著者

加瀬 佳年 由井薗 倫一

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.740-747, 1961-05-25 (Released:2010-02-19)

参考文献数

30

被引用文献数

3

---

The pharmacology of d-N, N, 1-trimethyl-3-(ethylsulfonyl)-3, 3-diphenylpropylamine hydrochloride (A-5) was described in detail. A-5 showed a long-acting antitussive activity, duration of the effect being 18.9 times that of codeine (intravenous) and 13.5 times that of codeine (oral), though 50% antitussive dose is only 1.4 and 1.7 times that of codeine in dogs and cats, respectively. The site of action seemed to be the cough center per se. Toxicity in mice (subcutaneous) is 1.5 times that of codeine and 30% that of Methadone. No tendency to establish tolerance, cumulative action, or addiction liability was found by long-term administration. Analgesic action and other actions were discussed.

著者

角 保男

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.652-655, 1961-05-25 (Released:2010-02-19)

参考文献数

5

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Leucoriboflavin 5′-phosphate derivatives were prepared by reductive acylation of riboflavin 5′-phosphate. These compounds were rather unstable and were easily hydrolyzed to riboflavin 5′-phosphate derivatives, regaining the yellow color. On heating with 17% hydrochloric acid, leucoriboflavin 5′-phosphate tetraacetate and monoethylformate yielded riboflavin 2′, 5′-anhydride, m.p. 300-302°. This substance was sensitive to light and formed lumichrome as the photo-decomposition product on exposure to light.

著者

角 保男

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.647-651, 1961-05-25 (Released:2010-02-19)

参考文献数

3

---

Leucoriboflavin, reduced form of riboflavin, is easily oxidized to riboflavin when shaken with air. To retain the leuco state, riboflavin was reduced with sodium dithionite or with zinc in acid solution to the leuco compound and its acylation with acetic anhydride or benzoyl chloride gave leucoriboflavin acylate. These compounds were stable in solid state but were easily decomposed to riboflavin acylate on exposure to sunlight or by heating, regaining the yellow color. Several decomposition products of leucoriboflavin acylate are described.

著者

久保 博昭

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.19, no.12, 1983

著者

川瀬 清

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.20, no.12, 1984

著者

馬 銭子

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.7, 1985

著者

ET 生

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.23, no.3, 1987

著者

森江 洞泥

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.23, no.3, 1987

著者

石井 永

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.14, no.2, 1978

著者

馬 銭子

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.23, no.4, 1987

著者

塚越 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.23, no.10, 1987

著者

村田 忠一

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.26, no.9, 1990

著者

立浪 良介 高橋 恭兵 大場 達也 丹保 好子

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.129, no.1, pp.147-153, 2009 (Released:2009-01-01)

参考文献数

32

被引用文献数

2 6

---

Methylglyoxal (MG), a highly reactive dicarbonyl compound, is a metabolic by-product of glycolysis. MG is often detected at high levels in the blood of diabetic patients. We examined whether MG was capable of inducing reactive oxygen species (ROS) production in bovine aortic endothelial cells (BAECs). The viability of BAECs decreased with time on treatment with 5 mM MG, and was almost completely lost at 24 h. In contrast, MG at 1 mM had little influence on BAEC viability up to 24 h, but induced the elevation of intracellular glutathione content at 24 h. Exposure of BAECs to MG caused a dose-dependent increase in oxidized-hydroethidine fluorescence intensity, indicating ROS production. In addition, aconitase inactivation, which is an indicator of intracellular superoxide, was observed in MG-treated cells. Finally, we found that MG at 5 mM increased the fluorescence intensity of BES-So, a specific probe for superoxide. Together, the results suggest that MG induces superoxide production in endothelial cells, and that the accumulation of ROS may be linked to cytotoxic effects.

著者

吉富 英助 甲斐 晋

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

vol.1926, no.530, pp.307-308, 1926-04-26 (Released:2009-10-22)

著者

岸本 桂子 羽坂 亜希子 山浦 克典 福島 紀子

出版者

公益社団法人 日本薬学会

雑誌

薬学雑誌. 乙号 (ISSN:00316903)

巻号頁・発行日

vol.136, no.10, pp.1401-1413, 2016

被引用文献数

3

---

&emsp;Pharmacy is required to shift toward human service such as hearing the complaints of health. But the study about help-seeking behavior to pharmacist is not really investigated. We hypothesized that a decrease in expression visibility, due to pharmacists' typical masks, may negatively impact help-seeker' trust in pharmacist. The sample included 100 drugstore customers aged ≥18 years. Participants were stratified by gender and randomly assigned to two groups: evaluation of clear-masked and normal-masked pharmacists. After viewing a video with either male or female pharmacists wearing either clear or normal masks, participants completed a questionnaire. The primary outcome was trust in pharmacist measured by the Trust Scale and the secondary outcome was impression of the pharmacist measured by nineteen pairs of adjectives. There were no differences by gender on trust scores. Results revealed that both male and female pharmacists who wore clear masks were rated as more trustworthy than normal-masked pharmacists (<i>p</i><0.001, d=0.903, and <i>p</i>=0.001, d=0.716, respectively). Sixteen of nineteen adjectives reported for pharmacists wearing normal masks indicated greater negative intention than those with clear masks (d=0.431-1.469). In most cases, among pharmacists wearing clear masks, results showed positive correlations between trust and each impression adjective (r=0.279-0.710). Our findings indicate that pharmacists wearing normal masks, which partially hide facial expressions, may decrease customer's trust in pharmacist. Further, normal masks were associated with negative impression. To avoid the inhibition of help-seek behavior, we recommend that pharmacists wear a clear mask and increase non-verbal communication.<br>

著者

樽井 敦

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.11, pp.1245-1253, 2015 (Released:2015-11-01)

参考文献数

51

被引用文献数

2

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Multi-substituted β-lactam compounds have not only attracted considerable interest as core structures of pharmaceutical compounds such as antibiotics but also have been used as building blocks for the construction of β-amino acids. Electrophilic β-lactams can be used to enhance essential biological activities. Furthermore, the ring-opening reactions of electrophilic β-lactams can be used to provide facile access to β-amino acids. The introduction of an electronegative fluorine atom to a β-lactam ring to give the corresponding fluoro-β-lactam can be used as an effective strategy for the preparation of electrophilic β-lactams. In this review, we provide a summary of our recent research towards the direct functionalization of fluoro-β-lactams. This review has been divided into four topics, including: 1) the alkylation and hydroxyalkylation of α-bromo-α-fluoro-β-lactams (1); 2) the nickel-catalyzed cross coupling reaction of 1; 3) the asymmetric synthesis of fluoro-β-lactams using chiral ligands; and 4) the utilization of fluoro-β-lactams as highly electrophilic building blocks.

著者

鮫元 博文

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.29, no.7, 1993

著者

水田 博彰 鮫元 博文 小川 建志

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.111, no.8, pp.445-450, 1991-08-25 (Released:2008-05-30)

参考文献数

13

被引用文献数

1 1

---

The effects of triglycerides on the gastrointestinal absorption of 2-[3-(3, 5-di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo [3, 4-b] pyridin-1-yl] ethyl acetate (1) were investigated in dogs. The enhancing abilities of the triglycerides on the absorption of 1 were demonstrated as in the order of trilinolein>triolein>tristearin>tripalmitin. Among the series of fatty acids and monoglycerides, namely, digestive products of triglycerides by pancreatic lipase, linoleic acid and monolinolein showed the most potent solubilizing activities of 1 in a solution of bile salt. The incorporation of 1 into mixed micelle formed by lipids and bile salts was presumed to play an important role in the accelerated absorption of 1 after ingestion of triglycerides. On the basis of these findings, an emulsion containing 1 was prepared with soybean oil. The emulsion exhibited a remarkable improvement of the absorption of 1 compared to a suspension of the drug in methylcellulose solution.

著者

Matsuda Akira Takenuki Kenji Itoh Hiroko Sasaki Takuma Ueda Tohru

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.35, no.9, pp.3967-3970, 1987

被引用文献数

32

---

We have synthesized 2'-deoxy-2' (S) -methylcytidine (7), a new antileukemic nucleoside. The carbonyl methylation of 2'-ketonucleoside (1) with MeLi, Me<SUB>3</SUB>Al and MeMgX was examined. Only in the reaction with MeMgX, did the more hindered &beta;-attack afford the 2'-methyl-t-alcohol (2b). Compound 2b was converted into the methyl oxalate (4), which was subjected to radical deoxygenation to give the 2'-deoxy-2' (S) -methyl derivative (5). The deprotection of 5 followed by substitution with NH<SUB>3</SUB> furnished 7. The structure-activity relationships of 7 and some other 2'-branched-chain sugar cytidines against L1210 cells are also described.

著者

松田 彰 南川 典昭 佐々木 琢磨 上田 亨

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.36, no.7, pp.2730-2733, 1988

被引用文献数

32

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The design, synthesis and antileukemic activity of 5-alkynel-1-&beta;-D-ribofuranosylimidazole-4-carboxamides (6) are described. The cross-coupling reaction of 5-iodo-1-(2, 3, 5-tri-O-acetyl-&beta;-D-ribofuranosyl)imidazole-4-carboxamide (8) with various terminal alkynes in the persence of bis(benzonitrile)palladium dichloride and triethylamine in acetonitrile gave 5-alkylnyl derivatives (9) in high yields. Coupling of 8 with (trimethylsilyl)acetylene gave hte undesired dimer (10). Instead of (trimethylsilyl)acetylene, treatment of trimethyl[(tributyl-satannyl)ethynyl]silane with 8 in the absence of triethylamine produced the desired 5-[2-(trimethylsilyl)ethynyl] derivative (9f) in 77% yield. Deblocking of these nucleosides (9) gave the target nucleosides (6a-f). Among them, 5-ethynyl-1-&beta;-D-ribofuranosylimidazole-4-carboxyamide (6f) is the most potent inhibitor of the growth of murine L1210 cells in vitro (IC<SUB>50</SUB>=0.18 &mu;g/ml).