11C-radiolabeling of hallucinogenic psilocin, a potential radioligand for studying the role of serotonin receptors in psychotic symptom formation

Autor: Pius A. Schubiger, J. Patt, H.-F. Beer, Franz X. Vollenweider, Simon M. Ametamey, Daniel Bourquin, Felix Hasler
Rok vydání: 1998
Předmět:
Zdroj: Journal of Labelled Compounds and Radiopharmaceuticals. 41:585-594
ISSN: 0362-4803
DOI: 10.1002/(sici)1099-1344(199807)41:7<585::aid-jlcr115>3.0.co;2-u
Popis: The desmethyl compound, 4-hydroxy-N-methyltryptamine (4), was synthesized via a four-step reaction sequence starting from 4-benzyloxyindole (1). Psilocin (4-hydroxy-N,N-dimethyltryptamine), an indole hallucinogen, was labeled by N-monomethylation of the side chain using the classical methylating agent [ 11 C]CH 3 I in 20±5% (decay corrected from [ 11 C]CH 3 I) radiochemical yield. Specific activities obtained ranged from 900-2300Ci/mmol at EOS (end of synthesis). The radiosynthesis, semi-preparative HPLC and formulation were completed in an average time of 45 minutes.
Databáze: OpenAIRE