Tissue distribution studies of [18F]haloperidol, [18F]-beta-(4-fluorobenzoyl)propionic acid, and [82Br]bromperidol by external scintigraphy.

Journal Article (Journal Article)

Tissue distribution studies of [18F]haloperidol and [82Br]bromperidol, two potent neuroleptic drugs, were performed in rats by serial sacrifice. The usefulness of external scintigraphy in obtaining tissue distribution data in large animals is demonstrated by the tissue distribution of [18F]haloperidol in rhesus monkeys. Both serial sacrifice and external scintigraphic studies demonstrated that uptake of the two drugs after intravenous administration into their target organ, the brain, was very fast and that the ratio of brain to blood levels was high throughout the 2-hr observation. Bromperidol appeared to reach peak brain levels faster than its chloro analog, haloperidol. Both bromperidol and haloperidol concentrated overwhelmingly in the rat lung. Haloperidol also showed a high affinity for the monkey lung. The disposition pattern in rats of [18F]-beta-(4-fluorobenzoyl)propionic acid, an apparent intermediate in butyrophenone metabolism, was entirely different from that of the parent drugs. This metabolite did not concentrate in the rat brain.

Full Text

Duke Authors

Cited Authors

  • Digenis, GA; Vincent, SH; Kook, CS; Reiman, RE; Russ, GA; Tilbury, RS

Published Date

  • September 1, 1981

Published In

Volume / Issue

  • 70 / 9

Start / End Page

  • 985 - 989

PubMed ID

  • 6101168

International Standard Serial Number (ISSN)

  • 0022-3549

Digital Object Identifier (DOI)

  • 10.1002/jps.2600700904


  • eng

Conference Location

  • United States