Metabolism of the PET ligand [11C]SCH 23390. Identification of two radiolabelled metabolites with HPLC

Metabolism of the PET ligand [11C]SCH 23390. Identification of two radiolabelled metabolites with HPLC
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PET 配体 [11C]SCH 23390 的代谢。用 HPLC 鉴定两种放射性标记代谢物

DOI:
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发表时间:
1994
期刊:
影响因子:
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通讯作者:
G. Sedvall
G. Sedvall
中科院分区:
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文献类型:
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作者:
C. Swahn;C. Halldin;L. Farde;G. Sedvall

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[11C]SCH 23390是一种放射性配基,用于对活体人脑中的D_1-多巴胺受体进行正电子发射计算机断层扫描。建立了人血浆中[11C]SCH-23390及其放射性标记代谢物的高效液相色谱分析方法,并与正电子发射计算机断层扫描研究相结合。静脉注射后。[11C]SCH 23390在血浆中迅速下降,约50%的放射性配基在4分钟后保持不变,约10%在40分钟后保持不变。下降遵循了两个指数的时间进程。合成并表征了SCH 23390的两个可能的代谢物--O-硫酸盐和O-葡萄糖醛酸苷。血浆中的两种放射性物质与这些参考化合物共同迁移。
[11C]SCH 23390 is a radioligand used for PET determination of the D1‐dopamine receptor in the living human brain. An HPLC procedure was developed for analysis of [11C]SCH 23390 and its radiolabelled metabolites in plasma after injection of the radioligand into human subjects in realtion to PET studies. After i.v. injection [11C]SCH 23390 rapidly declined from plasma, about 50 per cent of the radioligand remaining unchanged after 4 min and about 10 per cent after 40 min. The decline followed a biexponential time course. Two of the probable metabolites, the O‐sulphate and the O‐glucuronide of SCH 23390 were synthesized and characterized. Two radioactive substances in plasma co‐migrated with these reference compounds.
肺血管内皮细胞对内源性和外源性物质的代谢。
DOI: 10.1016/0163-7258(89)90037-5
发表时间: 1989
影响因子: 13.5
作者:
Ryan,US;Grantham,CJ
通讯作者: Grantham,CJ