Chosson E, Uzan S, Gimenez F, Wainer I W, Farinotti R
Unité de Dosage de Médicaments, Hôpital Pitié Salpetriere, Paris, France.
Chirality. 1993;5(2):71-7. doi: 10.1002/chir.530050206.
Specific ligand markers for the various binding sites of human serum albumin (HSA) have been described in the literature. Some of these markers (medium chain fatty acids, warfarin, digoxin, and bilirubin) were used as mobile phase modifiers. Using a high performance liquid chromatographic (HPLC) column containing HSA as stationary phase, their influence was investigated on the separation in this phase of the enantiomers of three benzodiazepines (temazepam, oxazepam, and lorazepam). Displacement effects were observed with medium chain fatty acids. This influence was proportional to the chain length and to the concentration of acid. Allosteric cooperative effects were noted with digoxin for the three benzodiazepines. Both displacement and cooperative effects were observed with warfarin. Stereoselectivity was decreased for temazepam and oxazepam and increased for lorazepam.
文献中已描述了人血清白蛋白（HSA）各种结合位点的特异性配体标记物。其中一些标记物（中链脂肪酸、华法林、地高辛和胆红素）被用作流动相改性剂。使用以HSA为固定相的高效液相色谱（HPLC）柱，研究了它们对三种苯二氮䓬类药物（替马西泮、奥沙西泮和劳拉西泮）对映体在该相中分离的影响。观察到中链脂肪酸的置换效应。这种影响与链长和酸的浓度成正比。地高辛对三种苯二氮䓬类药物具有变构协同效应。华法林同时观察到置换和协同效应。替马西泮和奥沙西泮的立体选择性降低，而劳拉西泮的立体选择性增加。
