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单次口服给药后3H-8-甲氧补骨脂素及其代谢产物在大鼠器官中的分布。

Distribution of 3H-8-MOP and its metabolites in rat organs after a single oral administration.

作者信息

Wulf H C, Andreasen M P

出版信息

J Invest Dermatol. 1981 Apr;76(4):252-8. doi: 10.1111/1523-1747.ep12526090.

Abstract

Concentrations of 3H-8-methoxypsoralen (MOP), its lipid- and water soluble metabolites and tritiated water have been measured in rat serum, liver, kidney, and skin, using liquid scintillation, thin-layer chromatography and other techniques. Radioactivity in whole blood, plasma, ovary, adrenals, and pancreas has also been measured. The radioactivity has been measured up to 1 week after medication, whilst 3H-8-MOP and metabolite concentrations have been measured from 10 min to 24 hr after medication with a single dose of 1 mg 3H-8-MOP in solution/kg bodyweight. Maximum 8-MOP concentrations were seen from 10 to 30 min after dosing. The concentrations in microgram/kg 10 min, 2 hr, and 24 hr after medication were as follows: serum--686, 57, 2.1; liver--489, 45, 3.3; kidney--1708, 139, 4.3; and skin--55, 16, 3.8. The concentrations of water soluble metabolites were very high in the liver and only slightly lower in the kidney. The concentrations of these metabolites might accumulate after doses repeated 4 times a week. 3H-8-MOP and its other metabolites would not show similar accumulation. Most of the radioactivity present after 1 week is due to tritiated water.

摘要

利用液体闪烁、薄层色谱法及其他技术,测定了大鼠血清、肝脏、肾脏和皮肤中3H-8-甲氧基补骨脂素(MOP)、其脂溶性和水溶性代谢产物以及氚化水的浓度。还测定了全血、血浆、卵巢、肾上腺和胰腺中的放射性。给药后长达1周都对放射性进行了测定,而在以1毫克3H-8-MOP溶液/千克体重的单剂量给药后10分钟至24小时内测定了3H-8-MOP和代谢产物的浓度。给药后10至30分钟出现8-MOP的最大浓度。给药后10分钟、2小时和24小时时以微克/千克计的浓度如下:血清——686、57、2.1;肝脏——489、45、3.3;肾脏——1708、139、4.3;皮肤——55、16、3.8。水溶性代谢产物的浓度在肝脏中非常高,在肾脏中仅略低。这些代谢产物的浓度在每周重复给药4次后可能会累积。3H-8-MOP及其其他代谢产物不会表现出类似的累积。1周后存在的大部分放射性归因于氚化水。

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