盐酸莱克多巴胺代谢物鉴定大鼠胆汁分泌。

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史密斯DJ,吉丁斯JM Feil VJ,保尔森GD

盐酸莱克多巴胺代谢物鉴定大鼠胆汁分泌。

Xenobiotica。1995年5月,25 (5):511 - 20。

PubMed ID

7571724 (在PubMed

]

文摘

1。前大鼠口服2.85 + / - 0.30毫克[14 c]莱克多巴胺盐酸[(1 r *, 3 r *) (1 r *, 3 s *) 4-hydroxy-alpha - [[[3 - (4-hydroxyphenyl) -甲基丙基)氨基)甲基]([U-14C]大)盐酸]包含1.44 + / - 0.15 microCi放射性排出58 + / - 7%的管理放射性的胆汁在24 h。快速吸收和排泄放射性管理放射性碳的55%被分泌到胆汁在第一次8小时集合。2。放射性物质在大鼠胆汁分泌分区XAD-2柱层析法和反相高效液相色谱法至少七种不同的原油代谢物;代表大约76%的胆汁代谢物的放射性物质被分离和识别四原油代谢物。3所示。大约46%的胆放射性被认定为sulphate-ester,葡萄糖醛酸diconjugate莱克多巴胺。识别是基于1 h - nmr、负离子FAB-ms光谱学。酶和化学水解sulphate-ester co-chromatography紧随其后的水解和合成莱克多巴胺mono-glucuronides产品,建立了网站C-10硫酸化的“苯酚(苯酚与甲醇)和glucuronidation C-10苯酚(苯酚连着methylpropyl胺)的莱克多巴胺。4所示。 A metabolite representing approximately 6% of the biliary radioactivity was identified as a ractopamine mono-sulphate conjugate by using mass spectral and 1H-nmr techniques. Sulphate was conjugated at the C-10' phenol of ractopamine and was not stereospecific. 5. Approximately 25% of the biliary radioactivity was identified as ractopamine mono-glucuronides. The major site of glucuronidation was at the C-10 phenol, but ractopamine glucuronidated at the C'-10 phenol was also present.

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药物

莱克多巴胺