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

[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.

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