PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635

Richard E. Carson, Lixin Lang, Hiroshi Watabe, Margaret G. Der, H. Richard Adams, Elaine Jagoda, Peter Herscovitch, William C. Eckelman

Research output: Contribution to journalArticlepeer-review

62 Citations (Scopus)

Abstract

We synthesized [18F]FCWAY, an analog of [carbonyl-11C]WAY-100635 ([11C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2- (pyridinyl))cyclohexanecarboxamide), by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [18F]FC and [18F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [18F]FCWAY has very similar kinetic characteristics to [11C]WAY-100635.

Original languageEnglish
Pages (from-to)493-497
Number of pages5
JournalNuclear Medicine and Biology
Volume27
Issue number5
DOIs
Publication statusPublished - 2000 Jul
Externally publishedYes

Keywords

  • 5-HT receptors
  • FCWAY
  • Modeling
  • Volume of distribution

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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