[35s]标记的生长促进剂:双胍[(n1 -ΜΕΤΗΥΙl -Ν2 -ΜΕΤΗΥΙlsulΡΗΟΝΥl)胍基乙基]二硫化物的代谢和处置研究

V. Facchini, M. Jones, Geoffrey E. Smith
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引用次数: 0

摘要

研究了[35S]标记的生长促进剂[n1 -甲基- n2 -甲基磺基)胍基乙基]二硫化合物在大鼠口服后的配置和代谢。在给药后1小时,血浆和大多数取样组织的最大浓度证明了药物衍生产品的快速和显著吸收,并且广泛的肾脏清除率,在12小时内尿液中排出了超过62%的剂量。尿液分析显示,所给化合物已完全代谢为五种代谢物,其中两种主要产物已被表征。代谢途径涉及二硫键的还原裂解,随后的s甲基化和硫氧化似乎参与了化合物的生物转化。
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METABOLISM AND DISPOSITION STUDIES WITH A [35S]-LABELLED GROWTH PROMOTOR: BIS[( N1-ΜΕΤΗΥΙL-Ν2-ΜΕΤΗΥΙLSULΡΗΟΝΥL) GUANIDINYL ETHYL] DISULPHIDE
The disposition and metabolism of the [35S]-labelled growth promotor bis[N1-methyl- N2-methylsulphonyl) guanidinylethyl] disulphide was studied in the rat following oral administration. There was rapid and significant absorption of drug-derived products evidenced by maximum concentrations for plasma and the majority of sampled tissues at 1 h post dose, and extensive renal clearance, with greater than 62% of dose voided in urine in 12 h. Analysis of urine revealed that the administered compound had been completely metabolised to five metabolites of which the two major products have been characterised. A metabolic pathway involving reductive cleavage of the disulphide bond, followed by S-methylation and sulphoxidation would appear to be involved in the biotransformation of the compound.
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