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Volume 86, Issue 9
Displaying 1-29 of 29 articles from this issue
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Kiichiro Kakemi, Takaichi Arita, Mikiko Hashi, Kiyoko Sumii1966 Volume 86 Issue 9 Pages 739-744
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe binding of 1-cyclohexyl-5-n-butyl-2, 4, 6-trioxoperhydropyrimidine (BCP) to bovine serum albumin was investigated using equlibrium dialysis method. BCP appears to be bound to two groups of sites on albumin (n1=1.02, n2=6.98) with the values for K1 of 108×103 M-1 and K2 of 1.35×103 M-1. It was demonstrated by the use of control human serum and crystallized human serum albumin that albumin had the most significant binding properties among the protein in human serum. The extent of binding was influenced by buffer constitution ; no significant difference in the binding with phosphate buffer, inhibitory effect with formate buffer, and with ammonium buffer, Cl- ion was inhibitory and NH4+ ion was accelerating. With increasing pH values, a progressive decrease in their binding occurred between pH 4 and 10 where there was a marked decrease in the binding. By investigating the effect of phenylbutazone on BCP binding, it was observed that BCP had some common binding sites with phenylbutazone and the binding affinity of BCP on this sites was 4 times weaker than phenylbutazone.View full abstractDownload PDF (687K) -
Gas Chromatographic Determination of Diisopropylamine Dichloroacetate in Pharmaceutical PreparationsKazue Hasegawa, Setsuya Seno1966 Volume 86 Issue 9 Pages 744-748
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFundamental conditions were examined for the gas chromatographic determination of diisopropylamine dichloroacetate (DADA) by the method of nitrosation-extraction. To 10 ml. of the sample solution containing 1∼10 mg. of DADA, 2.5 ml. of glacial acetic acid and 5 ml. of 50% sodium nitrite solution are added, and the mixture is allowed to react for 5 minutes at 60°. When cooled, the solution is made alkaline with 7 ml. of 50% potassium hydroxide solution, and extracted with 10 ml. of cyclohexane containing 5 mg. of p-dibromo-benzene as an internal standard. The extracted solution is centrifuged, concentrated in a vacuum to 0.5∼1 ml., and injected at column temperature of 160° into the gas chromatograph with polyethylene glycol succinate (5%) on Celite 545 column. When N-nitrosodiisobutylamine is used as an internal standard, 10 ml. of 0.5% diisobutylamine hydrochloride solution is added to the sample solution, nitrosated, and extracted with 10 ml. of cyclohexane. The proposed method is reproducible and may be used for samples containing many other substances, such as biological fluids.View full abstractDownload PDF (607K) -
Motoyoshi Yamazaki, Noriko Honjo, Kanji Noda, Yayoi Chono, Masatomo Ha ...1966 Volume 86 Issue 9 Pages 749-755
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS2-Halogenoquinoline 1-oxides were prepared in comparatively good yield by the use of permaleic acid as the N-oxidation agent, making it possible to obtain compounds which had hitherto been difficult to prepare. 2-Chloro-and 2-bromo-quinoline 1-oxides and 2-chloro-and 2-bromo-lepidine 1-oxides were prepared by this method. Several kinds of 2-substituted quinoline 1-oxides were prepared by the reaction of 2-chloroquinoline 1-oxide and lepidine 1-oxide with various nucleophilic reagents.View full abstractDownload PDF (819K) -
Kazuko Ohta1966 Volume 86 Issue 9 Pages 756-759
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSLocal anesthetic action of recently synthesized 2-naphthalenealkylamines was tested. Surface anesthetic action was tested by the corneal reflex of a guinea pig and N-alkyl-N-methyl-2-naphthaleneethyl (or propyl) amines (XIb∼f, XIIb∼f) all showed activites stronger than that of procaine, and N-methyl-N-pentyl-2-naphtha1eneethylamine (XIf) was especially strong, the potency being 16 times that of procaine. The activity decreased when the compounds of this series were derived to methiodide, and only the N-butyl and N-pentyl compounds showed a weak activity. This fact seems to indicate the possibility that the base of a compound takes part in appearance of the activity. Primary amines (IIa to Xa) generally had strong irritant psoperty N, N-Dimethyl derivatives (IIb to Xb) showed the activity only when the number of carbon atoms in the side chain was 2 (IVb) or 3 (Vb), and all higher homologs had strong toxicity necrosis. Conduction anesthetic activity was examined with frog sciatic nerve in compounds of XI and XII series and their potency was compared with that of procaine. Approximately similar structure-activity relationship as in the case of surface anesthetic activity was found.View full abstractDownload PDF (462K) -
Shin-ichiro Sakai, Akinori Kubo, Takenori Hamamoto, Chikako Ueda1966 Volume 86 Issue 9 Pages 760-763
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSCondensation of tryptamine with ethyl β-diethoxyethylmalonate (II) and ethyl 3-diethoxy-carbonyl-5-diethoxyvalerate (III) was carried out by the Pictet-Spengler reaction. The products of this reaction were ethyl 3-oxo-1, 2, 3, 5, 6, 11b(H)hexahydroindo1o[3, 2-g]pyrrocoline-2-carboxylate (V) (Fig.2), and diethyl 4-oxo-1, 2, 3, 4, 6, 7, 12, 12b-octahydroindolo[2, 3-a]pyrido-coline-2-dicarboxylate (VII), and a by-product, ethyl 2-ethoxycarbonyl-3-oxo-1, 2, 3, 5, 6, 11b-hexahydroindo1o[3, 2-g]pyrrocoline-2-acetate (VIII). V was identified by its derivation to the known 3-oxo-1, 2, 3, 5, 6, 11b-hexahydro-11H-indolo[3, 2-g]pyrrocoline.View full abstractDownload PDF (574K) -
Masao Tomita, Sheng-Teh Lu, Yueh-Ying Chen1966 Volume 86 Issue 9 Pages 763-766
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAlkaloidal components in the tree bark of Formosan Hernandia ovigera L. (Hernandiaceae) were examined and thalicarpine (IV), xanthoplanine (V), and a new aporphine-type alkaloid, hernovine were isolated. Hernovine, m.p. 143∼145° (sint. 130°), C18H15O4N, was proved to have the structure represented by formula (I) from the measurement of ultraviolet spectrum (Fig.1) and NMR spectrum.View full abstractDownload PDF (601K) -
Toshihiko Okamoto, Sadao Hayashi1966 Volume 86 Issue 9 Pages 766-773
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSCoupling of diazonium salt with N-aminopyridinium derivatives (I and II) affords an azido derivative and pyridine. Diazonium salts used were p-nitro-(III), m-nitro-(IV), and o-nitro-benzene (V), and diazonium chlorides of benzene (VI), pyridine (VII), pyridine 1-oxide (VIII), 4-ethoxycarbonylpyrazole (XXIV), 4, 5-dimethylthiazole (XXVII), and 2, 4-dinitrobenzenediazonium sulfate (XXX). Attempts to isolate the intermediate (XXIII or XXV) in the reaction of III or XXIV with N-aminopyridinium chloride (I) did not materialize due to the lability of the intermediate but some assumption was made on the mechanism of deamination which is similar to that of deoxygenation of pyridine 1-oxide with phosphorus trichloride. Reaction of III with N-aminopyridinium iodide (II) afforded p-nitroiodobenzene (XIX) and a small amount of the azido compound (IX), while the reaction of XXVII and I afforded an azoxy compound (XXVIII) besides the azido compound (XXIX).View full abstractDownload PDF (904K) -
Akira Mizutani, Masaki Saito, Katsuhiko Yamamoto1966 Volume 86 Issue 9 Pages 774-778
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSEffect of the intravenous injection of Parotin-A on serum citric acid in rabbits was investigated. Parotin (clinical use) was examined simultaneously in order to compare with the citric acid activity of Parotin-A. When the experiments were carried out using rabbits which were fed as usual, the variations of percentage decrease in serum citric acid were so large that the difference between the treated animals and controls injected with 0.9% saline solution was not statistically significant, especially when small doses were employed such as in this experiment. For that reason, the experiments were followed by use of the fasting animals. After fasting for 24 hours, the rabbits were injected with 0.1 mg. of Parotin-A per kg. body weight. The blood was drawn just before the injection and also 9 and 24 hours after injection, and serum citric acid was measured. In the case of 0.1 mg. administration only 9 hours' value differed significantly from that of the controls, and in the case of 0.3 mg. administration, both 9 and 24 hours' values were statistically significant. On the other hand, administration of 1.0 mg./kg. of Parotin (clinical use) caused significant decrease of serum citric acid only at 9 hours' value.View full abstractDownload PDF (621K) -
Kiichiro Kakemi, Takaichi Arita, Ryohei Hori, Tomoaki Kiyotaki, Hirosh ...1966 Volume 86 Issue 9 Pages 778-785
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSω, ω'-Bis(2, 3, 4-trihydroxyphenyl)alkanes, which are pyrrogallol derivatives, with zero to 10 carbons in the chain were systematically synthesized and their antioxidant action against vitamin A acetate was examined. The starting material used was pyrrogallol trimethyl ether which was condensed with dicarboxylic chloride by the Friedel-Crafts reaction to form ketones, which were catalytically reduced, and finally demethylated to the objective compounds. For the examination of the antioxidant action of these derivatives, vitamin A acetate was dissolved in pure ethyl laurate to obtain a vitamin A oil, a definite amount of each of these derivatives was added to the oil, and the decomposition rate of vitamin A acetate was compared with that of the control in the absence of the antioxidation agent. Some of the compounds showed a fairly good effect compared to nordihydroguaiaretic acid.View full abstractDownload PDF (847K) -
Kiichiro Kakemi, Takaichi Arita, Ryohei Hori, Hiroshi Takenaka1966 Volume 86 Issue 9 Pages 785-791
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn continuation of the previous work on the syntheses of pyrrogallol-methylene-bis derivatives to obtain effective antioxidant for vitamin A, systematic syntheses were carried out on hydroquinone derivatives, ω, ω'-bis(2, 5-dihydroxyphenyl)alkanes and ω, ω'-bis(2-hydroxy-5-methoxyphenyl)alkanes. The former was obtained generally by the condensation of hydroquinone dimethyl ether and dicarboxylic chloride by the Friedel-Crafts reaction to the ketones, which were catalytically reduced, and finally demethylated to the objective compounds. The latter was obtained by acetylation of the hydroxyketones, formed during the Friedel-Crafts reaction, and catalytic reduction of its product to the objective compounds. Antioxidant action of these derivatives was tested by the decomposition rate of vitamin A acetate, as reported before, and all the hydroquinone derivatives showed antioxidant activity, and ω, ω'-bis(2-hydroxy-5-methoxyphenyl)alkanes, in which one of the hydroxyls had been methylated, showed especially good antioxidant activity.View full abstractDownload PDF (815K) -
Kiichiro Kakemi, Takaichi Arita, Ryohei Hori, Hiroshi Takenaka1966 Volume 86 Issue 9 Pages 791-796
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn order to elucidate the correlation between chemical structure and antioxidant effect, syntheses were systematically carried out on the phenol derivatives of ω, ω'-bis(2-hydroxyphenyl)alkanes (Ia), ω, ω'-bis(3-hydroxyphenyl)alkanes (Ib), and ω, ω'-bis(4-hydroxyphenyl)-alkanes (Ic), and cresol derivatives of ω, ω'-bis(2-hydroxy-3-methylphenyl)alkanes (IIa), ω, ω'-bis(2-hydroxy-4-methylphenyl)alkanes (IIb), and ω, ω'-bis(2-hydroxy-5-methylphenyl)alkanes (IIc), with 5, 7, and 10 carbons in the chain. Compounds of Ia, IIa, and IIb series were obtained by deriving the corresponding phenols to their esters, their Fries rearrangement to hydroxyketones, and their Clemmensen reduction to the objective compounds. Compounds of Ib series were obtained from m-nitro derivatives by hydroxylation by the conventional method. Compounds of Ic and IIc series were obtained from the methyl ethers of the corresponding phenols by the method previously described. Antioxidant ability of these derivatives was examined and the compounds of II series with methyl group had better antioxidant activity than those of I series without the methyl group.View full abstractDownload PDF (662K) -
Kiichiro Kakemi, Takaichi Arita, Ryohei Hori, Hiroshi Takenaka, Hirosh ...1966 Volume 86 Issue 9 Pages 797-802
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFollowing the systeinatic syntheses of various phenol derivatives and examination of a relation the kind, number, and position of their substituents to the antioxidant action of these compounds, systematic syntheses were carried out to obtain compounds having an amino group with marked electrondonating nature. The compounds synthesized were p-aminophenol derivatives of ω, ω'-bis(2-hydroxy-5-aminophenyl)alkanes (A), ω, ω'-bis(2-hydroxy-5-dimethylaminophenyl)alkanes (C), ω, ω'-bis(2-hydroxy-4-methyl-5-aminophenyl)-alkanes (D), and ω, ω'-bis(2-hydroxy-3, 4-dimethoxy-5-aminophenyl)alkanes (E), with 5, 7, and 10 carbons in the alkanes. Compounds of (A), (D), and (E) series were obtained by deriving the corresponding phenols to azo compounds and reduced with sodium thiosulfate. Compounds of (B) series were obtained by formylation of (A) compounds and reduction of its products with lithium aluminum hydride. Compounds of (C) series were obtained by catalytic reduction of (A) compounds in the presence of formaldehyde. Examination of the antioxidant activity of these compounds was examined as in the preceding work, and all the compounds showed a fairly good antioxidant effect, especially those of the (B) series.View full abstractDownload PDF (771K) -
Hikaru Ozawa, Susumu Sato1966 Volume 86 Issue 9 Pages 802-809
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPharmacological properties, mainly in adrenergic mechanisms, of several geanethidine analogues were comparatively examined with the following compounds : [2-(hexahydro-1-azepinyl) ethyl] guanidine sulfate (G-7), [2-(1-piperidino) ethyl]guanidine sulfate (G-6), [2-(1-pyrrolidinyl)ethyl]guanidine sulfate (G-5), [2-(diethylamino)ethyl)guanidine sulfate (I), [2-(dipropylamino)ethyl]guanidine sulfate (II), [2-(diisopropylamino)ethyl]guanidine sulfate (III), [2-(dibuthylamino)ethyl]guanidine sulfate (IV), [2-(methylphenylamino)ethyl]guanidine sulfate (V), [2-(diphenylamino)ethyl]guanidine sulfate (VI), [2-(dibenzylamino)ethyl]guanidine sulfate (VII), and [2-(methylcyclohexylamino)ethyl]guanidine sulfate (VIII). The antagonistic action of the compounds against inhibitory effect of adrenergic nerve stimulation on isolated rabbit ileum was examined. The pyrrolidinyl (G-5) and piperidino analogues (G-6) possessed only moderate activities which increased in the hexahydro-1-azepinyl analogue (G-7) and reached a maximum in the eight-membered ring (guanethidine). The compound with the nitrogen atom outside the ring, viz., methylcyclohexylamino analogue (VIII) had a reduced activity. The diethylamino analogue (I) possessed only a moderate activity, which declined with larger dialkylamino analogue (II, III, IV), and the activity was completely lost by replacement of the two alkyl groups with aromatic (VI) or aralkyl (VII) group. Guanethidine, G-7, G-6, G-5, I, and V caused supersensitivity to noradrenaline or adrenaline, and subsensitivity to tyramine in rat blood pressure and cat nictitating membrane, but the activity of VIII was very slight. Furthermore, these compounds also inhibited the contraction of cat nictitating membrane which was elicited by electrical stimulation to preganglionic superior cervical nerve.View full abstractDownload PDF (944K) -
Tetsuji Kametani, Kunio Ogasawara, Masahisa Shio1966 Volume 86 Issue 9 Pages 809-815
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSynthesis of streptonigrin (I) and its derivative (II) was attempted. The demethyl derivative of the A/B ring of I and A/B ring of II have already been synthesized and, in the present series of work, synthesis of C/D ring of these compounds was examined. At the same time, pharmacological activities of the compounds formed during the syntheses were examined. For this purpose, attempt was made to extend the synthetic reactions used by Eby and Hauser in which benzoylacetonitrile was treated with polyphosphoric acid to obtain the amide which, without its isolation, was treated with acetone to obtain 6-methyl-4-phenyl-2-pyridone. In order to increase one methyl group in 5-position and to obtain the pyridone compound which can be derived to the C/D ring of streptonigrin, a preliminary experiment was carried out with benzoylacetonitrile and methyl ethyl ketone which were treated with polyphosphoric acid. The product thereby obtained was found to have a methyl group in the 5-position, as was expected, by examination of its NMR spectrum. Therefore, 2, 3, 4, -trimethoxybenzoylacetonitrile was prepared and this was treated as above and 4-(2, 3, 4-trimethoxyphenyl)-5, 6-dimethyl-2-pyridone (VIIIb) was obtained. In order to introduce an amino group into the 3-position of this compound, nitration and bromination were attempted but no satisfactory result was obtained.View full abstractDownload PDF (888K) -
Tetsuji Kametani, Kunio Ogasawara, Atsuto Kozuka1966 Volume 86 Issue 9 Pages 815-822
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSome of the polysubstituted 4-phenylpyridine derivatives show pharmacological activity and, therefore, synthesis was attempted for compounds having a structure similar to the 4-phenylpyridine skeleton present in the structure of streptonigrin. First, examinations were made for the synthesis of C-D rings in streptonigrin and synthesis was effected for 4-(3, 4-methylenedioxyphenyl)-3-cyano-5-ethoxycarbonyl-6-methyl-2-quinolylpyridine, which has a streptonigrin skeleton and a substituent that could be derived to its C ring. The methods used for these syntheses can be classifield into the following three : (1) Condensation of α-cyanocinnamide and ethyl 3-aminocrotonate, (2) Condensation of cyanoacetamide with the product of the Claisen-Schmidt reaction, and (3) the Hantzsch-type synthesis. 4-Phenylpyridine was obtained as the product using methods (1) and (2). The condensation intermediate in these reactions was dihydropyridone compound and its oxidation to pyridone gave a poor yield of the product but the oxidation product was obtained directly when the substituent in the 4-position was piperonal. Attempt to introduce one more substituent into the pyridine ring by the method (2) did not materialize. Oxidation of 1, 4-dihydropyridine derivatives (XXa∼b), obtained by method (3), to pyridine derivatives (XXIa∼b) was not effected by the use of dilute nitric acid, chromic acid, palladium black, or palladium carbon, and it is interesting that the oxidation product was finally obtained by heating the dihydro compounds in a sealed tube with mercury acetate to above the melting point of them.View full abstractDownload PDF (972K) -
Tetsuji Kametani, Seiichi Takano, Osamu Umezawa, Hideo Agui, Kazuko Ka ...1966 Volume 86 Issue 9 Pages 823-828
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSReaction of various heterocyclic carboxylic acid hydrazides, such as 2-thiophenecarboxylic acid, 2-furancarboxylic acid, picolinic acid, nicotinic acid, and isonicotinic acid, with alkylamines, aralkylamines, and aromatic and hydroaromatic amines in the presence of chloral was carried out to effect a new type of dehydrazination to obtain amides including 14 kinds of hitherto unknown heterocyclic amido compounds. During this reaction, the with reaction of 1-picolinoyl-2-(2, 2, 2-trichloroethylidene)hydrazine (X), one of the intermediates, aniline in the cold afforded a new substance considered to be 1-(picolinoyl)-2-[2-anilino-2-(N-phenylimino)ethylidene]hydrazine (XVIII) in a good yield.View full abstractDownload PDF (810K) -
Ichizo Okabayashi, Kayoko Okochi1966 Volume 86 Issue 9 Pages 828-832
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSXanthenatom-9-ol (I) undergoes condensation with many compounds possessing an active hydrogen atom but not with diethyl malonate under ordinary conditions. Diethyl xanthene-9-malonate (IV) was obtained by the reaction of silver xanthene-9-malonate and ethyl iodide. I underwent facile condensation with ethyl malonate to form monoethyl xanthene-9-malonate (V) which was derived to 2-diethylaminoethyl ethyl xanthene-9-malonate hydro chloride (VI) and ethyl xanthene-9-malonamate (VII). In a similar manner, diethyl thioxan thene-9-malonate (XI), monoethyl thioxanthene-9-malonate (XII), 2-diethylaminoethyl ethyl thioxanthene-9-malonate hydrochloride (XIII), and ethyl thioxanthene-9-malonamate (XIV) were synthesized from thioxanthen-9-ol (VIII). Oxidation of XII with hydrogen peroxide gave monoethyl thioxanthene-9-malonate 10, 10-dioxide (XV) which was derived to 2-diethylaminoethyl ethyl thioxanthene-9-malonate 10, 10-dioxide hydrochloride (XVII). Oxidation of XIV gave ethyl thioxanthene-9-malonamate 10, 10-dioxide (XVIII). Antiacetylcholine action of XVII is stronger than that of 2-diethylaminoethyl thioxanthene-9-acetate 10, 10-dioxide hydrochloride, but both VI and XIII have weaker antiacetylcholine, anti-barium chloride, and antihistamine activities than the corresponding acetate derivatives.View full abstractDownload PDF (681K) -
Masaru Aoki, Noboru Yata1966 Volume 86 Issue 9 Pages 832-836
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTen kinds of dibucaine salts were prepared. Effects of some counter ions on effective duration of surface anesthesia with dibucaine base on the rabbit cornea were studied, with reference to their effects on physicochemical properties of the base. Solvent affinity of dibucaine base, especially solubility in water and distribution ratio between chloroform and water were found to be influenced by the presence of counter ions. It seemed that the change in solvent affinity was influenced by the change of hydrolytic constant of dibucaine salts. Logarithmic plots of effective duration against distribution ratio revealed a significant correlation coefficient of r=0.81. It was demonstrated that the higher the distribution ratio, the longer the effective duration.View full abstractDownload PDF (661K) -
Masaru Aoki, Noboru Yata1966 Volume 86 Issue 9 Pages 836-840
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA new method for evaluating local anesthetic action was devised. The apparatus is equipped with compartment box shown in Fig.1, which enabled the frog sciatic nerve fibers to be perfused with saline solution with or without anesthetics. Frog sciatic nerve fibers, following elimination of epineurium, were perfused initially with saline solution followed by an anesthetic solution until the action potential of nerve fibers dropped to one-half the initial potential which had been set at 400 μV. At this stage perfusion was made with the initial saline solution until the action potential recovered by 100 μV. The time required for 50% reduction of the initial action potential was recorded as the "onset time of anesthesia, " and the time required for recovery of action potential by 100 μV as "effective duration of the anesthesia." One-half blocking concentration of anesthetics was determined from the dose-reponse curve thereby obtained. Three local anesthetics were evaluated in terms of onset time, effective duration, and a half-blocking concentration.View full abstractDownload PDF (784K) -
Masaru Aoki, Noboru Yata1966 Volume 86 Issue 9 Pages 841-845
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSEffects of counter ions on the onset time, effective duration, and half-blocking concentration of dibucaine base were evaluated by the method described previously. They were also reviewed in reference to the ratio and rate of distribution between chloroform and water, the rate of permeation through the cellophane membrane, and the rate of diffusion in water were additionally pursued. A certain relationship was found between the ratio of distribution and half-blocking concentration, as was the case between the rate of distribution and onset time or effective duration.View full abstractDownload PDF (627K) -
Masaru Aoki, Noboru Yata1966 Volume 86 Issue 9 Pages 846-849
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSEffects of counter ions on the interaction of dibucaine base and bovine serum albumin were investigated in reference to relations between anesthetic action and thermodynamic properties on protein binding. It seemed that entropy change of the interaction of dibucaine base and albumin was responsible for effective duration and half-blocking concentration of dibucaine base, determined on frog sciatic nerve fibers.View full abstractDownload PDF (520K) -
Masayuki Nakagaki, Naofumi Koga, Hiroshi Terada1966 Volume 86 Issue 9 Pages 849-853
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn order to find the relationship between electric charge and pH of α- and β-crystallins, the main protein of lens cortical proteins, titration curves of these proteins were calculated. 1) Iso-ionic point of α-crystallin was 5.03 and that of β-crystallin, 5.82. Addition of potassium chloride to the iso-ionic protein solution resulted in increased pH value in both proteins. This was thought to indicate that Cl- is selectively bounded to both proteins. 2) Titration curves of α- and β-crystallins were obtained for various ionic strength of potassium chloride, using hydrochloric acid and potassium hydroxide. Dissociation of these proteins was found to be affected by other dissociating groups and by chlorine ion. Structural change was found to occur in α-crystallin at around pH 3.7 and in β-crystallin at around pH 3.4.View full abstractDownload PDF (592K) -
Minoru Sekiya, Yoshiro Osaki1966 Volume 86 Issue 9 Pages 854-856
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS(Formamidocyanoacetyl)urea, (acetamidocyanoacetyl)urea, and their 3-methyl analogs were synthesized. These compounds underwent uracil cyclization by catalytic action of a base, with the exception of (formamidocyanoacetyl)urea, which was directly converted to 3-methylxanthine.View full abstractDownload PDF (454K) -
Shin-ichiro Sakai, Akinori Kubo, Minoru Inaba, Michiko Katagiri, Kayok ...1966 Volume 86 Issue 9 Pages 856-858
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSVarious kinds of 5, 6-dihydropyrro1o[2, 1-a]isoquinolines, listed in Table I, were obtained by the condensation of 1-methyl-3, 4-dihydroisoquinoline and its 6, 7-dimethoxy derivatives with various halogen ketones. Condensation of 1-methyl-3, 4-dihydro-β-carboline with halogen ketone afforded 2-methyl-3-ethoxycarbonyl-5, 6-dihydropyrrolo [2, 1-a] -β-carboline (IX).View full abstractDownload PDF (427K) -
Naobumi Oi1966 Volume 86 Issue 9 Pages 859-860
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA simple infrared spectrophotometric method is offered for rapid simultaneous determination of acetanilide and phenacetine in their pharmaceutical preparations containing acetanilide, phenacetine, and caffeine. Acetone is chosen as the solvent, and the key bands used for acetani1ide and phenacetine are 695 and 827 cm-1, respectively, and these two components can be determined easily without interference of other components by the use of two available base lines. This method gave good results in both standard mixed samples and unknown samples.View full abstractDownload PDF (343K) -
Fukujiro Fujikawa, Isao Yamashita, Tazuko Seno, Motoo Sasaki, Masukazu ...1966 Volume 86 Issue 9 Pages 861-864
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAntibacterial action against human tubercle bacillus, was tested with 23 kinds of indole-3-carboxaldehyde derivatives, including 4-alkylthiosemicarbazones, 4-arylthiosemicarbazones, benzoylhydrazones, and amidinohydrazone hydrochlorides. The microorganisms tested were sensitive strain of H37Rv and heavy resistant strains resistant to 300 γ/ml. of streptomycin, 50γ/ml. of p-aminosalicylic acid, and over 50γ/ml. of isonicotinic acid hydrazide. While the control INAH inhibited the growth for 4 weeks at 0.25 γ/ml. and TBI at 50 γ/ml., most of the compounds tested inhibited the growth at 25 γ/ml. concentration. Therefore, there seemed to be none with excellent antibacterial activity but these compounds were found to have bacteriostatic activity in vitro two times stronger than that of TBI.View full abstractDownload PDF (494K) -
Masatsugu Matsumoto, Michihiko Miyazaki1966 Volume 86 Issue 9 Pages 864-866
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSD-Ribonolactone and D-ribose indicate reduction wave in 1×10-1M tetramethylammonium chloride solution (A solution) or in 1×10-1M tetramethyl ammonium chloride-3×10-2M boric acid solution (B solution, whose half-wave potentials are -2.45, -1.96, -1.86, and -1.97 (vs. S.C.E.). Utilizing this nature, electrolytic reduction of D-ribonolactone with controlled cathode potential was carried out in A or B solution. The product obtained by the use of A solution was D-ribitol and that with B solution was mainly D-ribose. This result was interpreted from the point of half-wave potential. The reason for increased yield of D-ribose in the constant-current electrolyeis of D-ribonolactone by the addition of boric acid was presumed from the foregoing point.View full abstractDownload PDF (466K) -
Torizo Takahashi, Minoru Furukawa, Yoshifumi Maki1966 Volume 86 Issue 9 Pages 867-869
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSN, N-Dimethyl-1-phenyl-3-alkoxypyrazole-5-carboxamide (V : R=CH3, C2H5, C3H5) and N, N-dimethyl-1-phenyl-2-methyl-4-chloro-3-oxopyrazole-5-carboxamide (VI) were synthesized, and (V : R=CH3, C2H5) was found to have an analgesic activity comparable to that of aminopyrine.View full abstractDownload PDF (477K) -
Shin-ichi Sasaki, H.C. Chiang, Kazuo Habaguchi, Taiji Yamada, Koji Nak ...1966 Volume 86 Issue 9 Pages 869-870
Published: September 25, 1966
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFrom several medicinal plants in Taiwan the following compounds were isolated and identified with authentic samples : Dulcitol, uracil, euparin, morin, arjunolic acid, and serratenediol monoacetate.View full abstractDownload PDF (357K)
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