PARABOLIC DEPENDENCE OF DRUG ACTION UPON LIPOPHILIC CHARACTER AS REVEALED BY A STUDY OF HYPNOTICS
PARABOLIC DEPENDENCE OF DRUG ACTION UPON LIPOPHILIC CHARACTER AS REVEALED BY A STUDY OF HYPNOTICS
复制标题
DOI:
10.1021/jm00307a001
复制
发表时间:
1968-01-01
影响因子:
7.3
通讯作者:
BENTLEY, D
中科院分区:
文献类型:
--
作者:
HANSCH, C;STEWARD, AR;BENTLEY, D
The hypnotic activity of groups of barbiturates depend almost entirely on their relative lipophilic character as defined by their octanol-water partition coefficients. Ideal lipophilic character is defined for each set by the constant log P0. This constant for the barbiturates is about 2. Many other sets of hypnotics structurally unrelated to the barbiturates also have log P0. values near 2. The rate of metabolism of barbiturates is linearly related to their partition coefficients. Certain guidelines are suggested for the design of new central nervous system depressants.