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著者
大蔵省印刷局 [編]
出版者
日本マイクロ写真
巻号頁・発行日
vol.1910年09月20日, 1910-09-20
著者
石黒 正路 今城 精一
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.54, no.5, pp.427-436, 1996-05-01 (Released:2009-11-16)
参考文献数
30
被引用文献数
2 2

Complex structures of neocarzinostatin (NCS) and β-lactamase/β-lactam antibiotics were built using NMR and crystallographic data of the proteins. On binding of ligands to proteins, particular amino acid side chains as well as ligands show dynamic character to exhibit specific molecular recognition. NMR studies and conformational analysis of the Phe 78 side chain of NCS revealed that the Phe 78 residue plays a major role on the chromophore binding through conformational change of the side chain aromatic moiety. Crystal structures and computational modeling of the enzyme-ligand complexes indicated that at the active site, the carboxylate of β-lactam antibiotics induces the conformational change of the Lys 73 residue and acts as a trigger of the hydrolytic reaction (acylation). Modeling of the acyl-enzyme structures also suggested the role of a mobile water molecule at the active site for deacylation. Experimental (NMR and X-ray crystallography) and computational results provided a fruitful information about molecular interaction between proteins and ligands.
著者
小松 生明
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.136, no.2, pp.329-335, 2016-02-01 (Released:2016-02-01)
参考文献数
34

Morphine with its potent analgesic property has been widely used for the treatment of various types of pain. However, the intrathecal (i.t.) administration of morphine at doses far higher than those required for antinociception exhibited nociceptive-related behaviors consisting of scratching, biting and licking, hyperalgesia, and allodynia in mice. Morphine-3-glucuronide (M3G), one of the major metabolites of morphine, has been found to evoke nociceptive behaviors similar to those after high-dose i.t. morphine. It is plausible that M3G may be responsible for nociception seen after high-dose i.t. morphine treatment. This article reviews the potential mechanism of spinally mediated nociceptive behaviors evoked by i.t. M3G in mice. We discuss the possible presynaptic release of nociceptive neurotransmitters/neuromodulators such as substance P, glutamate, dynorphin, and Leu-enkephalin in the primary afferent fibers following i.t. M3G administration. It is possible to speculate that i.t. M3G could indirectly activate NK1, NMDA, and δ2-opioid receptors that lead to the release of nitric oxide (NO) in the dorsal spinal cord. The major function of NO is the production of cGMP and the activation of protein kinase G (PKG). The NO-cGMP-PKG pathway plays an important role in M3G-induced nociceptive behavior. The phosphorylation of extracellular signal-related kinase (ERK) in the dorsal spinal cord was also evoked via the NO-cGMP-PKG pathway through the activation of δ2-opioid, NK1, and NMDA receptors, contributing to M3G-induced nociceptive behaviors. The demonstration of a neural mechanism underlying M3G-induced nociception provides a pharmacological basis for improved pain management with morphine at high doses.
著者
野口 照久 橋本 喜信 小坂 璋吾 菊池 正義 宮崎 幸信 先本 礼次 加治 有恒
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.88, no.3, pp.344-352, 1968-03-25 (Released:2008-05-30)
参考文献数
21

Some observations were made on the anti-trichophyton action of 2-naphthyl N-methyl-N-arylthiocarbamate (A). In vitro antifungal activity decreased slightly when the thiocarbamate was changed to carbamate, and a marked lowering in the in vitro effect was observed. The antifungal activity disappeared entirely when the thiocarbamate was changed to dithiocarbamate and thiolcarbamate. When the aryl group in A is a naphthyl, antifungal activity is present only when 1-naphthyl is present and other three combinations are entirely ineffective. When the aryl is a substituted phenyl, compounds having methyl, methoxyl, or halogens, those with the Hammet constant in the range of +0.23 to -0.27, have marked antitrichophyton activity in vivo, but those with nitro, formyl, carboxyl, sulfonamido hydroxyl, or dimethylamino group show marked decrease in the effect. The series of compounds having the A type will henceforth be designated as naphthiomates.
著者
野口 照久 小坂 璋吾 橋本 喜信 菊池 正義 宮崎 幸信 加治 有恒
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.88, no.3, pp.353-358, 1968-03-25 (Released:2008-05-30)
参考文献数
16
被引用文献数
1 2

Examinations were made on the effect of oral administration of 2-naphthyl N-methyl-N-arylthiocarbamates (naphthiomates), an effective antimicotic agent for external use, against experimental trichophytosis. Finely powdered 2-naphthyl N-methyl-N-(m-tolyl)-thiocarbamate (naphthiomate-T) and 2-naphthyl N-methyl-N-(1-naphthyl) thiocarbamate (naphthiomate-N) showed an effect comparable to griseofulvin in about four-fold dose of the latter. In vivo metabolism of naphthiomate-T was examined in guinea pigs and rabbits, and it was found that the majority is excreted in the feces without decomposition, and little is absorbed through the intestinal tract. N-Methyl-m-toluidine and β-naphthol were detected from urine, feces, and blood as the metabolites.
著者
石黒 正路 今城 精一
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.42, no.8, pp.722-731, 1984-08-01 (Released:2009-11-13)
参考文献数
52
被引用文献数
1 1

Recent application of three dimensional computer graphics technics has widely expanded to molecular modeling. This article describes a brief history of computer graphics use in molecular modeling, function of hardware and software and its application to molecular modeling in Suntory computer aided drug-design system.
著者
マイケル スロート
出版者
有斐閣
雑誌
哲学雑誌 (ISSN:03873366)
巻号頁・発行日
vol.127, no.799, pp.126-161, 2012
著者
深井 誠一 五井 正憲
出版者
香川大学農学部
雑誌
香川大学農学部学術報告 (ISSN:03685128)
巻号頁・発行日
vol.53, no.106, pp.25-29, 2001-03
被引用文献数
1

一重咲きタイプのバレリーナ,八重咲きタイプのアンジェリケ,枝咲きタイプのオレンジブーケの3品種のチューリップの花芽分化を走査型電子顕微鏡で観察した.バレリーナの場合,3枚の普通葉を分化した後茎頂が肥大し,その外花被,内花被,雄ずい第1環,第2環の順で3つずつの原基が分化した.その後茎頂の中央部は三角形になり,その頂部がへこみ始め雌ずいへと分化した.雄ずいが伸長し雌ずいを囲みその後花被が伸長して全体を覆った.八重咲きのアンジェリケでは,花被の分化に引き続き多数の突起状の原基が分子し,そのうち外側の多くは花被化し内側のいくつかは雄ずい化した.枝咲きのオレンジブーケでは中心の花芽の分化完成後,腋芽の茎頂は1枚の普通葉を分化した後花芽を分化した.
著者
山下史路著
出版者
文藝春秋
巻号頁・発行日
2005