巻号一覧
36 巻, 1 号
選択された号の論文の69件中1～50を表示しています
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中垣 正幸, 井上 和博, 小松 裕明, 半田 哲郎, 宮嶋 孝一郎1988 年 36 巻 1 号 p. 1-7
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe effect of sodium dodecyl sulfale (SDS) concentration on the efficiency of the photooxidation of Methyl Orange sensitized by tetraphenylporphyrin (TPP) in the surfactant solution was investigated. It was found that the efficiency of the photooxidation is lower above the critical micelle concentration of SDS-TPP mixed solution (cmcmix) than below the cmc<mix>. By taking into consideration the formation of an oligomer complex between one TPP molecule and several SDS molecules below the cmc<mix>, it was possible to explain the relatively lower efficiency above the cmc<mix> in terms of the lower reactivity between singlet oxygen produced by the excited TPP and methyl orange (MO) in the less polar environment on the micellar surface.抄録全体を表示PDF形式でダウンロード (688K) -
金岡 又雄, 矢野 三郎, 加藤 弘巳, 中田 貴子, 川村 和弘1988 年 36 巻 1 号 p. 8-14
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーEnzyme immunoassay of glycyrrhetic acid was developed by employing antisera elicited from in rabbits immunized with C-3 bridged glycyrrhetic acid-bovine serum albumin (BSA) conjugate (15, 16) and C-3 bridged glycyrrhetic acid-β-galactosidase conjugate (17, 18) as labeled antigens. Hemisuccinyl and hemiglutaryl groups, which were chosen as the chemical bridges, were introduced at the hydroxy group of tert-butyl glycyrrhetate (2). Immunoassay was performed with bridge heterologous combinations such as anti-glycyrrhetic acid-hemisuccinate-BSA (15) antiserum and glycyrrhetic acid-hemiglutarate-β-galactosidase conjugate (18) and the reverse combination (16 and 17). The sensitivity of enzyme immunoassays (EIA) expressed as the midpoint (logit B/B0=0) was higher in the former combination (2.4 ng/tube) than the reverse combination (8.6 ng/tube). The cross reactivities of the anti-C-3 bridged glycyrrhetic acid antisera with C-3 substituted derivatives of glycyrrhetic acid were higher than those of the anti-C-30 bridged glycyrrhetic acid antiserum.抄録全体を表示PDF形式でダウンロード (729K) -
末宗 洋, 田中 正一, 尾葉石 浩, 酒井 浄1988 年 36 巻 1 号 p. 15-21
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーSynthesis of prostaglandin A2 (PGA2) by means of a route involving enzymatic reactions is described. Enantioselective reduction and hydrolysis of trans-3, 4-bis(methoxycarbonyl)cyclopentanone (1) were examined using yeasts or enzymes, and it was found that (+)- and (-)-1 are easily obtained by an enzymatic procedure. Compound (+)-1 was converted to the Corey intermediate for PGA2 via the regioselective hydrolysis of the (+)-diacetate (8) with porcine pancreatic lipase. This synthesis based on the enzymatic approach was proved to be useful for the synthesis of both PGA and PGE from (-)-1.抄録全体を表示PDF形式でダウンロード (819K) -
早川 聡史, 馬場 順子, 岡本 正夫, 太田 俊作1988 年 36 巻 1 号 p. 22-32
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーReaction of 1, n-bis(1-methyl-1H-imidazol-2-yl)alkane-1, n-dione (8) with an excess of Grignard reagent was examined. In the cases of n=4 and 5, precursors (14) for synthesis of various asymmetric 1, 4- and 1, 5-diketones (12 : R1≠R2), respectively, were obtained in good yields by treating 8 with an excess of methylmagnesium iodide in ether followed by trimethylsilylation. In the case of n≥8, the two carbonyl groups of 8 were both attacked by the Grignard reagent, and the products (11 : R1=R2=CH3) were convertible to symmetrical diketones (12 : R1=R2=CH3) in good yields. In cases of n=6 and 7, the mode of the Grignard reaction was transitional between the two types.抄録全体を表示PDF形式でダウンロード (1119K) -
森元 聡, 野中 源一郎, 西岡 五夫1988 年 36 巻 1 号 p. 33-38
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーNew proanthocyanidin trimers (14 and 15) and tetramers (16 and 17) have been isolated from the whole body of Vaccinium vitis-idaea L. (Ericaceae). The structures of these proanthocyanidins were established by thiolytic degradation and by analyses of the proton and carbon-13 nuclear magnetic resonance spectra. In addition, the presence of (-)-epicatechin (1), (+)-catechin (2), (-)-epigallocatechin (3), (+)-gallocatechin (4), procyanidins B-1 (5), B-3 (6), A-1 (8), and A-2 (9), and cinnamtannins B1 (10), D1 (11), B2 (12), D2(13) in this plant was demonstrated.抄録全体を表示PDF形式でダウンロード (622K) -
森元 聡, 野中 源一郎, 陳 栄福, 西岡 五夫1988 年 36 巻 1 号 p. 39-47
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーTogether with (-)-epiafzelechin (1) and its 3-O-glucoside (4), (-)-epicatechin (2) and procyanidin B-2 (3), seven new biflavanoids (5-7, 9-12) and two triflavanoids (8, 13) have been isolated from the leaves of Cassia fistula L.(Leguminosae). On the basis of chemical and spectroscopic evidence, the structures of 5-8 were established to be proanthocyanidins each having (-)-epiafzelechin unit(s) in the molecule, while 9-13 were shown to consist of (2S)-7, 4'-dihydroxyflavan and (-)-epiafzelechin units.抄録全体を表示PDF形式でダウンロード (906K) -
森 淳, 永井 慎一, 榊原 仁作, 竹谷 和視, 堀田 芳弘1988 年 36 巻 1 号 p. 48-59
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーIn order to investigate the relationship between the chemical structures and the biological activities of proscillaridin (1) and related compounds, transformations of the lactone (1) into the lactams (2a-i) with monoalkylamines, into 1, 4-cycloadducts (3, 5) with dimethyl acetylenedicarboxylate, and into epoxides (6-8) with tris(acetylacetonate)iron(III)-H2O2 have been under-taken. Further, alkoxyalkylation of the teriary C14β-hydroxy group was carried out with alkoxyalkyl halides. The biological activities of the resulting proscillaridin derivatives were studied by the use of isolated guinea-pig papillary muscle preparations and an Na+, K+-adenosine triphosphatase preparation from dog kidney.Although the activities of proscillaridin derivatives were less potent than that of 1, compounds 2a, 2g, 3 and 9 showed slightly expanded concentration ranges of positive inotropic effect development on guinea-pig papillary muscle preparations.A significant correlation was obtained between the van der Waals volumes (Vw) and pIC50 values of 1 and 2a-h (r=-0.09, p<0.01).抄録全体を表示PDF形式でダウンロード (1096K) -
田中 圭, 陳 星, 木村 禎治, 米田 文郎1988 年 36 巻 1 号 p. 60-69
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーVarious 5-arylidene 1, 3-dimethylbarbituric acid derivatives and closely related compounds were synthesized as models of redox coenzymes and used for oxidation of alcohols.Under mild neutral conditions, 5-arylidene 1, 3-dimithylbarbituric acid derivatives, especially those having an electron-withdrawing group on the aromatic ring, effectively oxidized allylic and benzylic alcohols to the corresponding carbonyl compounds. The relationship between the oxidizing ability and the structure of the oxidant (coenzyme model) was investigated and it was found that the electron density on the carbon-carbon double bond is a critical factor for the oxidation. In the case of the deuterium-labeled compound, the observed value of normal and primary isotope effect was 3.3 and so it was concluded that mechanism of this oxidation mainly involves the hydride transfer from the alcohol. An electrochemical investigation was also carried out and the redox potentials of the coenzyme models, 5-arylidene 1, 3-dimethylbarbituric acid derivatives and related compounds, were measured.抄録全体を表示PDF形式でダウンロード (961K) -
家永 和治, 東浦 邦彦, 豊巻 芳男, 松浦 博秀, 木村 宏1988 年 36 巻 1 号 p. 70-77
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe physicochemical and immunochemical properties of fourteen taurine dipeptides (1-14) containing one of eleven neutral L-amino acids or three neutral D-amino acids were examined. These taurine peptides were synthesized by a conventional method using chemical coupling of taurine with an amino acid. Alternatively, the dipeptides (1-9) containing L-amino acid were also synthesized, with a few exceptions (10, 11), by a new method using a general substitution reaction of a sulfo group for chlorine or bromine via the β-halogenoethyl amide of each amino acid. When sodium sulfite or ammonium sulfite was used in the substitution, the new method gave pure taurine dipeptides in good yield without racemization. All the dipeptides (1-14), including naturally occurring Ser-Tau, showed high cross-reactivities with antisera against haptenic taurine or γGlu-Tau.抄録全体を表示PDF形式でダウンロード (1026K) -
伊藤 允好, 松岡 望, 月田 潔, 関 隆晴1988 年 36 巻 1 号 p. 78-86
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe geometrical isomers of (±)-3-hydroxyretinals were synthesized and characterized. Subsequently, simultaneous separation of eight isomers of 2- and 3-hydroxyretinals by high-performance liquid chromatography (HPLC) was accomplished and, in addition, complete separation of eight syn-anti isomers of 3-hydroxyretinaloximes by HPLC was achieved. Under these analytical conditions, the chromophore of the fly (Drosphila melanogaster) visual pigment was identified as 11-cis-3-hydroxyretinal (10).抄録全体を表示PDF形式でダウンロード (962K) -
西澤 信, 出原 留利子, 金子 光, 腰原 康子, 藤本 康雄1988 年 36 巻 1 号 p. 87-95
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーFive 5-lipoxygenase inhibitors, chlorogenic acid (1), 6''-p-coumaroyl genipin gentiobioside (2), 3, 4-di-O-caffeoylquinic acid (3), 3-O-caffeoyl-4-O-sinapoylquinic acid (4) and 3, 5-di-O-caffeoyl-4-O-(3-hydroxy-3-methyl)glutaroylquinic acid (5), were isolated from Gardeniae Fructus. The structures of the new compounds (2, 4 and 5) were elucidated on the basis of spectral data and chemical evidence. These hydroxycinnamic acid derivatives inhibit 5-lipoxygenase activity, and 3 was the most potent inhibitor. The inhibitory effects were enhanced on methylation of the carboxyl group(s) of 1, 3, 4 and 5, and the ID<50> values of the methyl esters of 3, 4 and 5 were of the order of 10<-8>M.抄録全体を表示PDF形式でダウンロード (910K) -
豊岡 康平, 久保田 晴寿1988 年 36 巻 1 号 p. 96-106
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーNovel 3, 5-disubstituted 4, 5-dihydro-1H-1, 2, 4-triazoles were synthesized by nucleophilic substitution of 1, 4-diacetyl-3-methylsulfonyl-4, 5-dihydro-1H-1, 2, 4-triazoles (15a-c), which were obtained by oxidation of 1, 4-diacetyl-3-methylthio-4, 5-dihydro-1H-1, 2, 4-triazoles (5a-c) with 2 mol eq of m-chloroperbenzoic acid. Acetylation of aldehyde or ketone S-methylisothiosemicarbazones (3a-c) with acetic anhydride at room temperature gave aldehyde or ketone 4-acetyl-3-methyl-isothiosemicarbazones (4a-c), which cyclized with acetic anhydride under heating to give 5a-c. Compounds 5a-c were also obtained by the reaction of 3a-c with acetic anhydride under heating.抄録全体を表示PDF形式でダウンロード (1085K) -
藤井 澄三, 斎藤 徹, 井上 勲, 熊澤 幸成, 田村 克巳1988 年 36 巻 1 号 p. 107-117
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーOn treatment with boiling 1 N aqueous NaOH for 2 h, 3, 7-dialkyladenine salts (7 : R1, R2=Me, Et, or PhCH2; X=Br, I, or ClO4) gave 1-alkyl-4-(N-alkylamino)-1H-imidazole-5-carboxamides (8), 1-alkyl-4-amino-1H-imidazole-5-carboxamides (11), and N6, 7-dialkyladenines (14) in 33-59%, 2-10%, and 2-5% yields, respectively. Under slightly miler reaction conditions, 3, 7-dimethyl-adenine hydriodide (7a : X=I) afforded 1-methyl-4-(N-methylamino)-1H-imidazole-5-carboxamide (8a) together with 3, 7-dimethylhypoxanthine (2a) as a by-product; 7-benzyl-3-methyladenine hydrobromide (7c : X=Br) furnished a small amount of 1-benzyl-4-(N-methylamino)-1H-imidazole-5-carboxamidine (5c) besides 1-benzyl-4-(N-methlamino)-1H-imidazole-5-carboxamide (8c), 1-benzyl-4-amino-1H-imidazole-5-carboxamide (11c), and 7-benzyl-N6-methyladenine (14c). These results are best interpreted in terms of pathways involving hydrolytic deamination, ring fission in the pyrimidide and imidazole moieties, cyclization, and Dimroth rearrangement. The instability of 7a (X=I) in aqueous alkali was compared with that of the four possible Nx, 9-dimethyl isomers, and the relative ease with which the adenine ring underwent hydrolytic ring fission was found to decrease in the order 3, 9- (17)>7, 9- (18)>1, 9- (19)>3, 7- (7a)»N6, 9-dimethyl isomer (20).抄録全体を表示PDF形式でダウンロード (1195K) -
川瀬 靖総, 岩井 成憲, 大塚 栄子1988 年 36 巻 1 号 p. 118-121
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーSelf-complementary hexanucleotides d(GGINCC) (N=C, A, G, T) were synthesized by the phosphotriester method. The circular dichroism (CD) spectra of these oligonucleotides showed that the oligonucleotides containing I : C or I : A pairs seem to possess a shape similar to deoxyribonucleic acid (DNA) with right-handed stacking.抄録全体を表示PDF形式でダウンロード (454K) -
野水 基義, 赤路 健一, 深田 順一, 井村 裕夫, 井上 敦子, 仲田 義啓, 瀬川 富朗, 藤井 信孝, 矢島 治明1988 年 36 巻 1 号 p. 122-133
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーA tetracontapeptide corresponding to the entire amino acid sequence of a frog skin peptide, sauvagine, was synthesized by assembling eight peptide fragments of established purity followed by deprotection with 1 M trimethylsilyl trifluoromethanesulfonate-thioanisole in trifluoroacetic acid. The synthetic peptide stimulated secretion of immunoreactive corticotropin from rat pituitary cells and its potency was estimated to be equivalent to that of synthetic ovine corticotropin releasing factor. Synthetic sauvagine displayed long-lasting hypotensive action in rats.抄録全体を表示PDF形式でダウンロード (1264K) -
木下 工, 宮田 昌明, / 藤本 善徳, 柿沼 勝己, 池川 信夫, 森崎 益雄, MASUO MORISAKI1988 年 36 巻 1 号 p. 134-141
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーFour diastereoisomers at the C-24 and C-25 positions of 3α, 7α, 12α, 24-tetrahydroxy-5β-cholestan-26-oic acid (varanic acid) were synthesized in a stereochemically defined manner and also by a non-stereoselective route, followed by chromatographic separation. Their stereochemistry at the C-24 and C-25 positions was established on the basis of the known stereochemical course of the reactions employed for the synthesis, and 1H and 13C-nuclear magnetic resonance spectroscopic data of these isomers. It is concluded from the present work that the previous stereochemical assignment for the (24R, 25S) and (24R, 25R) isomers must be revised.抄録全体を表示PDF形式でダウンロード (795K) -
藤本 善徳, 木下 工, 大谷 いずみ, 柿沼 勝己, 池川 信夫, 園田 よし子, 佐藤 良博, 森崎 益雄1988 年 36 巻 1 号 p. 142-145
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe four diastereoisomers at the C-24 and C-25 positions of the title compound (varanic acid) were incubated with rat liver mitochondrial fraction supplemented with adenosine triphosphate, coenzyme A, nicotinamide adenine dinucleotide, and MgCl2. All of these isomers were converted into cholic acid. Thus, the stereochemical configuration at the C-24 and C-25 positions has no significant effect on the efficiency of side chain cleavage of the tetrahydroxy acid into cholic acid.抄録全体を表示PDF形式でダウンロード (465K) -
小山 清隆, 名取 信策1988 年 36 巻 1 号 p. 146-152
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーSeven new bis(naphtho-γ-pyrone) derivatives, named ustilaginoidins D (8), E (9), F (10), G (11), H (12), I (13), and J (14), were isolated in addition to ustilaginoidins A (1), B (2), and C (3) from Claviceps virens. Their structures were elucidated chiefly on the basis of nuclear magnetic resonance data.抄録全体を表示PDF形式でダウンロード (709K) -
北川 勲, 王 恵康, 谷山 登志男, 吉川 雅之1988 年 36 巻 1 号 p. 153-161
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーA full account of the structure revision of soyasapogenols is presented. The structures of soyasapogenols A, B, and E have been confirmed to be expressed as 3β, 21β, 22β, 24-tetrahydroxy-olean-12-ene (1), 3β, β22β, 24-trihydroxyolean-12-ene (2), and 3β, 24-dihydroxyolean-12-en-22-one (5), respectively, rather than the previously reported 3β, 21α, 22α, 24-tetrahydroxyolean-12-ene (1'), 3β, 21α, 24-trihydroxyolean-12-ene (2'), and 3β, 24-dihydroxyolean-12-en-21-one (5'). In consequence, the structures of soyasaponins I, II, and III are formulated as 3-O-[α-Lrhamnopyranosyl(1→2)-β-D-galactopyranosyl(1→2)-β-D-glucuronopyranosyl]soyasapogenol B (8), 3-O-[α-L-rhamnopyranosyl(1→2)-α-L-arabinopyranosyl(1→2)-β-D-glucuronopyranosyl]soyasapogenol B (9), and 3-O-[β-D-galactopyranosyl(1→2)-β-D-glucuronopyranosyl]soyasapogenol B (10), respectively.抄録全体を表示PDF形式でダウンロード (999K) -
吉村 祐一, 佐野 友春, 松田 彰, 上田 亨1988 年 36 巻 1 号 p. 162-167
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーCondensation of 5-O-tert-butyldimethylsilyl-1, 2-O-isopropylidene-α-D-erythro-3-pentulo-furanose (4) with 2, 4-dimethoxypyrimidin-6-ylmethyllithium (5) afforded a 3-pyrimidinylmethyl-ribose derivative (6). The protecting groups of 6 were changed to give the 5-O-benzoyl-1, 2-di-O-acetyl derivative (8). The intramolecular glycosylation of 8 by treatment with stannic chloride furnished the 6, 3'-methanol-O4-methyluridine derivative (9), which was further converted to 6, 3'-methanouridine (10) and 6, 3'-methanocytidine (11). The 2'-deoxygenation of 9 by way of the 2'-imidazolylthiocarbonyl dericative gave, after appropriate derivatization, 2'-deoxy-6, 3'-methanocytidine (16) and -uridine (17).抄録全体を表示PDF形式でダウンロード (768K) -
山中 宏, 新妻 節子, 酒井 正美, 坂本 尚夫1988 年 36 巻 1 号 p. 168-171
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーTreatment of 4-alkoxy-6-methylpyrimidine 1-oxides with acetic anhydride followed by reaction with diketene gave 7-acetyl-4-alkoxy-2-methylisoxazolo[4, 5-c]pyridines and 7-acetyl-4-alkoxy-3-methyloxazolo[4, 5-c]pyridines, respectively. The structure elucidation of these compounds on the basis of spectral data and chemical reactions, and the reaction pathway of the ring transformation are described.抄録全体を表示PDF形式でダウンロード (550K) -
末宗 洋, 小田 晃造, 佐伯 清太郎, 酒井 浄1988 年 36 巻 1 号 p. 172-177
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThis paper describes the conversions of (-)-limonene to four nepetalactones (1, 2, ent-3 and 4) in a stereocontrolled manner. The cis-3, 4-disubstituted cyclopentanone (5) obtained from (-)-limonene via Rh(I)-catalyzed cyclization of the 4-pentenal, could be converted to the bicyclo[3.3.0]octenone (6). After the stereoselective conversion of 6 into the diastereomeric isomers of the ketones (8 and 16), a sequence of reactions involving the silyl enol ethers (18 and 19), ozonolysis, and subsequent lactonization afforded the target molecules.抄録全体を表示PDF形式でダウンロード (757K) -
岡本 加世子, 渡辺 正純, 森本 浩, 今田 伊助1988 年 36 巻 1 号 p. 178-189
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーDemethyl dirivatives (3a and 3b) of 6(10-hydroxydecyl)-2, 3-dimethoxy-5-methyl-1, 4-benzoquinone (1, CV-2619), demethyl derivative (4) of the metabolite 2-4, and compounds (13, 20, 21, 23a and 23b) in which the hydroxyalkyl chain of 1 is modified, were synthesized for metabolic studies and evaluation of their biological activities. In rats, 13 and trans-23a were metabolized more slowly than 1. These compounds, except for the demethyl derivatives (3a, 3b and 4), showed an electron tansfer effect comparable to that of 1 in the succinate oxidation system. Compounds 13 and 23b inhibited the lipid peroxidation of rat liver homogenate.抄録全体を表示PDF形式でダウンロード (1120K) -
前田 ひろし, 鈴木 護, 菅野 紘, 山村 道夫, 石田 柳一1988 年 36 巻 1 号 p. 190-201
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーIn order to find compounds having selective central nervous system (CNS) actions, various thyrotropin-releasing hormone (TRH) analogs in which the pyroglutamic acid residue is replaced by (3S)-1-oxo-1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylic acid (Otc-OH) and related derivatives were prepared and their CNS actions were investigated in mice.Otc-His-Pro-NH2 (9a) showed 3.5-10 times stronger CNS actions than TRH (1). However, it was also 3-4 times more potent than TRH in thyrotropin (TSH)-releasing activity.抄録全体を表示PDF形式でダウンロード (1189K) -
中本 信一, 阿知波 一雄1988 年 36 巻 1 号 p. 202-208
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーSynthesis of biologically active 3-deoxy-D-manno-2-octulosonic acid (KDO)-(α2→6)-D-glucosamine-4-phosphate analogs of lipid A is described.抄録全体を表示PDF形式でダウンロード (847K) -
周東 智, 伊東 裕通, 植田 成, 今村 茂行, 福川 清史, 辻野 正俊, 松田 彰, 上田 亨1988 年 36 巻 1 号 p. 209-217
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーPhospholipase D from Streptomyces effectively catalyzed the transfer reaction of the phosphatidyl residue from 3-sn-phosphatidylcholine to the 5'-hydroxyl group of nuclesides in a two-phase system. Thus, a variety of 5'-(3-sn-phosphatidyl)nucleosides could be readily prepared in high yields by means of this reaction. Among them, phosphatidyl-FUR (3b), phosphatidyl-Ara FC (8b), and phoshatidyl-neplanocin A (12b) each produced a significant increase in the life span mice bearing i.p.-implanted P388 leukemia, being more effective than the parent nucleosides.抄録全体を表示PDF形式でダウンロード (928K) -
池田 昇司, 坂本 文夫, 平山 良一, 武部 靖, 外村 幹夫, 塚本 悟郎1988 年 36 巻 1 号 p. 218-226
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーSeveral (5-methyl-2-oxo-1, 3-dioxol-4-yl)methyl esters of β-lactamase inhibitors were prepared and evaluated for oral absorbability. Sulbactam (5-methyl-2-oxo-1, 3-dioxol-4-yl)methyl ester (5a) was found to prodece a 5-fold higher serum level of sulbactam than sulbactam itself after oral administration to mice. The diester (15), in which ampicilling is bonded to the 5-methyl group of the above sulbactam ester (5a), was also prepared, but this diester (15) did not produce high serum levels of ampicillin and sulbactam after oral administration to mice.抄録全体を表示PDF形式でダウンロード (952K) -
千坂 武司, 松田 久司, 窪村 安司, 望月 道彦, 山原 絛二, 藤村 一1988 年 36 巻 1 号 p. 227-233
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe mechanism of the anti-hypercholesteremic effect of (-)-epigallocatechin gallate (EGCG), a component of green tea, was explored in rats from the viewpoint of cholesterol metabolism.1) The in vitro incorporation of 14C-acetate into cholesterol was not affected by the presence of EGCG in liver slices from normal rats or by oral pretreatment of the animals with EGCG in liver slices from normal and Triton-induced hypercholesteremic rats.2) The kinetics of serum levels of 14C-cholesterol given orally and of 3H-cholesterol given intravenously revealed that EGCG, when orally administered, suppressed the absorption of 14C-cholesterol from the digestive tract and had an enhancing effect on elimination of serum 3H-cholesterol at higher doses.3) In situ uptake in the intestine of 14C-choresterol given in the lumen was suppressed by the presence of EGCG.In conclusion, these results indicated that the anti-hypercholesteremic effect EGCG in rats is mainly due to suppression of the absorption of exogenous cholesterol from the digestive tract, and partly due to the enhancement of the elimination of endogenous cholesterol.抄録全体を表示PDF形式でダウンロード (691K) -
笠井 良次, 松本 一浩, 〓 瑞麟, 周 俊, 田中 治1988 年 36 巻 1 号 p. 234-243
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーFrom rhizomes of Hemsleya panacis-scandens collected in Yunnan, China, eight new cucurbitane glycosides named scandenosides R1-R7 and dihydrocucurbitacin F glucoside (2-O-β-D-glucopyranoside of 23, 24-dihydrocucurbitacin F) were isolated, along with six known cucurbitane glycosides. The structures of these new glycosides were determined on the basis of chemical and spectral data except for the configuration at C-20. Of these new glycosides, scandenoside R6 tastes sweet and R5 and dihydrocucurbitacin F glucoside taste bitter, while the others are tasteless. The structure-taste relationships of cucurbitane glycosides are discussed.抄録全体を表示PDF形式でダウンロード (950K) -
野呂 忠敬, 関谷 猛, 加藤(旧姓阿部) 正子, 小田 康司, 宮瀬 敏男, 黒柳 正典, 上野 明, 福島 清吾1988 年 36 巻 1 号 p. 244-248
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーXanthine oxidase (XO) inhibitors were isolated from the rhizomes of Alpinia galanga (Zingiberaceae), and were identified as trans-p-coumaryl diacetate (1), trans-coniferyl diacetate (2), [1'S]-1'-acetoxychavicol acetate (3), [1'S]-1'-acetoxyeugenol acetate (4) and 4-hydroxybenzaldehyde (5). The type of inhibition by either 1 or 3 with respect to xanthine as a substrate was uncompetitive.抄録全体を表示PDF形式でダウンロード (518K) -
梨田(旧姓伊藤) 智子, 白石 隆幸, 宇田 裕1988 年 36 巻 1 号 p. 249-253
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーA simple method for the determination of cyanogenic glycosides by using a Conway's microdiffusional apparatus was investigated. The hydrolysis of cyanogenic glycosides by enzymes and the isolation of cyanide liberated were simultaneously performed in the same apparatus. The liberated hydrogen cyanide was determined by Epstein's method using pyridine-pyrazolon reagent. By this method, the recoveries of linamarin and amygdalin were over 90% and the coefficients of variation were 0.2 to 3.6% for both glycosides in the range of 0.5-400 μg of cyanide. This method was applied to the determination of cyanogenic glycosides in pastes of butter beans and apricot kernels and the results were compared with those obtained by the steam distillation method.抄録全体を表示PDF形式でダウンロード (531K) -
藤田 芳一, 森 逸男, 藤田 絹子, 中橋 義弘1988 年 36 巻 1 号 p. 254-262
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーAn attempt was made to apply saponin to analytical spectrophotomethy; color reactions between o-hydroxyhedroquinonephthalein (Qnph) and several metal ions in the presence of surfactants including saponin were studied in weakly basic media. A simple, sensitive and selective spectrophotometric determination of iron ion (iron<III>+iron<II>) was developed with Qnph and saponin. The apparent molar absorptivity for iron ion was 1.18×105 1 mol<-1>cm<-1> at 565 nm. It was suggested that saponin is a surfactant having complex-forming ability with metal ions, and iron ion combined with hydrophilic sugar groups in the saponin. The proposed method was applied to the assay of iron ion in rain water, tap water, human urine and calf serum, and the analytical results were in good agreement with those obtained by atomic absorption spectrometry, inductively coupled plasma atomic emission spectroscopy and spectrophotometry with bathophenanthroline.抄録全体を表示PDF形式でダウンロード (910K) -
金木 弘之, 中内 瑞夫, 田中 光也1988 年 36 巻 1 号 p. 263-273
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe interation of Rhizopus delemar C-lipase with 1, 1, 1-trichloro-2, 2-bis(4-chlorophenyl)ethane (DDT) and structurally related pesticides was studied. Binding assays and titration experiments revealed that the binding is distinctly cooperative and the 1 : 1 pesticide-lipase complex formation governs the ensuing complex formation. The chlorinated pesticides used here fall into three groups according to the mode of interaction with lipase. (1) DDT, 1, 1-dichloro-2, 2-bis(4-chlorophenyl)ethane (DDD) and 1, 1-dichloro-2, 2-bis(4-chlorophenyl)ethylene (DDE), the 1 : 1 pesticide-lipase complexes of which bind 8 further molecules of any pesticide used here to form 9 : 1 complexes with much higher activity. (2) Dimic and dichlorobenzophenone, the 1 : 1 pesticide-lipase complexes of which can bind 8 further molecules of the same pesticide without activation, but cannot bind any other pesticide. (3) Kelthane, chlorobenzilate and chloropropylate, which are non-competitive inhibitors of the intact lipase but behave as activators for 1 : 1 pesticide-lipase complexes of pesticides in group (1).The formation of the very tightly bound 9 : 1 DDT-lipase complex at pH 4.5 Chromatography on CM-Sephadex C25 gave results supporting the one-step formation of a 9 : 1 DDT-lipase complex from a 2 : 1 DDT-lipase complex.抄録全体を表示PDF形式でダウンロード (1044K) -
鄭 海泳, 横澤 隆子, 大浦 彦吉1988 年 36 巻 1 号 p. 274-278
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe acute effect of Salviae miltiorrhizae Radix extract on renal function was investigated in rats with renal failure induced by an adenine diet. Glomerular filtration rate (GFR), renal plasma flow (RPF), and renal blood flow (RBF) progressively decreased as renal impairment increased due to extended administration of adenine. Treatment with the extract significantly increased GFR by 50% in renal failure rats on the 12th d of adenine administration. The RPF in the extract-treated group also increased by 40% as compared with the control group. Similarly, Salviae miltiorrhizae Radix extract significantly increased RBF by 37%. However, the extract was ineffective in rats having renal failure with severe renal impairment, on the 24th d of adenine administration. On the other hand, the urinary excretions of urea and creatinine increased significantly by 27% and 19%, respectively, on the 12th d. These data suggest that Salviae miltiorrhizae Radix is an effective herb for the treatment of mild renal failure.抄録全体を表示PDF形式でダウンロード (616K) -
石光 進, 藤本 貞毅, 小原 晃1988 年 36 巻 1 号 p. 279-285
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーIncubation of L-phenylalanine with the soluble fractions of liver and adrenal in the presence of a pterine cofactor, 2-mercaptoethanol and catalase gave rise to a hydroxylated compound which was identified as 3, 4-dihydroxyphenylalanine (DOPA), as well as p-, m- and o-tyrosines, on the basis of reversed-phase high-performance liquid chromatography (HPLC) with fluorescence detection. Chromatographic peaks were identified on the basis of their retention behavior and the assignment of the DOPA peak of HPLC was verified by ion-exchange chromatographic analysis.The formation of DOPA from L-phenylalanine by purified phenylalanine hydroxylase [EC 1.14.16.1] and tyrosine hydroxylase [EC 1.14.16.2] from rat liver and adrenal, respectively, was observed. The hydroxylation of L-phenylalanine to m- and o-tyrosines was also found to be catalyzed by the purified phenylalanine and tyrosine hydroxylases. In addition, the hydroxylation of L-p-tyrosine to DOPA was caused by the purified phenylalanine hydroxylase.抄録全体を表示PDF形式でダウンロード (724K) -
山口 正義1988 年 36 巻 1 号 p. 286-290
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe physicochemical properties of a calcium-binding protein (CaBP) isolated from rat liver cytosol was investigated. Isoelectric focusing in a polyacrylamide gel plate using the Broad pI Calibration Kit showed that the isoelectric point is 5.20. The ultraviolet (UV) absorption spectrum of CaBP showed a maximum at 278 nm. The conformational changes induced by Ca<2+>-binding to CaBP were examined by measuring the UV difference, fluorescence emission, and circular dichroism (CD) spectra. These spectra were altered by titration of CaBP with 1.0 mM Ca<2+>. The alterations could be attributed to an increased exposure of tyrosine and tryptophan residues to a more aqueous environment, resulting in an increased hydrophobicity of CaBP. From the CD spectrum, the apparent α-helical content of CaBP in Ca<2+>-free buffer was estimated to be 34%. This value was decreased by 1.0 mM Ca<2+> addition. The results suggest that Ca<2+>-binding induces conformational changes of CaBP, and that the protein contains distinct and specific ligand-binding sites for Ca<2+>.抄録全体を表示PDF形式でダウンロード (618K) -
池原 森男, 藤本 和子, 松尾 徳幸, 玉造 滋, 吉田 毅治, 上村 春樹, 西川 諭, 上杉 晴一, 大塚 栄子1988 年 36 巻 1 号 p. 291-296
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーA gene for human tumor necrosis factor has been synthesized by joining 60 oligodeoxyribonucleotides of 13 to 20 residues using deoxyribonucleic acid (DNA) ligase. These oligodeoxyribonucleotides were prepared by the solid-phase phosphotriester method. The gene (483 base pairs) was designed to carry a Cla I site plus a start codon at the N-terminal end and stop codons plus a Sal I site at the C-terminal end. The gene was expressed in Escherichia coli under the control of the tryptophan promoter of E. coli, and the expressed product was purified and tested for cytotoxic activity.抄録全体を表示PDF形式でダウンロード (631K) -
武藤 里志, 荻野 秀敏, 五十嵐 かおる, 松本 優子, 由岐 英剛1988 年 36 巻 1 号 p. 297-304
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe effect of incubation time with lymphokines on macrophage activities was studied by use of the phorbol myristate acetate-induced luminol-dependent chemiluminescence method and cytotoxicity test. When thioglycollate-elicited ICR mouse peritoneal macrophages were incubated with lymphokines, their ability to generate chemiluminescence increased biphasically during incubation. That is, within one day, it reached a maximal level at about 4 h (early response), and then progressively decreased to the control level. However, when the incubation time was further prolonged, it began to increase again, and reached about 2-fold the control level after 3 d (late response). The increase in the chemiluminescence of lymphokine-treated macrophages with increasing incubation time is not due to the increase in the macrophage cell numbers. In contrast to the clear biphasic increase in chemiluminescence, there was no clear biphasic increase in cytotoxicity in lymphokine-treated macrophages. The activities in the lymphokine supernatants to induce the early and the late chemiluminescent response in macrophages disappeared together with the activity to induce cytotoxicity, on dialysis at pH 2 for 24 h or on heating at 80°C for 30 min, but not at 56°C for 30 min. Although the lymphokines increasing macrophage chemiluminescence were separated into two fractions in Sephadex G-100 gel filtration, each fraction had both activities to induce the early and the late chemiluminescent response, and the major fraction largely corresponded to that of the activity to induce cytotoxicity. These results suggested that there is a lymphokine which alters macrophage chemiluminescence biphasically by itself, and it may be interferon-γ.抄録全体を表示PDF形式でダウンロード (899K) -
久保 欣也, 渡辺 隆史, 須賀 哲弥1988 年 36 巻 1 号 p. 305-311
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーMany studies on eicosapentaenoic acid (EPA) have confirmed its metabolic transformation to prostaglandins (PGs). However, it is not yet clear whether or not a large part of the EPA contained in foods is metabolized and degraded through some pathway other than transformation to PGs. The purpose of this study was to clarify whether the peroxisomal β-oxidation system participates in the chain-shortening of EPA.EPA-CoA in a reaction mixture for β-oxidation assay was incubated with liver peroxisomes obtained by sucrose density gradient centrifugation and the reaction products were analyzed by gas liquid chromatography. Metabolites having chain lengths reduced by 2 and 4 carbon units from EPA were detected. Furthermore, in order to examine the contribution of the peroxisomal and mitochondrial β-oxidation systems, the activities of purified fatty acyl-CoA oxidase and fatty acyl-CoA dehydrogenase toward EPA were determined and extrapolated to obtain the activities in the rat liver. The activities in the normal rat were 139 U/g liver for peroxisomal β-oxidation and 549 U/g liver for in mitochondrial β-oxidation. On treatment with diethylhexyphthalate (DEHP), a peroxisomal proliferator, the activities in the two organelles were induced to similar extents.From these findings it is concluded that hepatic peroxisomes participate in the chain-shortening of EPA together with mitochondria.抄録全体を表示PDF形式でダウンロード (680K) -
渡辺 護, 竹部 幸子, 金 東鉱, 荒川 良, 上村 清, 小橋 恭一1988 年 36 巻 1 号 p. 312-315
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーA highly resistant strain of Culex tritaeniorhynchus was employed to clarify the mechanisms of the acquired resistance of mosquitoes to organophosphorus and carbamate insecticides by an enzymological approach. Carboxylesterase (CE) activity was higher in the abdomen than in the head and thorax, and was higher in every part of the body of the resistant strain as compared with the susceptible strain. Acetylcholinesterase (AChE) activity was high in the head, and was higher in every part of the body in the susceptible strain as compared with the resistant strain.Greater inhibition of CE by oxo-type organophosphorus insecticides was observed in the susceptible strain (11-, 8.2- and 22.3-fold greater inhibitions by fenitrooxon, malaoxon and dichlorvos, respectively) than in the resistant strain. Much stronger inhibition of AChE was observed in the susceptible strain (1227-, 76.5- and 183-fold inhibitions by fenitrooxon, malaoxon and dichlorvos, respectively) than in the resistant strain. These results suggest that both AChE and CE are involved in the development of the acquired resistance to organophosphorus and carbamate insecticides, and that the former enzyme plays the major role.抄録全体を表示PDF形式でダウンロード (486K) -
横澤 隆子, 鄭 海泳, 大浦 彦吉, 野中 源一郎, 西岡 五夫1988 年 36 巻 1 号 p. 316-320
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーAn attempt was made to isolate the active component which exhibits the improving effect on uremic symptoms from Salviae miltiorrhizae Radix. Systematic isolation from the aqueous extract of Salviae miltiorrhizae Radix was carried out and the effects of the fractions were assessed in terms of an index of decrease in blood urea nitrogen. It was found that one of the major blood urea nitrogen-decreasing components was compound I. Compound I, which was considered to be a tetramer of (dihydro) caffeic acid, showed improving effects on uremic symptoms, causing significant decreases in blood urea nitrogen, creatinine, methylguanidine, and guanidinosuccinic acid.抄録全体を表示PDF形式でダウンロード (554K) -
山口 正義, 森 聖一1988 年 36 巻 1 号 p. 321-325
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe effects of Ca<2+> and Zn<2+> on 5'-nucleotidase activity in rat liver plasma membranses were investigated. Addition of Ca<2+> (1.0-100 μM) caused a significant decrease of the enzyme activity. The decrease of 5'-nucleotidase activity induced by Ca<2+> (25μM) was completely restored by the presence of a calcium-binding protein (CaBP 5.0 μM). Of the various metals tested, 5'-nucleotidase activity was significantly decreased by the presence of Zn<2+> and Cd<2+>, while Cu<2+>, Co<2+>, Ni<2+> and Mn<2+> did not inhibit the enzyme. In particular, the effect of Zn<2+> was remarkable (decrease of about 60%). A significant decrease of the enzyme activity was also seen at 5.0 μM Zn<2+>, but not at 1.0 μM Zn<2+>. The inhibitory effect of 25μM Zn<2+> on 5'-nucleotidase was not appreciably blocked by the presence of CaBP (2.5 and 5.0 μM). The present data suggest that CaBP uniquely regulates the Ca<2+> effect on 5'-nucleotidase activity in the hepatic plasma membranes. It is proposed that CaBP, which may regulate the Ca<2+> effect on liver cell function, should be called regucalcin.抄録全体を表示PDF形式でダウンロード (624K) -
釜野 徳明, 佐藤 統夫, 仲吉 洋, / , CECIL R. SMITH1988 年 36 巻 1 号 p. 326-332
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーAn evaluation of thirty-four bufadienolides and two related cardenolides against a series of rhinoviruses in vitro has been completed. Most of the bufadienolides were found to display some inhibitory activity. Scillarenin and 3-O-[N-(tert-butoxycarbonyl)hydrazido]succinylbufalin were found to be the most active with chemotherapeutic indices of 32 and 16, respectively. In general, the 14β-hydroxy-bufadienolides showed the strongest antiviral activity, and were found more toxic than the corresponding 14β, 15β-epoxy-bufadienolides. Introduction of a 16β-hydroxy or 16β-acetoxy substituent into the 14β, 15β-epoxybufadienolides enhanced their antiviral activity. Substituents at the 3β-, 5β-, and 19-positions appeared to affect only the level of toxicity.抄録全体を表示PDF形式でダウンロード (698K) -
久保田 美穂, 中野 眞汎, 従二 和彦1988 年 36 巻 1 号 p. 333-337
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーPoly-β-hydroxybutyric acid (PHB) microspheres containing aclarubicin hydrochloride were prepared by a solvent-evaporation process. The release rates of the drug from the microspheres were significantly increased by incorporating ethyl or n-butyl esters of fatty acids. In order to clarify the effects of fatty acid esters on drug release, the powder X-ray diffraction patterns of microspheres, contents of fatty acid esters in microspheres and other factors were investigated. Powder X-ray diffraction, scanning electron microscopy and differential scanning calorimetry indicated no significant differences due to incorporation of the esters in the microspheres. The contents of fatty acid esters in the microspheres and the solubility of aclarubicin hydrochloride in the fatty acid esters greatly affected the release rate of the drug from the microspheres.抄録全体を表示PDF形式でダウンロード (695K) -
森 貴好, 西村 憲一, 田巻 聡, 中村 正平, 津田 浩一, 掛谷 宣治1988 年 36 巻 1 号 p. 338-344
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーBifunctional pro-drugs of disodium cromoglycate (DSCG), incorporating both lipophilic and hydrophilic pro-moieties, were desined to improve the oral absorption of DSCG, an antiallergic agent used clinically. The synthesized pro-drugs were found to prossess the desired properties for an orally active pro-drug. Among the pro-drugs tested, KY-556 (carrying twin ethyl pro-moieties and an L-lysyl pro-moiety) was particularly well absorbed orally and, as expected, displayed good antiallergic activity in the rat passive cutaneous anaphylaxis test.抄録全体を表示PDF形式でダウンロード (688K) -
藤原 洋, 河島 進, 山田 豊, 中井 正彦1988 年 36 巻 1 号 p. 345-353
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーIn this study, the stability of bacampicillin hydrochloride (BAPC) suspension was measured to clarify the kinetics in a consentrated solution. Then, the time courses BAPC in suspension were examined in the neutral pH region and at 35°C. In this suspension, not only total BAPC, but also the dissolved BAPC were decreased with time. This result indicates that particles of BAPC precipitate from the solution with time, and the infrared (IR) spectrum of the precipitates suggested that they consisted of BAPC base. Furthermore, the degradation of BAPC in suspension was very much faster than that in solution. This acceleration of the degradation was due to the simultaneous degradation of the precipitated and the dissloved BAPC. In addition, the apparent first-order degradation rate constant of the precipitated particles was larger than that of the dissolved BAPC. Thus, the degradation of the solid seems to be accelerated by hydroxyl ion.抄録全体を表示PDF形式でダウンロード (843K) -
今井 輝子, 小田切 優樹, 斉藤 肇, 上釜 兼人1988 年 36 巻 1 号 p. 354-359
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThe inclusion behavior of flurbiprofen (FP) with heptakis(2, 3, 6-tri-O-methyl)-β-cyclodextrin (TM-β-CyD) in solution and in the solid state was compared with that of FP with β-cyclodextrin (β-CyD) by microcalorimetry and solid-state nuclear magnetic resonance (NMR) measurements. Furthermore, solid somplexes of FP with β-CyD and TM-β-CyD were obtained in the molar ratio of 1 : 1, and their dissolution behavior, permeation through a silicone membrane and in vivo absorption behavior were examined, in comparison with those of FP alone. The data suggest that the inclusion behavior of FP with TM-β-CyD is somewhat different from that with β-CyD. The apparent rates dissolution, permeation and the bioavailability of FP were significantly increased by the inclusion complex formation. However, no differences between the pharmacokinetic parameters were found for the two complexes. It is concluded that the enhanced bioavailability of FP after oral administration may be due to the fast dissolution of the complexes.抄録全体を表示PDF形式でダウンロード (669K) -
土橋 洋史, 長友 孝文1988 年 36 巻 1 号 p. 360-366
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーThis experiment was designed to examine the effects of choline and inositol in Eagle's minimal essential medium (MEM), because the values of specific binding were increased when the 3H-dihydroalprenolol (3H-DHA) binding assay of β-adrenoceptors in the guinea pig and rat cerebral cortical membranes was carried out in Eagle's MEM instead of 60 mM Tris-HCl, 20 mM MgCl2 buffer (pH 7.4). All chemicals contained in the MEM were added to the 3H-DHA binding mixture and the values of the specific binding were compared with the control values obtained in the absence of the chemicals. The presence of choline (0.1-10 μM) or inositol (0.1-10 μM) induced an increase of the values of the specific binding. These effects of choline and inositol were observed after preinclubation for 20 and 1 min, respectively. After 30 min of incubation, no changes were observed upon removal of these chemicals. Furthermore, choline and inositol significantly increased the β-adrenoceptor density (β<max>) when 3H-DHA and <125>I-iodocyanopindolol were used as the radioligands, as determined by Scatchard analysis, but no significant change was observed in the value of the dissociation constant (Kd) in 3H-DHA binding. These results suggest that choline and inositol in the membranes could have a crucial role in drug-receptor interaction.抄録全体を表示PDF形式でダウンロード (724K) -
見谷 一也, 吉田 敏彦, 森川 宏二, 岩永 裕氏, 越中 栄一, 加藤 日出男, 伊藤 安夫1988 年 36 巻 1 号 p. 367-372
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーNovel α-isopropyl-α-[(phenoxyalkylamino)alkyl]benzeneacetonitrile derivatives, the phenoxyalkylamino moiety of which was introduced in place of the phenethylamino moiety of verapamil (known to be an excellent Ca2+-antagonist), were synthesized and their pharmacological activities were evaluated. These compounds exhibited α-bloking activity along with Ca2+-antagonistic activity, and their activities were influenced by the substituent on the amino nitrogen atom and by the number of carbons between the nitrogen atom and the benzeneacetonitrile moiety (m) as well as that between it and the pheoxy moiety (n). Among these compounds, the N-methyl derivative (2h) where m=n=3, was found to possess a high Ca2+-antagonistic activity and the N-H derivative (2c) in which m=3 and n=2 possessed a high α-blocking activity.抄録全体を表示PDF形式でダウンロード (641K) -
見谷 一也, 吉田 敏彦, 桜井 俊一郎, 森川 宏二, 岩永 裕氏, 越中 栄一, 加藤 日出男, 伊藤 安夫1988 年 36 巻 1 号 p. 373-385
発行日: 1988/01/25
公開日: 2008/03/31
ジャーナル フリーα-Alkyl-α-[(phenoxypropylamino)propyl]benzeneacetonitrile derivatives containing various substituents on the ring of the benzeneacetonitrile moiety (A), the quaternary carbon atom and the ring of the phenoxy moiety (B) were prepared, and their Ca2+-antagonistic activities were evaluated. Among these compounds, the N-Me derivatives with a 3, 4, 5-(OMe)3 group on the A ring, an iso-Pr group on the quaternary carbon atom, and a m-OMe, 3, 5-(OMe)2, 3, 5-Me2 or 3, 4, 5-(OMe)3 group on the B ring were found to possess Ca2+-antagonistic activity higher than pA2=9. The effects of substitutions at the A ring, the quaternary carbon atom and the B ring are discussed.抄録全体を表示PDF形式でダウンロード (1051K)