Imaging the 5-HT(1A) receptors with PET: WAY-100635 and analogues

Nucl Med Biol. 2000 Jul;27(5):463-6. doi: 10.1016/s0969-8051(00)00112-8.

Abstract

This paper summarizes our work on WAY-100635 and analogues, labeled either with carbon-11 or fluorine-18, as potential radioligands for the 5-hydroxytryptamine(1A) (5-HT(1A)) neuroreceptors. Other facets of our work include: (1) human studies with [O-methyl-(11)C]WAY-100634, the major radioactive metabolite of [O-methyl-(11)C]WAY-100635, and with [(11)C]CPC 222; (2) use of a human liver metabolism model to screen in vitro potential metabolic problems in humans; (3) modification of the "dry method" to prepare [carbonyl-(11)C]WAY-100635; and (4) validation studies in humans with [carbonyl-(11)C]WAY-100635.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Liver / metabolism
  • Piperazines / metabolism*
  • Piperidines / metabolism
  • Pyridines / metabolism*
  • Receptors, Serotonin / analysis*
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists / metabolism*
  • Tomography, Emission-Computed*

Substances

  • CPC 222
  • Piperazines
  • Piperidines
  • Pyridines
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide