著者

毛利 公則 竹本 常松 近藤 嘉和

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.102, no.3, pp.p310-312, 1982-03

被引用文献数

2

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Two new C-methyl flavanones, named matteucin (III) and methoxymatteucin (IV) were isolated from the root of Matteuccia orientalis TREV. (Aspidiaceae), together with the known desmethoxymatteucinol (I) and matteucinol (II). The structures of these flavanones were determined to be (2S)-5,7,2'-trihydroxy-6,8-dimethylflavanone and (2S)-5,7,2'-trihydroxy-5'-methoxy-6,8-dimethylflavanone, respectively, by spectroscopic evidence.

著者

伊藤 豊 矢野 真吾 渡辺 和夫 山中 悦二 相見 則郎 坂井 進一郎

出版者

公益社団法人日本薬学会

雑誌

Chem Pharm Bull (Tokyo) (ISSN:00092363)

巻号頁・発行日

vol.38, pp.1702-1706, 1990

被引用文献数

2

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We investigated the selectivities and structure requirements for alpha-1 and alpha-2 adrenoceptor blocking activities of yohimbine (YO) and its 12 related analogs, such as β-yohimbine (β-YO), dihydrocorynantheine (DHC) and (-)indoloquinolizidine ((-)IQ). The affinity of YO analogs to alpha-adrenoceptor was assessed by measuring their blockade of pressor responses to epinephrine in pithed rats. Among YO structure groups, the potency order was YO>DHC=β-YO>geissoschizine methylether>14β-hydroxy YO>14β-benzoyloxy YO (inactive). (-)IQ was slightly less potent than YO, but much stronger than (+)IQ. Among (±)IQ structure groups, the potency order was (±)IQ>(±)1,12b-trans-1-hydroxy IQ≫(±)1,12b-cis-1-hydroxy IQ (imactive). (±)Borrerine was active, but (±)desmethylborrerine was inactive. The alpha-1 blocking activities of the four compounds YO, β-YO, DHC and (-)IQ, were assessed in experiments of pressor responses to methoxamine in pithed rats and contractile responses to methoxamine in the rat vas deferens. The potency order was (-)IQ>YO>DHC>β-YO. Furthermore, the alpha-2 blocking activities of the four analogs were assessed in experiments of pressor responses to clonidine and inhibition of electrically driven cardioacceleration by clonidine, in pithed rats. The potency order was YO>β-YO>(-)IQ>DHC. Based on the potency ratio between alpha-1 and alpha-2 blocking activities, DHC or YO was most selective for alpha-1 or alpha-2 subtype, respectively, among the four YO analogs. These results suggest that the A, B, C and D rings of YO analogs and their planarity are necessary for the affinity to alpha-adrenoceptors and that the predominant conformation of the carboxymethyl or hydroxy group on the E ring of YO structure determines the selectivity for alpha-1 and alpha-2 blocking activities.

著者

KITAZATO KENJI TAKEDA SETSUO UNEMI NORIO

出版者

公益社団法人日本薬学会

雑誌

Journal of pharmacobio-dynamics (ISSN:0386846X)

巻号頁・発行日

vol.5, no.10, pp.803-810, 1982-10

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1,3,3,5,5-Pentaziridino-1-thia-2,4,6-traiza-3,5-diphosphorine-1-oxide (SOAz), a new antitumor agent, was evaluated for antitumor activity against various mouse- and rattumor systems. The optimal treatment regimens of SOAz (i.p.) gave 262% and 134% increase in life span (ILS) in mice P338 leukemia and L1210 leukemia implanted intraperitoneally, respectively, and 239% ILS in rats with Yoshida sarcoma of which 86% survived for 60 d after intraperitoneal tumor implantation. The compound showed a definite activity against Lewis lung carcinoma implanted intravenously. The compound also exhibited 80-100% inhibition of tumor local growth in all of four experimental tumor systems used in the present study. In contrast to cyclophosphamide, SOAz was active against B16 melanoma and Meth A, and demonstrated high activity against a subline of L1210 leukemia resistant to cyclophosphamide.

著者

藤井 節郎 奥田 拓道 赤沢 明 安田 行寛 川口 安郎 福永 育史 西川 栄郎

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.95, no.6, pp.732-740, 1975

被引用文献数

5

---

In order to investigate the fate of 1-(2-tetrahydrofuryl)-5-fluorouracil (FT-207) in comparison with that of 5-fluorouracil tritiated FT-207 (<SUP>3</SUP>H-FT-207) and 5-fluovouracil (<SUP>3</SUP>H-5-fluorouracil)were administered from the rectum in normal and AH-130 tumor-bearing rats, and rapid absorption of <SUP>3</SUP>H-FT-207 or <SUP>3</SUP>H-5-fluorouracil, was observed. Blood level of radioactivity after rectal administration of <SUP>3</SUP>H-FT-207 was higher and more continuous than that of <SUP>3</SUP>H-5-fluorouracil. Although the radioactivity after rectal administration of <SUP>3</SUP>H-FT-207 and <SUP>3</SUP>H-5-fluovouracil was widely distributed in the various tissues of the animal with or without tumor, the highest concentration of the radioactivity was observed in the kidneys, and higher in tumor. The radioactivity in lymphatic gland reached a maximum level within 2-4 hr after the rectal administration of <SUP>3</SUP>H-FT-207 and declined very slowly. The urinary excretion of radioactivity within 24 hr was about 30% of the administered dose of <SUP>3</SUP>H-FT-207. More than 85% of the excreted radioactivity accounted for FT-207 and its metabolite, &alpha;-fluoro-&beta;-alanine. Other metabolites such as 5-fluorouracil, &alpha;-fluoro-&beta;-ureidopropionic acid and tritiated water were detected in small amounts in rat urine. The radioactivity in blood and tumor, 4 hr after rectal administration of <SUP>3</SUP>H-FT-207, was found to represent FT-207. However, the radioactivity in liver was due to the presence of &alpha;-fluoro-&beta;-alanine. About 90% radioactivity in lymphatic gland within 2-6 hr after rectal administration of <SUP>3</SUP>H-FT-207 was detected as FT-207.

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

no.194, pp.361-367, 1898-04-26

著者

Ha Jeoung-Hee Lee Maan-Gee Chang Soo-Min LEE Jae-Tae

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.29, no.7, pp.1414-1417, 2006-07-01

被引用文献数

11

---

Fossilia Mastodi Ossis, which is a skeletal fossil of a Mastodon, an ancient mammal, has been found to have anxiolytic, sedative and anticonvulsant activities in Oriental medicine. In this study, in vivo characterization of the sedative activities of Fossilia Mastodi OSSIS was performed in order to obtain basic information for the development of a putative natural sedative. The 80% methanol extract of Fossilia Mastodi OSSIS given per os at a dose of 3g/kg in mice showed anxiolysis, potentiation of pentobarbital sleeping time, reduced locomotor activity, and anticonvulsive activity. Fossilia elicited GABA_A receptor-mediated anxiolysis. The data obtained suggest that the 80% methanol extract of Fossilia Mastodi OSSIS contains some biologically active principles with sedative activity.

著者

永吉 剛 木本 茂

出版者

公益社団法人日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.21, no.6, pp.511-514, 1985-06-01

著者

足達 郁夫 山守 照雄 平松 義春 酒井 克則 三原 伸一 川上 勝 升井 正生 宇野 攻 上田 元彦

出版者

公益社団法人日本薬学会

雑誌

Chem Pharm Bull (Tokyo) (ISSN:00092363)

巻号頁・発行日

vol.36, pp.4389-4402, 1988

被引用文献数

1

---

A series of 4-aryl-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylate derivatives (I) was synthesized and tested for binding affinity to Ca^<2+> channels in rat cerebral cortex membranes, coronary vasodilator effect in isolated guinea pig hearts, and antihypertensive activity in spontaneously hypertensive rats. Several compounds had potent coronary vasodilator and antihyper tensive activities. The structure-activity relationships of the series indicated that a lipophilic 3-alkyl substituent with moderate bulkiness was effective for enhancing the pharmacological potencies. Among them, methyl 4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)thieno[2,3-b]-pyridine-5-carboxylate (S-312) was selected as a promising cardiovascular agent. The relationship between the absolute configuration of S-312 and its biological activities is also presented.

著者

松岡 宏治 大田 雅照

出版者

公益社団法人日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.46, no.3, pp.215-222, 2010-03-01

参考文献数

48

著者

Koga Kenjiro Murakami Masahiro Kawashima Susumu

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.22, no.4, pp.402-406, 1999-04-15

参考文献数

22

被引用文献数

1

---

The effects of fatty acid glycerol esters and Tweens on the intestinal transport of ceftibuten were studied using a diffusion chamber system. The apparent permeation coefficient (P<SUB>app</SUB>) was used as an index of the mucosal permeability to ceftibuten. The P<SUB>app</SUB> markedly increased by the addition of hexaglycerol monostearate (HGMS) or hexaglycerol sesquistearate (HGSS) under an H<SUP>+</SUP>-gradient condition, while hexaglycerol tristearate (HGTS) and Tweens showed no effect on the absorptive ceftibuten permeability. These result are in agreement with those obtained in the previous study in the brush-border membrane vesicles. On the other hand, in the absence of an H<SUP>+</SUP>-gradient, the S-to-M transport of ceftibuten was proven to be significantly higher than the M-to-S one. In addition, either ATP-depletion of the mucosa or the addition of probenecid proved to enhance significantly the permeability of ceftibuten. These findings suggest the existence of an active secretory transport system for ceftibuten in the jejunal mucosa. To estimate potential effects of glycerol esters on efflux pumps as well as peptide transporters, the mucosal-to-serosal (M-to-S) and serosal-to-mucosal (S-to-M) permeability in the presence of the esters was further examined. HGMS, HGSS and HGTS markedly enhanced the M-to-S but not the S-to-M transport in the ATP-depleted jejunum without an H<SUP>+</SUP>-gradient, in which conditions contributions of both peptide transporter and efflux pump should be substantially small. HGMS and HGSS significantly enhanced the M-to-S ceftibuten transport in the ATP-depleted jejunum with an H<SUP>+</SUP>-gradient (p<0.01 vs. M-to-S transport without surfactant under the same conditions). Whereas, these glycerol esters were fround hardly to affect the P<app> of the S-to-M transport. These results indicate that the enhanced intestinal transport of ceftibuten due to the glycerol esters may be based on their effects on peptide transporters but neither on efflux pumps nor on the passive permeation routes.

著者

石津 利作

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

no.335, pp.1-12, 1910-01-26

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純粹度ヲ保シ難キ製品ニ就キ極メテ不確實ナル分析ヲ基礎トシテC_<16>H_<19>O_4SK+H_2Oナル化學記號ヲ設定スルハ大早計ナルヲ難シ純レスピラチン」ナルモノニ於テ喜多尾氏カ言明セルカ如キ特殊ノ形熊並ニ性状ヲ發見スルコト能ハサルヲ述へ同氏ガ「デブス氏法ニ依リテ硫黄ヲ定量シ其成績ニ甚シキ動揺アルハ偶々以テ自己技術ノ拙劣ヲ表ハスモノニシテ未タ純レスピラチン中硫黄定量ノ困難ナル證據トナスニ足ラサルヲ論シ終ニ藥學雜誌上ニ發表セラレタルカ如ク「チオヂクレオソール」ナル名稱ハ單ニ發明名稱ニシテ此名稱ニ依リ純レスピラチン」ノ分子構造ヲ表示セントスル意ニ非スシテ只其成分ノ列記ニ過キサルコトヲ齊シク他ノ雜誌並ニ新聞ニ廣古シ世人ヲ惑ハスカ如キ告白ヲ避ケ且ツ硫黄含量ノ確定スルニ至ル迄C_<16>H_<19>O_4SK+H_2Oノ如キ更ニ根據ナキ化學記號ヲ吹聽スルノ輕學ヲ戒メラレンコトヲ發明者ニ希望セリ

著者

Kwon Hak Cheol Jung Chil Mann Shin Cha Gyun LEE Jong Kyo CHOI Sang Un KIM Sun Yeou LEE Kang Ro

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.48, no.11, pp.1796-1798, 2000-11-01

参考文献数

17

被引用文献数

5

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The phytochemical study of the aerial parts of Aster scaber THUNB. (Asteraceae) yielded a new caffeoyl quinic acid, (-) 3,5-dicaffeoyl-muco-quinic acid (2) and three known compounds, (-) 3,5-dicaffeoyl quinic acid (1), (-) 4,5-dicaffeoyl quinic acid (3), (-) 5-caffeoyl quinic acid (4). The structures were established by high resolution spectroscopic methods. The antiviral effects against HIV-1 integrase of the compounds was evaluated. (-) 3,5-Dicaffeoyl-muco-quinic acid (2) exhibited potent antiviral activity with an IC_<50> value of 7.0±1.3 μg/ml.

著者

KITAGAWA Shuji SUGAYA Yoshio

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.19, no.2, pp.268-273, 1996-02-15

参考文献数

34

被引用文献数

4 1

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Characteristics of transport of an oral aminocephalosporin, cefroxadine, in rabbit small intestinal brush border membrane vesicles were examined. Uptake rate of cefroxadine was saturable in the presence of an inward H<SUP>+</SUP> gradient, and kinetic parameters were similar to those of cephradine. However, the uptake rate was almost linear with the concentration in the absence of an inward H<SUP>+</SUP> gradient up to 5mM. Overshoot phenomenon was observed in the presence of an inward H<SUP>+</SUP> gradient at 37°C, but it disappeared with decrease of temperature. The Arrhenius plot of uptake rate constant showed a break point at approximately 30°C. Cefroxadine uptake was optimum in the vicinity of pH 5.5 at 37°C, but the dependence on extravesicular pH disappeared at 15°C. The uptake of cefroxadine in the presence of an inward H<SUP>+</SUP> gradient was markedly inhibited by other aminocephalosporins such as cephalexin, but the inhibition was only slight in the absence of an inward H<SUP>+</SUP> gradient. Alkyl alcohols such as n-hexyl alcohol also inhibited H<SUP>+</SUP>-coupled uptake of cefroxadine at the concentration range at which the alcohols increased the membrane fluidity, and overshoot phenomenon diminished, suggesting that H<SUP>+</SUP>-coupled transport of cefroxadine is sensitive to the alcohol-induced increase in membrane fluidity. On the other hand, the alcohols rather stimulated its uptake in the absence of an H<SUP>+</SUP> gradient.

著者

古川

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

no.98, 1890-04-26

著者

田原

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

no.176, pp.1015-1016, 1896-10-26

著者

木村 善行 大南 宏治 有地 英子 奥田 拓道 有地 滋 林 輝明

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.102, no.7, pp.p666-669, 1982-07

被引用文献数

2

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It was found that high sugar diets induced an elevation in serum levels of triglyceride and insulin in rats by the oral administration for 2 months. When black substances isolated from crude black sugar were orally administered to rats with the high sugar diets, such elevation was not observed. In addition to these effects, black substances were found to reduce serum lipid peroxide. Black substances were found to inhibit absorption of glucose in the rat small intenstine. Therefore, it was suggested that the effect of black substances on hyperlipemia in rats fed with the high sugar diets might be partly attributable to an inhibition of glucose absorption in the small intenstine.

著者

大谷 靖 川瀬 勝凡 林 敬一郎 龝本 晃 平山 宏 中村 勝一 小倉 勲

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.89, no.8, pp.1115-1118, 1969-08

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Formation of azulene from hydronaphthalene by the application of Lang's method was observed when using decalin as the starting material, with single metal such as iron and Raney nickel or activated carbon as a catalyst, and the amount of the product was greater when using trans-decalin rather than cis-decalin. This is considered to be due to the difference in the distance between hydrogen atoms at 5- and 9-positions. A part of the cis isomer was found to change into the trans type when heated. There was no formation of azulene when using tetralin as the starting material. The spectra of azulene solution after irradiation of ultraviolet or γ-rays showed smaller change in absorption intensity than that of guaiazulene. Irradiation of γ-rays on azulene solution was found to produce reduction and polymerization, as in the case of guaiazulene, from the result of gas chromatographic analysis. In the case of oxygen-containing compounds, irradiation with ultraviolet or γ-rays was found to produce turbidity but isolation and identification of this product were not possible due to the minute amount formed. These irradiation experiments indicated that azulenes without a side chain were more stable than guaiazulenes.

著者

上野 金太郎

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

no.170, pp.363-373, 1896-04-26

著者

Takahiro Hayashi Saori Ikehata Haruna Matsuzaki Kimio Yasuda Toshiyasu Makihara Akihiko Futamura Yuki Arakawa Rika Kuki Kumiko Fukuura Hiroshi Takahashi Naoharu Mori Takashi Higashiguchi Shigeki Yamada

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.37, no.12, pp.1860-1865, 2014-12-01 (Released:2014-12-01)

参考文献数

25

被引用文献数

3 7

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Morphine, oxycodone, and fentanyl are commonly used to control cancer pain. Because these drugs have differences in receptor affinity or pharmacokinetic parameters, changing the opioid formulation may result in an unexpected outcome, depending on the patient’s condition. This study investigated whether low serum protein levels influence the effectiveness of opioid rotation by determining the impact of serum albumin levels on the analgesic effect before and after opioid rotation from morphine or oxycodone to fentanyl in cancer patients. The patients were classified into 3 groups according to their serum albumin levels before opioid rotation: group 1, <2.5 g/dL; group 2, from 2.5 g/dL to <3.0 g/dL; and group 3, ≥3.0 g/dL. There was no significant change in the percentage of patients with good pain control after rotation in group 1 or group 2; however, the percentage of patients with good pain control increased significantly in group 3. When the percentage of patients whose numerical rating scale scores increased, were unchanged, or decreased after rotation were compared, a significant difference in the percentage of those showing improvement was noted among the 3 groups and between groups 1 and 3. These findings suggest that monitoring serum albumin levels during fentanyl therapy is useful for pain management, and that the effectiveness of opioid rotation to fentanyl in patients with serum albumin levels of <2.5 g/dL should be carefully evaluated after rotation.

著者

浅川 義範

出版者

公益社団法人日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.21, no.11, pp.1157-1158, 1985-11-01