Tritium labelled (±)‐7‐chloro‐8‐hydroxy‐3‐methyl‐1‐phenyl‐2,3,4,5‐tetrahydro‐1H‐3‐benzazepine (SCH23390)

Steven D. Wyrick, Richard Mailman

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

The antipsychotic drug, SCH23390, once thought to be the first selective D1 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 D1 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.

Original languageEnglish (US)
Pages (from-to)189-195
Number of pages7
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume22
Issue number2
DOIs
StatePublished - Jan 1 1985

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Tritium
Antipsychotic Agents
Benzazepines
Dopamine D1 Receptors
Dopamine Antagonists
Palladium
Gases
SCH 23390

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

Cite this

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T1 - Tritium labelled (±)‐7‐chloro‐8‐hydroxy‐3‐methyl‐1‐phenyl‐2,3,4,5‐tetrahydro‐1H‐3‐benzazepine (SCH23390)

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AU - Mailman, Richard

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AB - The antipsychotic drug, SCH23390, once thought to be the first selective D1 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 D1 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.

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