Large scale preparation strategy for labelling of [123I]-SCH 23982, a dopamine D1 receptor binding agent

H F Beer; S Lin; I Novak-Hofer; P Bläuenstein; P A Schubiger

doi:10.1016/0883-2889(92)90242-7

Large scale preparation strategy for labelling of [123I]-SCH 23982, a dopamine D1 receptor binding agent

Int J Rad Appl Instrum A. 1992 Jun;43(6):781-7. doi: 10.1016/0883-2889(92)90242-7.

Authors

H F Beer¹, S Lin, I Novak-Hofer, P Bläuenstein, P A Schubiger

Affiliation

¹ Paul Scherrer Institute, Radiopharmacy Division, Villigen PSI, Switzerland.

PMID: 1319421
DOI: 10.1016/0883-2889(92)90242-7

Abstract

The labelling of the D1 antagonist SCH 23982 with 123I was studied in detail by following the nucleophilic and electrophilic approaches and the reaction conditions were optimized. The product was purified by reversed phase HPLC with a phosphoric acid/EtOH mixture which simply has to be neutralized and diluted before injection. Its binding was tested in vitro with rat striatal membranes proving the high affinity to D1 and very low affinity to D2 receptors.

MeSH terms

Benzazepines / analogs & derivatives*
Dopamine Antagonists*
Iodine Radioisotopes
Isotope Labeling / methods

Substances

8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol
Benzazepines
Dopamine Antagonists
Iodine Radioisotopes