Miyamoto E, Murata Y, Kawashima S, Ueda M
School of Pharmacy, Hokuriku University, Kanazawa, Japan.
J Pharm Pharmacol. 1992 Mar;44(3):269-71. doi: 10.1111/j.2042-7158.1992.tb03599.x.
The haemolytic action of various N-alkyl derivatives (lauryl; C12H25-, myristyl; C14H29-, palmityl; C16H33-) of 1,3-diaminopropane, 1,4-diaminobutane, 1,5-diaminopentate, 1,6-diaminohexane, 1,7-diaminoheptane, 1,8-diaminooctane was examined using rabbit red blood cells. The activities of the various derivatives were compared with those of antiplaque agents commonly used as mouthwashes; cetylpyridinium chloride (CP) and chlorhexidine acetate (CH). The haemolytic activities of these agents were dependent on the length of the N-alkyl chain, whereas the number of methylene groups between the nitrogen atoms had little effect. The order of potency was CP, N-palmityl derivatives, N-myristyl derivatives greater than N-lauryl derivatives greater than CH which was similar to the order of the antiplaque effect evaluated in-vitro.
使用兔红细胞检测了1,3 - 二氨基丙烷、1,4 - 二氨基丁烷、1,5 - 二氨基戊酸、1,6 - 二氨基己烷、1,7 - 二氨基庚烷、1,8 - 二氨基辛烷的各种N - 烷基衍生物（月桂基；C12H25 - 、肉豆蔻基；C14H29 - 、棕榈基；C16H33 - ）的溶血作用。将各种衍生物的活性与常用作漱口水的防菌斑剂的活性进行了比较；十六烷基氯化吡啶（CP）和醋酸氯己定（CH）。这些药剂的溶血活性取决于N - 烷基链的长度，而氮原子之间的亚甲基数量影响很小。效力顺序为CP、N - 棕榈基衍生物、N - 肉豆蔻基衍生物大于N - 月桂基衍生物大于CH，这与体外评估的防菌斑效果顺序相似。
