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Tritium labelled (±)‐7‐chloro‐8‐hydroxy‐3‐methyl‐1‐phenyl‐2,3,4,5‐tetrahydro‐1 H ‐3‐benzazepine (SCH23390)
Author(s) -
Wyrick Steven D.,
Mailman Richard B.
Publication year - 1985
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580220212
Subject(s) - chemistry , benzazepine , tritium , stereochemistry , dopamine , antagonist , d 1 , dopamine antagonist , medicinal chemistry , receptor , biochemistry , medicine , physics , nuclear physics
The antipsychotic drug, SCH23390, once thought to be the first selective D 1 dopamine antagonist, is now believed to possibly produce its profound antidopaminergic and antipsychotic effects via molecular sites that involve recognition characteristics similar to, or are a subpopulation of the D 1 dopamine receptors. Tritium labelled SCH23390 has been prepared in our laboratory by palladium catalyezed reductive aryl debromination of a brominated precursor with carrier free tritium gas in THF. The product is labelled in the 9‐position of the benzazepine ring and a specific activity of 5.6 Ci/mmole was obtained.