 3, 3', 4, 5'-tetrahydroxybibenzyl (4). The activities of these derivatives, however, were lower than those of 1, except for the phytogrowth-inhibitory and ichthyotoxic activities of 4. It is clear that for antifungal activity, both the hydroxyl groups attached to the benzene rings and the trans-olefin structure are necessary, while for the phytogrowth-inhibitory and ichthyotoxic activities, only the hydroxyl groups attached to the benzene rings are necessary.View full abstractDownload PDF (564K) -
Studies on Heart. XXIV. Inhibitory Effect of Antiarrhythmic Peptide (AAP) on Experimental ThrombosesSHIGERU AONUMA, YASUHIRO KOHAMA, TOSHITAKE MAKINO, KUNIHIRO HATTORI, Y ...1984 Volume 32 Issue 1 Pages 219-227
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe antithrombotic action of antiarrhythmic peptide (AAP) was studied by using various in vivo thrombosis models. AAP (1, 10 or 100mg/kg, i.v., 10 mg/kg, i.p. or 100mg/kg, p.o.) significantly inhibited white thrombus formation on a silken thread in the extracorporeal shunt models in rats, its ED50 being about 30mg/kg, i.v. AAP (10mg/kg, i.v.) was effective in protecting rats against the decrease in platelet count, incidence of electrocardiographic alterations (T wave inversion and ST segment depression) typical of myocardial ischemia, and development of ectopic beats in the coronary thromboembolism induced by intravenous infusion of adenosine 5'-diphosphate. The peptide (10mg/kg, i.p.) was also effective in preventing thrombus formation in the lung and the decrease of platelet count induced by lactic acidosis in rats, and it (10mg/kg, i.v.) clearly inhibited thromboembolic death induced by rapid intravenous injection of collagen in mice. Daily treatments with the peptide (10mg/kg/d, i.p.) resulted in significant delay of the progression of gangrene and mummification in laurate-induced peripheral arterial occlusive disease in rats. AAP did not affect venous thrombus formation, blood flow through the carotid artery, plasma recalcification time or fibrinolytic activity in rats. It is likely that the potent antithrombotic action of AAP is mainly due to its anti-platelet-aggregating action in vivo. Ticlopidine (100mg/kg, p.o.) also showed a comparatively wide antithrombotic spectrum, like AAP, in the present thrombosis models, but ticlopidine lacked the action against myocardial ischemia, like aspirin (50mg/kg, s.c.).View full abstractDownload PDF (887K) -
TAKASHI ABIKO, HIROSHI SEKINO1984 Volume 32 Issue 1 Pages 228-236
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSix common amino acid sequence fragments of thymosins β4, β8 and β9, H-Lys-Leu-Lys-Lys-Thr-Glu-Thr-Gln-Glu-Lys-Asn-OH (positions 16-26), H-Lys-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gln-OH (positions 31-39), H-Asp-Lys-Pro-Asp-OH (positions 2-5), H-Phe-Asp-Lys-OH (positions 12-14), H-Leu-Pro-OH (positions 28-29) and H-Glu-Ile-OH (positions 8-9), were synthesized by the solution method, and were tested to determine their effects on the low E-rosette forming cells of lupus nephritis patients. Two of the fragments, H-Lys-Leu-Lys-Lys-Thr-Glu-Thr-Gln-Glu-Lys-Asn-OH and H-Lys-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gln-OH, increased E-rosette forming capacity when incubated in vitro with patient's blood though they were less effective than thymosin β9, but the other four peptide fragments, H-Asp-Lys-Pro-Asp-OH, H-Phe-Asp-Lys-OH, H-Leu-Pro-OH and H-Glu-Ile-OH, had no effect.View full abstractDownload PDF (905K) -
JINICHI INOKUCHI, ATSUO NAGAMATSU1984 Volume 32 Issue 1 Pages 237-243
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of halides on the dipeptidyl and tripeptidyl carboxypeptidase activities of kininase II (angiotensin-converting enzyme, EC 3.4.15.1) purified from hog kidney were investigated. The dipeptidyl carboxypeptidase activity of the enzyme for bradykinin in the absence of halides was found to be buffer-dependent, and was decreased by the anions in potassium phosphate, N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid (Hepes), Tris-H2SO4, Tris-H3PO4 and Trisacetate buffers with increasing concentration of these buffers (1-100mM) ; however, the activity was unaffected by borate-sodium carbonate buffer in this concentration range. When boratesodium carbonate buffer was used, F- functioned as an activator by raising V (2-fold) without modifying Km, while the other halides (Cl-, Br- and I-) hardly influenced V/Km (there were decreases of both V and Km), despite the fact that all the halides functioned as activators in various buffers by raising V (maximum 14-fold) without markedly affecting Km when angiotensin I was the substrate. The stimulatory effect of F- on bradykinin hydrolytic activity was maximum at 10mM, and it was reversed by various other anions (Cl-, Br-, I-, PO3-4, SO2-4, Hepes and CH3COO-). The V value of the enzyme for Gly-Phe-Ser-Pro-Phe (des-Arg9-bradykinin analogue), which is a substrate for the tripeptidyl carboxypeptidase activity of the enzyme (Biochim. Biophys. Acta, 662, 300, 1981), was enhanced by the addition of halides in the order Cl->Br->I->F-. On the other hand, the V value of the tripeptidyl carboxypeptidase activity of the enzyme for Gly-Pro-Ser-Pro-Phe, which has a proline residue at P1, like bradykinin, was enhanced to a lesser degree by halides and the maximal activity was obtained by the addition of 100mM F- (which resulted in a 2-fold increase of V).View full abstractDownload PDF (650K) -
HARUHISA UEDA, NAOKI NAMBU, TSUNEJI NAGAI1984 Volume 32 Issue 1 Pages 244-250
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution profiles of chlorpropamide (CPM) polymorphs, especially the metastable form II reported by Al-Saieq et al., were investigated kinetically in detail by a dispersed amount method and a stationary disk method in comparison with those of the stable form. Form II showed a dissolution phenomenon involving simultaneous phase change from metastable form to stable form during dissolution. The saturated concentrations of metastable form II and stable form A, Csm and Cso, the rate constant of the crystallization process Kr and the dissolution rate constant, K1, were calculated by the stationary disk method. By analyzing the values of Csm and Cso obtained at various temperatures, the transition temperature and heat of transition were determined. Further, the activation energies of crystallization and the dissolution process were also determined by Arrhenius plots of Kr and K1 obtained at various temperatures.View full abstractDownload PDF (590K) -
HISOMU NAGASHIMA, YORIHISA TANAKA, HIDETOSHI WATANABE, RYOZO HAYASHI, ...1984 Volume 32 Issue 1 Pages 251-257
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEnantiomer ratios of 2-[4-(2-oxocyclopentylmethyl) phenyl] propionic acid (loxoprofen) and its monohydroxy metabolites in plasma of rats were determined by high performance liquid chromatography (HPLC) after derivatization with the chiral reagent, (1S)-1-(4-dimethylaminonaphthalen-1-yl) ethylamine. The ratios of (2S)-to (2R)-isomers of the parent acid and 2-[4-(trans-2-hydroxycyclopentylmethyl) phenyl] propionic acid (trans-alcohol) increased rapidly with time after oral administration of racemic and (2R)-loxoprofen, while the (2S)-configuration remained completely intact after dosing with (2S)-isomer. The results clearly indicate the occurrence of irreversible optical inversion of (2R)-to (2S)-loxoprofen in rats. The administration of trans-and cis-alcohols showed that : (1) the optical inversion also occurs in these monohydroxy metabolites, (2) the cis-alcohol is easily converted to the transalcohol through the parent acid, but the latter is not converted to the former.View full abstractDownload PDF (676K) -
SHUNJI NARUTO, YORIHISA TANAKA, RYOZO HAYASHI, ATSUSUKE TERADA1984 Volume 32 Issue 1 Pages 258-267
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe main metabolites of loxoprofen sodium were isolated from rat urine by column chromatography. Their chemical structures were determined on the basis of spectral data and by comparison of the metabolites with authentic samples to be as follows : the parent acid (M-0), two reduction products, i.e., the cis-alcohol (M-1) and the trans-alcohol (M-2), the α-hydroxy ketone (M-3) and three diol metabolites (M-4, M-5 and M-6). The established metabolite structures all indicated that metabolic reactions of loxoprofen in rats occur only at the cyclopentanone moiety. The trans-alcohol metabolite, which has a high inhibitory activity on prostaglandin (PG)-synthetase, was determined to be optically pure, with (2S, 1'R, 2'S)-configurations, by high performance liquid chromatography (HPLC) analysis after derivatization to the diastereomeric amide of the carboxy group with (-)-α-phenylethylamine reagent, and subsequently to the ester of the hydroxy function using (-)-α-methoxy-α-trifluoromethylphenylacetyl chloride.View full abstractDownload PDF (856K) -
KAZUO KUSHIDA, KEIJI MASAKI, MASAYOSHI MATSUMURA, TAEYUKI OHSHIMA, HIR ...1984 Volume 32 Issue 1 Pages 268-274
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo improve drug penetration through the skin, we studied the effect of calcium thioglycolate (Ca-TGA) on the percutaneous absorption of theophylline in comparison with the promoting effects of dimethylsulfoxide (DMSO) and polyoxyethylenelaurylether (BL-9EX). Plasma theophylline concentrations were determined following dermal application of aminophylline to male rats in vivo. The use of aqueous 4w/v% Ca-TGA gave a plasma concentration about 40 times as high as that of the control. whereas 80v/v% DMSO and 20w/v% BL-9EX gave concentrations about 9 times as high as that of the control at most. To obtain a marked promoting effect with Ca-TGA, a pretreatment time of more than 10 min was needed. When Ca-TGA was removed, the promoting effect gradually disappeared and the control value was reached at 48h. Furthermore, when pretreatments with Ca-TGA and BL-9EX were combined, the transdermal delivery of theophylline was promoted more than by each treatment alone.View full abstractDownload PDF (690K) -
KANETO UEKAMA, AKIHIKO FUJISE, FUMITOSHI HIRAYAMA, MASAKI OTAGIRI, KOH ...1984 Volume 32 Issue 1 Pages 275-279
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSInclusion complexation of prostaglandin E1 (PGE1) with γ-cyclodextrin (γ-CyD) in aqueous solution and in the solid phase was assessed by the solubility method, X-ray diffractometry, and thermal analysis. A solid complex of PGE1-γ-CyD in a 1 : 2 molar ratio was obtained, and its dissolution behavior and chemical stability were examined. The dissolution rate of the γ-CyD complex was extremely large compared with that of PGE1. In addition, the dehydration of PGE1 to PGA1 was significantly retarded by inclusion complex formation. The data suggest that γ-CyD complex may have great utility as a fast-dissolving form of PGE1 with good storage properties.View full abstractDownload PDF (520K) -
TAKESHI OHYA, SABURO KANNO1984 Volume 32 Issue 1 Pages 280-283
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCyanogen chloride was formed by the reactions of aromatic amino acids such as phenylalanine, tyrosine, tryptophan and histidine with hypochlorous acid in the presence of ammonium ion. It was found that the formation of cyanogen chloride was due to cleavage of the aromatic rings of the aromatic amino acids by chloramine.View full abstractDownload PDF (418K) -
HIDEJI ITOKAWA, KOICHI TAKEYA, NOBORU MORI, TOSHINORI HAMANAKA, TORU S ...1984 Volume 32 Issue 1 Pages 284-290
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe details of the isolation and antitumor activity of cyclic hexapeptides (RA-VII, RA-V, RA-IV and RA-III) isolated from Rubia cordifolia are reported. Studies on a spectrum of experimental tumors in mice revealed that the peptides exhibited significant activity against leukemias and ascites tumors, P-388, L1210, B-16 melanoma and solid tumors, colon 38, Lewis lung carcinoma and Ehrlich carcinoma. RA-V had an especially potent effect on MM2 mammary carcinoma in mice. The effective dose range of RA-IV against P-388 leukemia was different from those of the other cyclic hexapeptides.View full abstractDownload PDF (587K) -
KAZUMI SUEMATSU1984 Volume 32 Issue 1 Pages 291-294
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA C≡N bond was found to transform into a C=N bond under such a mild conditions as to mix trichloroacetonitrile, metal salts and methanol at 20 C. Ni (II) and Co (II) gave dimeric ring complexes and Mn (II) gave amidine, aminotriazine and brown powder. The aminotriazine was isolated as unstable liquid which spontaneously transformed into the crystal. A trimer structure was proposed for the liquid. In anhydrous systems, any oligomerization did not occur, so water was concluded to participate in the initiation.View full abstractDownload PDF (429K) -
YASUAKI HIRAI, SHUICHI SANADA, YOSHITERU IDA, JUNZO SHOJI1984 Volume 32 Issue 1 Pages 295-301
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe constituents of the leaves, stems and underground parts of Trachycarpus fortunei (HOOK.) H. WENDL. (Palmae) have been investigated. Glucoluteolin (3), luteolin 7-O-rutinoside (=scolymoside, 4) and methyl proto-Pb (6) from the leaves, dioscin (1), Pb (2), methyl protodioscin (5) and methyl proto-Pb (6) from the stems, and dioscin (1) and methyl proto-Pb (6) from the underground parts were isolated and identified. This is the first report of the isolation of steroidal saponins from Palmae plants and these results are interesting from the standpoint of chemotaxonomy.View full abstractDownload PDF (720K) -
YOSHIKI HAMADA, ISAO TAKEUCHI, KAZUKO YAMAMOTO, MINORU HIROTA, HIROKO ...1984 Volume 32 Issue 1 Pages 302-304
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe title compounds were prepared by nucleophilic substitution by tetrazole anion of the corresponding bromide (1). followed by hydrolysis and methanesulfonylation. The site of alkylation of the tetrazole anion was determined by comparison of the 13C-nuclear magnetic resonance spectrum with those of N-methyltetrazoles.View full abstractDownload PDF (373K) -
ISAO OZAWA, ISAO TAKEUCHI, KAZUKO YAMAMOTO, YOSHIKI HAMADA, TOMIYOSHI ...1984 Volume 32 Issue 1 Pages 305-312
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe condensation of 4-halo-o-toluidine with salicylic acid or 5-halosalicylic acid was carried out by the use of phosphorus trichloride in xylene to obtain the salicylanilides 1-13, 4-Halo (or nitro)-o-toluidine, 4-halo-o-nitroaniline or 2, 4-dihaloaniline was condensed with 3, 5-dihalosalicylic acid to provide the salicylanilides 14-30 by the same method. The salicylanilides 2-15, 26 and 27 gave the acetylated compounds 31-46 on treatment with acetic anhydride and pyridine. The salicylanilides 26 and 27 gave the methylated compounds 47 and 48 on treatment with dimethyl sulfate. In the antimicrobial activity tests of the synthesized compounds, 4', 5-dihalo-2'-methylsalicylanilides 1-13 and the acetylated compounds 31-42 showed strong antimicrobial activity against some Eumycetes at the minimum inhibitory concentration (MIC) of 0.8 μg/ml. Compound 3 was shown to have a strong preventive activity against downy mildew of cucumber.View full abstractDownload PDF (627K) -
YOSHISUKE TSUDA, KEIICHI YAMAGUCHI, SHINICHIRO SAKAI1984 Volume 32 Issue 1 Pages 313-317
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSingle crystals of onoceranedione-I grown in CH2Cl2-methanol are orthorhombic, a=13.326, b=16.507, c=12.092 Å, U=2659.9 Å3, Dc=1.11g/cm3, Z=4, with space group P212121. The structure, solved by use of the MULTAN program, revealed that the conformations of the two terminal rings are boat forms, which are flexible even in the crystalline state. The positive circular dichroism spectrum of the compound is discussed in connection with the above results.View full abstractDownload PDF (425K) -
MICHIO KIMURA, ICHIZO OKABAYASHI, NORITAKE YASUOKA1984 Volume 32 Issue 1 Pages 318-321
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe molecular and crystal structure of 5-amino-2, 4-dihydro-2-phenyl-3H-pyrazol-3-one was examined by the X-ray diffraction method to establish the predominant tautomeric form (the CH-form) due to the pyrazol-3-one ring. In the crystal, the molecules are linked by the intermolecular hydrogen bond between the NH2 and C=O groups to form four hydrogen bonds with three adjacent molecules. The title compound, C9H9N3O crystallizes in space group P21/a with lattice parameters a=10.187 (5), b=11.481 (4), c=7.392 (4) Å, β=102.43 (5)°, and Z=4.View full abstractDownload PDF (442K) -
TETSUYA TAKEYA, SEISHO TOBINAGA1984 Volume 32 Issue 1 Pages 322-324
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxidation of the di (1-propenyl)-biphenyl 3a with the CrO3-HBF4-MeCN reagent system gave a novel oxidation product 4a, which was subsequently transformed to the phenanthrenes 5 and 6.View full abstractDownload PDF (364K) -
ATSUSHI NUMATA, TAKAKO KATSUNO, KYOKO YAMAMOTO, TOMOKO NISHIDA, TSURUK ...1984 Volume 32 Issue 1 Pages 325-331
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNine species of plants having antifeeding activities for the larvae of the yellow butterfly, Eurema hecabe mandarina DE L'ORZA, were found. From one of them, Arachniodes standishii (MOORE) OHWI, the known compound, 1-(2, 4, 6-trimethoxyphenyl) but-trans-2-en-1-one (I), was isolated as an antifeedant. This compound was synthesized according to the Friedel-Crafts procedure, which also gave two new compounds, 1, 3-bis (2, 4, 6-trimethoxyphenyl) butan-1-one (VI) and 1-(2, 4, 6-trimethoxyphenyl)-3-[3-(2-trans-butenoyl)-2, 4, 6-trimethoxyphenyl] butan-1-one (VII), as by-products. Treatment of 1, 3, 5-trimethoxybenzene (V) with ferric chloride was found to afford 2, 2', 4, 4', 6, 6'-hexamethoxybiphenyl (VIII), which has been synthesized according to Ullmann's procedure.View full abstractDownload PDF (597K) -
TAKAO KANEKO, MITSUYOSHI MATSUO1984 Volume 32 Issue 1 Pages 332-335
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe rearrangement of linoleic acid hydroperoxides, (9Z, 11E)-13-hydroperoxy-9, 11-and (9E, 11E)-13-hydroperoxy-9, 11-octadecadienoic acids (13-Z, E-LOOH and 13-E, E-LOOH, respectively), occurred under argon and under degassed conditions, as well as under aerobic conditions. In argon-saturated benzene, 13-Z, E-LOOH isomerized to 9-E, E-and 13-E, E-LOOHs, and 13-E, E-LOOH to 9-E, E-LOOH ; the E, E-isomers hardly isomerized to E, Z-isomers. The hydroperoxides isomerized rapidly in benzene and chloroform, but slowly in n-propyl ether and methanol. However, they decomposed extensively in chloroform, and moderately in benzene and methanol. Decomposition was very slight in n-propyl ether. The isomerization rate of the 9Z, 11E-isomer was much higher than that of the 9E, 11E-isomer. Since the rate was found to be slow under degassed conditions, traces of dissolved molecular oxygen may be responsible for the isomerization.View full abstractDownload PDF (428K) -
EISUKE SATO, MAKIKO MIYAKAWA, YUICHI KANAOKA1984 Volume 32 Issue 1 Pages 336-339
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Amino-7-nitrobenz-2-oxa-1, 3-diazole (1b) is a potentially useful key fluorogenic amine. As an example of the application of this amine, 7-(N-tosyl-and N-mesyl-L-phenylalanyl) amino-4-nitrobenz-2-oxa-1, 3-diazole (2) were prepared and shown to be good fluorogenic substrates for the assay of chymotrypsin.View full abstractDownload PDF (431K) -
TSUNEJI NAGAI, SOMPOL PRAKONGPAN1984 Volume 32 Issue 1 Pages 340-343
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe solubilities of acetaminophen (N-(4-hydroxyphenyl) acetamide) (ACA) were determined in various aqueous cosolvent mixtures, i.e., ethanol-water, polyethylene glycol 400 (PEG 400)-water and polyethylene glycol 4000 (PEG 4000)-water, by ultraviolet spectrophotometry at 244nm, a 30±2°C. The mixed solvents were prepared by mixing known volumes of solvents except in the case of PEG 4000-water where weight by volume (w/w) was used. In the above aqueous cosolvent systems, the solubility of ACA increased with cosolvent concentration and the maximum appeared at about 80% cosolvent concentration. When the solubilities of ACA were plotted against the approximate dielectric constants, which were calculated from the sum of the product of the volume composition with the dielectric constants of the individual components, peaks were found at dielectric constant values of 25 and 35 for PEG 400-water and ethanol-water, respectively. The solubility was fitted to a log linear solubility equation proposed by Yalkowski et al., which gave a good linear fit up to 40% cosolvent in all water-cosolvent mixtures. These results should be useful in the formulation of both oral and injectable ACA solutions.View full abstractDownload PDF (473K) -
TAKAKO INOUE, YUKIO KANDA, TOHRU KISHI, TOKIYASU SAKAI, SHINICHI SUZUK ...1984 Volume 32 Issue 1 Pages 344-347
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethamphetamine excreted in urine of habitual users was analyzed by radioimmunoassay using specific antiserum prepared by the method previously described. As a labeled compound, 3H-methamphetamine was employed instead of the 125I-methamphetamine derivative used in previous studies, on grounds of sensitivity. The results obtained by this radioimmunoassay were compared with those obtained by conventional methods, and good agreement was found.View full abstractDownload PDF (418K) -
SABURO KANNO, TAKESHI OHYA1984 Volume 32 Issue 1 Pages 348-349
Published: January 25, 1984
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was found that aniline [13C6] reacted with nitrous acid to give 13CN- and that benzene [13C6] or aniline [13C6] reacted with hypochlorous acid in the presence of ammonium ion to give 13CNCl. These results clearly indicate that the benzene ring was cleaved by nitrous acid or chloramine to give cyanide ion or cyanogen chloride.View full abstractDownload PDF (315K)