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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Nielsen P, Dalgaard L

Xenobiotica. 1978 Nov;8(11):657-64. doi: 10.3109/00498257809069577.

Urine from goats and pigs after intravenous administration of [14C]trimethoprim contained an unidentified fraction of 'other water-soluble metabolites'. This fraction accounts for 56% of the administered dose in goat urine and 65% in pig urine. 2. A sulphate metabolite comprising the major part of the latter fraction in both goat and pig urine was isolated by gel filtration and paper chromatography and identified by spectroscopic methods as 2,4-diamino-5-(3,4-dimethoxy-5-sulphooxybenzyl)pyrimidine. 3. No hydrolysis of the sulphate metabolite occurred on treatment with aryl sulphatase from (a) Helix pomatia, (b) limpets and (c) Aerobacter aerogenes, while treatment with aryl sulphatase from abalone entrails led to very slow hydrolysis.

静脉注射[14C]甲氧苄啶后，山羊和猪尿液中含有未鉴定的“其他水溶性代谢物”部分。该部分在山羊尿液中占给药剂量的56%，在猪尿液中占65%。2. 通过凝胶过滤和纸色谱法从山羊和猪尿液中分离出构成后一部分主要成分的硫酸盐代谢物，并通过光谱法鉴定为2,4-二氨基-5-(3,4-二甲氧基-5-磺氧基苄基)嘧啶。3. 用(a) 苹果螺、(b) 帽贝和(c) 产气气杆菌的芳基硫酸酯酶处理时，硫酸盐代谢物未发生水解，而用鲍鱼内脏的芳基硫酸酯酶处理则导致非常缓慢的水解。

Nielsen P, Dalgaard L

Xenobiotica. 1978 Nov;8(11):657-64. doi: 10.3109/00498257809069577.

Urine from goats and pigs after intravenous administration of [14C]trimethoprim contained an unidentified fraction of 'other water-soluble metabolites'. This fraction accounts for 56% of the administered dose in goat urine and 65% in pig urine. 2. A sulphate metabolite comprising the major part of the latter fraction in both goat and pig urine was isolated by gel filtration and paper chromatography and identified by spectroscopic methods as 2,4-diamino-5-(3,4-dimethoxy-5-sulphooxybenzyl)pyrimidine. 3. No hydrolysis of the sulphate metabolite occurred on treatment with aryl sulphatase from (a) Helix pomatia, (b) limpets and (c) Aerobacter aerogenes, while treatment with aryl sulphatase from abalone entrails led to very slow hydrolysis.

静脉注射[14C]甲氧苄啶后，山羊和猪尿液中含有未鉴定的“其他水溶性代谢物”部分。该部分在山羊尿液中占给药剂量的56%，在猪尿液中占65%。2. 通过凝胶过滤和纸色谱法从山羊和猪尿液中分离出构成后一部分主要成分的硫酸盐代谢物，并通过光谱法鉴定为2,4-二氨基-5-(3,4-二甲氧基-5-磺氧基苄基)嘧啶。3. 用(a) 苹果螺、(b) 帽贝和(c) 产气气杆菌的芳基硫酸酯酶处理时，硫酸盐代谢物未发生水解，而用鲍鱼内脏的芳基硫酸酯酶处理则导致非常缓慢的水解。