Mackie C E, English H E, Lelievre E, Gordon B H, Génissel P, Robinson B V
Department of Pharmacology, UMDS, Medical School, St., Thomas Hospital, London, UK.
J Pharm Biomed Anal. 1997 Apr;15(7):917-28. doi: 10.1016/s0731-7085(96)01924-3.
S9788, 6-[4-(2,2-di-(fluorophenyl)-ethylaminol-1-piperdinyl]-N,N'-d i-2-propenyl-1, 3,5-triazine- 2, 4-diamine, is a novel compound designed to reverse tumour multidrug resistance associated with cancer chemotherapy. A specific and sensitive radioimmunoassay has been developed for the analysis of S9788 in serum samples and adapted for samples obtained by microdialysis. The limit of quantitation is 0.2 ng ml-1 in perfusion medium and there is no cross reactivity of the antibody with known metabolites of the parent compound or with certain cytotoxic compounds likely to be coadministered with S9788. Maximum probe recovery during microdialysis was 66% at a flow of 1 microliter min-1, using Ringer/BSA (70 mg ml-1) as the perfusion medium. The assay has sufficient sensitivity, precision, accuracy and specificity for the analysis of rat and human serum and microdialysis perfusate samples. The assay has been successfully applied to the determination of S9788 in rat plasma (total concentration) and the microdialysate of the same samples.
S9788，即6-[4-(2,2-二(氟苯基)乙氨基]-1-哌啶基]-N,N'-二-2-丙烯基-1,3,5-三嗪-2,4-二胺，是一种旨在逆转与癌症化疗相关的肿瘤多药耐药性的新型化合物。已开发出一种特异性和灵敏的放射免疫分析法，用于分析血清样本中的S9788，并适用于通过微透析获得的样本。在灌注介质中定量限为0.2 ng/ml，该抗体与母体化合物的已知代谢物或可能与S9788共同给药的某些细胞毒性化合物无交叉反应。使用林格氏液/牛血清白蛋白（70 mg/ml）作为灌注介质，在流速为1微升/分钟时，微透析过程中的最大探针回收率为66%。该分析法对大鼠和人血清及微透析灌注液样本的分析具有足够的灵敏度、精密度、准确度和特异性。该分析法已成功应用于大鼠血浆（总浓度）及同一样本微透析液中S9788的测定。
