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4'-(9-吖啶基氨基)-甲磺基间茴香胺(NSC 141549,AMSA)的人体组织分布

Human tissue distribution of 4'-(9-acridinylamino)-methanesulfon-m-anisidide (NSC 141549, AMSA).

作者信息

Stewart D J, Zhengang G, Lu K, Savaraj N, Feun L G, Luna M, Benjamin R S, Keating M J, Loo T L

出版信息

Cancer Chemother Pharmacol. 1984;12(2):116-9. doi: 10.1007/BF00254602.

Abstract

Concentrations of AMSA were determined by HPLC in autopsy tissue samples from five patients who had received the drug antemortem. Relative organ concentrations of AMSA varied from patient to patient; however, concentrations were generally highest in gallbladder, liver, and kidney, while low levels were generally but not invariably found in lung, testicle, muscle, fat, spleen, bladder, pancreas, colon, prostate, and brain. One patient with ventricular fibrillation and seizures had high tissue AMSA concentrations in myocardium, but low concentrations in brain. Another patient with seizures during treatment had high brain concentrations of AMSA. Relative organ concentrations were similar to those found in mice, except that mice have high AMSA concentration in their spleens whereas our patients did not, even when the spleen was infiltrated with leukemic cells. High tissue concentrations of AMSA were still present 2 weeks after treatment. AMSA concentration was lower in a renal oncocytoma (1.1 micrograms/g) than in surrounding kidney (2.4 micrograms/g).

摘要

通过高效液相色谱法(HPLC)测定了五名生前接受过该药物治疗的患者尸检组织样本中氨甲吖啶(AMSA)的浓度。AMSA的相对器官浓度因患者而异;然而,浓度通常在胆囊、肝脏和肾脏中最高,而在肺、睾丸、肌肉、脂肪、脾脏、膀胱、胰腺、结肠、前列腺和大脑中通常较低,但并非总是如此。一名患有心室颤动和癫痫发作的患者心肌中的组织AMSA浓度较高,但大脑中的浓度较低。另一名在治疗期间出现癫痫发作的患者大脑中的AMSA浓度较高。相对器官浓度与在小鼠中发现的浓度相似,只是小鼠脾脏中的AMSA浓度较高,而我们的患者即使脾脏被白血病细胞浸润,其脾脏中的AMSA浓度也不高。治疗两周后,组织中仍存在高浓度的AMSA。肾嗜酸细胞瘤中的AMSA浓度(1.1微克/克)低于周围肾脏中的浓度(2.4微克/克)。

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