著者
清水 當尚 宇野 準 伊藤 継孝 増田 義信 黒川 美貴雄
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.116, no.7, pp.533-547, 1996-07-25 (Released:2008-05-30)
参考文献数
55
被引用文献数
4 8

Zonisamide (1, 2-benzisoxazole-3-methanesulfonamide, AD-810) is a broad spectrum antiepileptic drug which has been launched in Japan and South Korea. It lacks the ureide structure included in most of the existing antiepileptic drugs. Zonisamide was synthesized by the sulfonation and the successive amination of 1, 2-benzisoxazole-3-acetic acid in a very poor yield. After several efforts to optimaize the compound, zonisamide was selected based on the balance of the efficacy and safety. The yield was greatly improved by the development of new synthetic routes. Zonisamide suppressed maximal electroshock seizures in mice, rats, rabbits and dogs. Its therapeutic plasma concentration range between anticonvulsant and neurotoxic effects was much wider than that of the existing antiepileptic drugs. In electroencephalographic studies on animal models of epilepsy, zonisamide, like phenytoin and carbamazepine, restricted the spread or propagation of seizures and, like sodium valproate, it suppressed the epileptogenic focus activity. Zonisamide was effective in several kindling models. In clinical studies, zonisamide exerted the efficacy against partial seizures (simple, complex, secondarily generalized seizures) and some generalized seizures (tonic-clonic, tonic, atypical absence seizures) that were comparable to that of carbamazepine and sodium valproate, respectively. Zonisamide was also effective in monotherapy. The adverse effects related with zonisamide were mainly drowsiness, ataxia, loss of appetite and gastrointestinal symptoms. Serious adverse effects which may be life-threatening have not been reported.
著者
小松 謙
出版者
京都府立大学
雑誌
京都府立大学学術報告. 人文 (ISSN:18841732)
巻号頁・発行日
no.68, pp.55-91, 2016-12
著者
池上 四郎 柴崎 正勝
出版者
The Society of Synthetic Organic Chemistry, Japan
雑誌
有機合成化学協会誌 (ISSN:00379980)
巻号頁・発行日
vol.38, no.11, pp.1037-1052, 1980-11-01 (Released:2010-04-23)
参考文献数
67
被引用文献数
5 6

This review, including two parts, deals with recent progress in the prostaglandin field. The first part is concerned with the synthetic studies of endoperoxides, thromboxanes, prostacyclins and leukotrienes. The second describes briefly the biological properties of various stable synthetic analogs.
著者
佐藤 真理子 趙 羅衡 田村 照子
出版者
一般社団法人 日本家政学会
雑誌
一般社団法人日本家政学会研究発表要旨集
巻号頁・発行日
vol.66, 2014

目的 民族衣装には,気候・風土に適応可能な素材の選択,姿勢・動作を含む生活様式を反映したデザインの工夫等,長い年月にわたり積み重ねられてきた知恵が詰まっている.本研究では,アジアにおける民族服の下衣に着目し,素材とデザインが温熱的快適性,運動機能性へ及ぼす影響について検討を行った.<br>方法 被験者は23&plusmn;1歳の若年女性5名,実験衣はシャルワール(インド),バジ(韓国),ストレートパンツ(現代服)の3種である.運動機能性評価としては,同一素材で製作した実験衣を着用し,9種の動作時(立位,椅座,正座,胡坐,立膝,横座り,体育座り,日本のお辞儀,韓国のお辞儀)における衣服圧測定と官能評価,温熱的快適性評価としては,各市販品(ポリエステル100%・重量約200gで統一.インド,韓国,東京で購入)による物性試験と衣服気候計測(27℃・50%RH環境下で立位安静&rarr;足踏み運動&rarr;座位安静)を行った.<br>結果 シャルワールは,通気性と透湿性に優れ,接触冷温感が高く,暑熱気候への適応性が示された.バジは,接触冷温感が低く,衣服内温度は高く,防寒機能に優れていると考えられる.現代服は,正座,胡坐,立膝,日本と韓国のお辞儀において,高い衣服圧を示し,床に座っての姿勢や動作の多い&ldquo;伝統的所作&rdquo;に適さない様子が明らかとなった.
著者
柴崎 正勝
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.101, no.12, pp.1073-1091, 1981-12-25 (Released:2008-05-30)
参考文献数
69
被引用文献数
2 3

The present article describes our recent synthetic studies on various biologically active compounds, including synthesis and biological properties of prostacyclins, synthetic approach toward thromboxanes, and total syntheses of coriolin and hirsutic acid C. In the final part of this review, some new reactions, exploited in connection with synthetic studies on prostacyclins, are also described.
著者
MARUYAMA Akiko
出版者
GRIPS Policy Research Center
雑誌
GRIPS Discussion Papers
巻号頁・発行日
vol.18-15, 2018-11

This study analyzes a two-sided search model in which agents are vertically heterogeneous and agents on one side do not know their own type. Agents with imperfect self-knowledge update their beliefs based on the offers or rejections they receive from others. The results are as follows. An agent with imperfect self-knowledge lowers his or her reservation level if the agent receives a rejection that leads him or her to revise belief downward. However, an agent with imperfect self-knowledge does not raise his or her reservation level even if the agent receives an offer that leads him or her to revise his or her belief upward. As a result, an agent with imperfect self-knowledge has the highest reservation level when he or she has just entered the market; after that, a series of meetings gradually lowers his or her reservation level over the duration of the search.
著者
坪島 正巳 松本 公一郎 新井 義信 若塚 弘久 川崎 晃義
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.112, no.7, pp.447-469, 1992-07-25 (Released:2008-05-30)
参考文献数
54
被引用文献数
3 4

The therapeutic use of prostaglandins (PGs) which contain various biological activities and are unstable was successfully achieved. PGs were produced in a large scale according to the Corey method and could be stabilized by the formation of a clathrate compound with cyclodextrin, which enabled the production of marketable form of highly pure PGs. Diligence in the development of native PGs and their structural analogs for human therapy resulted in the following six drugs now being on the market in Japan : PGF2α as the first drug of PGs in the world which induces labor ; PGE2 as an orally active labor inducing drug ; PGE1 for the treatment of peripheral vascular diseases ; gemeprost for therapeutic abortion in the middleterm ; ornoprostil, as an oral anti-ulcer agent ; limaprost for the treatment of peripheral vascular diseases as an oral agent.
著者
鶴田 峯生 三ケ島 浩 大江 孝範 川崎 和幸 瀬戸口 信郎 中 洋一 田原 哲治
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.109, no.1, pp.33-45, 1989-01-25 (Released:2008-05-30)
参考文献数
28
被引用文献数
7 5

Several imidazolylpyridinemethanols and imidazolylbenzenemethanols were prepared and evaluated for an inhibitory activity against arachidonic acid-induced platelet aggregation. The result shows that the arylmethanol moiety is essential for the activity and may correspond to the 15-OH group of prostagrandin H2 (PGH2). Among the compounds tested, 4-[α-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3, 5-dimethylbenzoic acid (XV) was found to have a potent inhibitory activity and a long duration of action. Structureactivity relationships are also discussed briefly.