Metabolism of N-(3', 5'-Dichlorophenyl) succinimide in Rats and Dogs
Metabolism of N-(3', 5'-Dichlorophenyl) succinimide in Rats and Dogs
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N-(3, 5-二氯苯基)琥珀酰亚胺在大鼠和狗中的代谢
DOI：
10.1271/bbb1961.38.1359
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发表时间：
1974
期刊：
影响因子：
--
通讯作者：
J. Miyamoto
中科院分区：
文献类型：
--
作者：
H. Ohkawa;Y. Hisada;N. Fujiwara;J. Miyamoto
当N-(3‘，5’-二氯苯基)琥珀酰亚胺(DSI)-碳-14C和-苯基-3H分别经口给药时，无论标记部位，大部分剂量都很容易消除。雄性和雌性大鼠的排泄率无差异。给药后24小时，组织器官中未检测到放射性残留物。尿代谢物包括N-(3‘，5’-二氯苯基)琥珀酸(DSA)、N-(3‘，5’-二氯苯基)丙二酸(DMA)、N-(3‘，5’-二氯苯基)-2-羟基琥珀酸(2-OH-DSA)和2-OH-DSA衍生物。在狗身上，大部分给药剂量是在尿液和粪便中等量排泄的。2-羟基-DSA衍生物是尿液的主要代谢物，粪便放射性碳主要来源于完整的DSL。本研究结果表明，DSI是一种可生物降解的化合物，不太可能在动物体内留下任何持久性残留。DSI降解为DSA是由一种芳酰胺酶类型的水解酶介导的，这种水解酶存在于兔肝的微粒体部分中。
When N-(3′,5′-dichlorophenyl)succinimide (DSI)-carbonyI-14C and –pheny-3H were each orally administered to rats, regardless of the label site, most of the dose was readily eliminated. There was no difference in the excretion rate between male and female rats. No radioactive residues were detected in tissues and organs 24 hr after dosing. Urinary metabolites consisted of N-(3′,5′-dichlorophenyl) succinamic acid (DSA), N-(3′,5′-dichlorophe-nyl) malonamic acid (DMA), N-(3′5’-dichlorophenyl)-2-hydroxysuccinamic acid (2-OH-DSA) and 2-OH-DSA derivatives. In dogs, most of the administered dose was excreted in equal amounts in urine and feces. 2-OH-DSA derivatives were main urinary metabolites and most of fecal radiocarbon was due to intact DSL. The results of this study indicate that DSI is a biodegradable compound which is unlikely to leave any persistent residues in animals.The degradation of DSI to DSA was mediated by an arylamidase-type hydrolase, which was present in the microsomal fraction of rabbit liver....