YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
118 巻, 1 号
選択された号の論文の3件中1~3を表示しています
  • 兼松 顯
    1998 年 118 巻 1 号 p. 1-18
    発行日: 1998/01/01
    公開日: 2008/05/30
    ジャーナル フリー
    For understanding the three-dimentional mechanisms that control potency and selectivity of the ligand binding at the atomic level, we have analysed opioid receptor-ligand interaction based on the receptor's 3D model. The analyses of the interactions of some opioid ligands with the predicted ligand binding sites are consistent with the results of the affinity labeling experiments. On the basis of the three-dimentional structures of the putative binding sites in the opioid receptors, a potent κ agonist KT-95 was designed in our laboratory.
  • 松永 浩和, 三宅 荘八郎, 西島 功二
    1998 年 118 巻 1 号 p. 19-26
    発行日: 1998/01/01
    公開日: 2008/05/30
    ジャーナル フリー
    The stability of cefozopran monohydrochloride was studied by the non-isothermal method which was defined as a linear relationship between time and temperature. The value of activation energy (Ea) was calculated by applying the nonlinear least-square method. For the determination of the stability of cefozopran monohydrochloride in an aqueous solution, the respective Ea values at pH 2, pH 4 and pH 6 calculated by the non-isothermal method were 16.3, 21.8 and 20.7 kcal/mol (the mean value of Ea at 5°C/h and 10°C/h). The results were in good agreement with Ea value calculated by the isothermal method (pH 2; 16.2, pH 4; 21.8 and pH 6; 20.7 kcal/mol). For the determination of the stability of cefozopran monohydrochloride in a solid state, the Ea value calculated by the non-isothermal method was 18.7 kcal/mol (that calculated by the isothermal method was 19.5 kcal/mol). These results indicated that the non-isothermal method described in this paper could be adequately used for the stability study and was a rapid and accurate method for the determination of Ea values.
  • 池上 文雄, 関根 利一, 藤井 祐一
    1998 年 118 巻 1 号 p. 27-30
    発行日: 1998/01/01
    公開日: 2008/05/30
    ジャーナル フリー
    "Mokusaku-eki, " a kind of pyroligneous acid, is a dark brown color solution obtained from the charcoal burner of such Quercus spp. woods as a by-product. This is used as a folk medicine in water eczema. The n-hexane fraction of this solution contained several phenolic compounds such as 4-ethyl-2-methoxyphenol (3) and 2, 6-dimethoxyphenol (4), which could not be found in the fresh woods. Among these compounds, 3 has the highest anti-dermaptophyte activity against Trichophyton mentagrophytes at minimum inhibitory concentration (MIC) 150 μg/ml.
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