McGraw N P, Callery S C, Castagnoli N
J Med Chem. 1977 Feb;20(2):185-9. doi: 10.1021/jm00212a001.
The stereoselective metabolism [R/S (metabolized) less than 1] of the psychotomimetic amine (R,S)-1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane in 10 000g rabbit liver homogenate supernatant and 100 000g microsomal fractions has been demonstrated with the aid of the chiral reagent (S)-N-pentafluorobenzoylprolyl-1-imidazolide and GLC analyses. In contrast to the enantiomeric discrimination observed with racemic amine, the individual isomers were metabolized at approximately the same rate. This apparent enantiomeric interaction illustrates the fact that racemates should be viewed as unique chemical species with pharmacodynamic and toxicologic profiles potentially different from the individual antipodes.
借助手性试剂（S）-N-五氟苯甲酰基脯氨酰-1-咪唑酯和气相色谱分析，已证实了拟精神病胺（R,S）-1-（2,5-二甲氧基-4-甲基苯基）-2-氨基丙烷在10000g兔肝匀浆上清液和100000g微粒体组分中的立体选择性代谢[R/S（代谢产物）小于1]。与外消旋胺所观察到的对映体识别不同，各个异构体的代谢速率大致相同。这种明显的对映体相互作用说明了一个事实，即外消旋体应被视为具有与单个对映体潜在不同的药效学和毒理学特征的独特化学物质。
