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

1994; Wiley; Volume: 9; Issue: 1 Linguagem: Inglês

10.1002/hup.470090103

1099-1077

Carl‐Gunnar Swahn, Christer Halldin, Lars Farde, Göran Sedvall,

Schizophrenia research and treatment

Abstract [ 11 C]SCH 23390 is a radioligand used for PET determination of the D 1 ‐dopamine receptor in the living human brain. An HPLC procedure was developed for analysis of [ 11 C]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 [ 11 C]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.