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.50, pp.155-157, 1886-04-26
著者
新川 蘭順 木曽 達也 片岡 博文 礒井 孝 柿田 孝雄 正垣 武志 大坪 義和
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.116, no.10, pp.783-791, 1996-10-25

The antagonism of histamine H_2-receptor by SWR-104SA (1'-bromo-N-[3-[3-(1-piperidinylmethyl) phenoxy] propyl]-spiro [1,3-dioxolane-2,9'-pentacyclo-[4. 3. 0. 0.^<2,5>0.^<3,8>0.^<4,7>] nonane]-4'-carboxamide monooxalate) was estimated using the isolated guinea-pig atrium and gastric acid secretion in rats. The concentration-response curves for the positive chronotropic effect of histamine on the atrium were displaced to the right in parallel without change in the maximum response by SWR-104SA and roxatidine acetate hydrochloride (roxatidine). The pA_2 values of SWA-104SA and roxatidine acetate hydrochloride were 7.27 and 7.38,respectively. The slopes of the regression line of log (DR-1) against log SWR-104SA and roxatidine concentration were 1.00 and 0.92,respectively. There was no significant difference between the two compounds with respect to the histamine H_2-receptor antagonism and/or binding manner in vitro. In the rat gastric fistula model stimulated by histamine, however, antisecretory potency of SWR-104SA was 3 times less than that of roxatidine. SWR-104SA given p.o. prevented the formation of gastric lesion induced by HCl-ethanol and indomethacin dose-dependently, roxatidine also prevented its formation by HCl-ethanol, but failed to prevent that by indomethacine. These antiulcer activities of SWR-104SA were shown at the lesser doses of antisecretory activity. On the other hand, roxatidine did not prevent the ulcer formation at the same dose level of antisecretory activity. These results indicate that the antiulcer effect of SWR-104SA is not caused by the antisecretory action alone. In addition, the mucosal protective activity of SWR-104SA for HCl-ethanol induced gastric lesion was independent of endogenous prostaglandins. Moreover SWR-104SA had inhibitory effects on indomethacin-induced gastric hypermotility in rats. These actions may partly explain the gastric protection of this compound and additional mechanisms such as mucosal blood flow could be involved in the antiulcer efficacy. Consequently, it appears that SWR-104SA is a new antiulcer drug that exerts a potent cytoprotective effect in addition to its gastric antisecretory activity.
著者
王 誠明 太田 節子 篠田 雅人
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.109, no.12, pp.949-953, 1989-12-25
被引用文献数
2

The survival effect of mice irradiated with a lethal dose of X-ray was studied by use of 60 kinds of Chinese traditional medicines. Methanol extracts of these medicines were prepared, and then each extract injected intraperitoneally into male mice before or after whole-body irradiation. As a result of these studies, the survival effects with Ogi-kentyu-to, Simotu-to, Sessyoin, Zokumei-to and Boi-ogi-to were observed by intraperitoneal injection before irradiation. Of these effective methanol extracts, only Zokumei-to was shown to have a significant survival effect by intraperitoneal injection after irradiation.
著者
大島 健吉
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.154, pp.1114-1118, 1895-12-26
著者
菅澤
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.512, pp.869-870, 1924-10-26
著者
松南 千壽
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.520, pp.540-552, 1925-06-26

Tropacocainhydrochlorid kann eine Stunde lang auf 130° erhitzt werden, ohne dass dabei eine Veranderung (sowohl in chemische als auch in physikalischer Hinsicht) zu befurchten. Erst bei zwei stundigem Erhitzen auf 135-140° wird eine geringe Veranderung wahrnehmbar, die jedoch die Erfordernisse von Ph. Jap. nicht beeintrachigt. Sterilisirt man eine 2% ige wasserige salzsaure Tropacocainlosung nach der ublichen Methode, so bemerkt man ein Zeichen von Verseifung, indem man aus 10 g Salz 0.0004-0.0005 g Benzoesaure und 0.0006-0.0007 g Pseudotropin erhalt. Gegen Hitze ist die wasserige Losung des Pseudotropins sehr bestandig. Erst beim Erhitzen im Einschliessrohr auf 170-180° wird eine Spur Tropidins gebildet.Der Alkaligehalt des weichen Glases wirkt beforded auf die Verseifung der salzsauren Tropacocainlosung. Dem Sonnenlicht bezw. Urtraviolettstrahlen ausgesetzt zeigte das Tropacocainhydrochlorid und seine Losung eine auffallende Bestandigkeit.
著者
衣笠
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.319, pp.946-948, 1908-09-26
著者
沢田 英夫 矢野 博子 木戸 啓
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.92, no.10, pp.1237-1241, 1972-10-25

Besides the unchanged drug, two major metabolites were found from the urine of animals that received orally high doses of bromazepam, 7-bromo-1,3-dihydro-5-(2-pyridyl)-2H-1,4-benzodiazepin-2-one. The metabolites were purified by column chromatography on silica gel and recrystallization. From the spectral and elemental analysis data, the structure of these metabolites were identified as 2-amino-5-bromobenzoylpyridine and assumed to be 2-amino-5-bromo-3-hydroxybenzoylpyridine, the latter being excreted as its glucuronide in the urine. It may be concluded that bromazepam after opening of the diazepine ring undergoes a process of hydroxylation.
著者
沢田 英夫 原 明
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.95, no.4, pp.430-438, 1975-04-25

Five metabolites appearing in the urine of the rabbit fed bromazepam were isolated; these are 2-(2-amino-5-bromobenzoyl)pyridine (ABBP), 2-(2-amino-5-bromo-3-hydroxybenzoyl)pyridine (3-OH ABBP), 3-hydroxybromazepam, and two new matabolites, 9-hydroxybromazepam and 5'-hydroxybromazepam. The new metabolites were characterized by thin-layer chromatography (TLC) ; elemental analysis, and infrared, nuclear magnetic resonance, and mass spectrometries. Metabolites, which were excreted mainly as conjugates of glucuronic acid and/or sulfuric acid, were measured by preparative TLC and characteristic colorimetric method after enzymic hydrolysis of the conjugates. Urinary excretion of bromazepam and its metabolites have been studied in dogs, rabbits, mice, rats and guinea pigs after massive doses of bromazepam. The conjugated 3-OH ABBP was the major metabolite in rabbits (17.1% of the dose) and dogs (6.2% of the dose) during 24 hr. The major metabolites found in rats, however, were the conjugated form of 3-OH ABBP (5.3% of the dose), 5'-hydroxybromazepam (4.2% of the dose), and ABBP (3.8% of the dose), and 9-hydroxybromazepam was not excreted. In mice the major metabolite was the unconjugated form of 3-hydroxybromazepam (7.5% of the dose). In guinea pigs, two unknown metabolites, besides the above five metabolites, were excreted, and it was confirmed that one of them was benzhydrol analog of ABBP. When intraperitoneal injection was compared with oral administration of the same dose in the rabbit, the urinary excretion of the ring-cleaved metabolites, ABBP and 3- OH ABBP, decreased, but that of the others, 3-hydroxybromazepam and 5'-hydroxybromazepam, increased. On the basis of these data, pathways of bromazepam were postulated (Chart 1). Quantitative differences in the urinary metabolites of bromazepam in each species was clearly observed during the first 24-hr period.
著者
金尾 清造
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.1927, no.540, pp.102-120, 1927-02-26 (Released:2010-11-30)
参考文献数
33
被引用文献数
1
著者
藤田 勇三郎 上原 郁恵 森本 泰子 中嶋 真由美 波多野 力 奥田 拓男
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.108, no.2, pp.129-135, 1988
被引用文献数
38

Inhibitory effects of caffeoylquinic acids isolated from leaves of Artemisia species and other related compounds on the lipoxygenase dependent peroxidation of linoleic acid were studied by kinetic and electron spin resonance(ESR) measurements. The order of inhibition activity was as follows : 3, 5-dicaffeoylquinic acid (ID<SUB>5</SUB>0=2.0&times;10<SUP>-</SUP>5 M)=rosmarinic acid > geraniin (2.8&times;10<SUP>-</SUP>5 M)>&alpha;-tocopherol (3.7&times;10<SUP>-</SUP>5 M)>chlorogenic acid (7.5&times;10<SUP>-</SUP>5 M)=caffeic acid>ferulic acid (2.5&times;10<SUP>-</SUP>4 M). This order coincided well with that obtained from the measurement of radical scavenging activities of these compounds against 1, 1-diphenyl-2-picryl hydrazyl. The inhibition profile of these compounds on lipid peroxidation in the lipoxygenase system was quite similar to those obtained previously in the biological systems of rat liver mitochondria and microsomes. In the separate ESR measurements in alkaline dimethyl sulfoxide solution, all caffeoyl-quinic acids exhibited relatively stable ESR signals assigned as a radical derived from the one-electron oxidation of dihydroxyphenyl group. From these results, it was concluded that the radical scavenging mechanism is commonly operative in both chemical and biological peroxidation systems.