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溴化物镇静催眠药物、溴戊酮(溴异戊酰脲)和溴米那,以及它们的氯代类似物在小鼠体内的比较。

Comparison of the bromureide sedative-hypnotic drugs, bromvaletone (bromisoval) and carbromal, and their chloro analogues in mice.

作者信息

Mrongovius R I, Gaff G A, Rand M J

出版信息

Clin Exp Pharmacol Physiol. 1976 Sep-Oct;3(5):443-7. doi: 10.1111/j.1440-1681.1976.tb00621.x.

Abstract
  1. The central depressant effects of bromvaletone, carbromal and six non-bromo analogues were compared in mice. 2. The chloro analogues of bromvaletone and carbromal were slightly less potent as central depressant agents than the bromo compounds. 3. The chloro analogue of bromvaletone had the greatest margin between central depressant and lethal doses. 4. Lipophilicity (octanol-water partition coefficient) did not provide a unifying relationship for potency within this group of eight acylureas. However, within each of the two subsets of compounds, a linear relationship was found between relative potency and lipophilicity.
摘要
  1. 在小鼠中比较了溴戊酮、卡溴脲及六种非溴类似物的中枢抑制作用。2. 溴戊酮和卡溴脲的氯类似物作为中枢抑制药的效力略低于溴化合物。3. 溴戊酮的氯类似物在中枢抑制剂量和致死剂量之间的差距最大。4. 亲脂性(辛醇 - 水分配系数)并未为这八种酰脲类化合物的效力提供统一的关系。然而,在每组两个化合物子集中,相对效力和亲脂性之间发现了线性关系。

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