Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter

Johan Sandell, Meixiang Yu, Patrick Emond, Lucette Garreau, Sylvie Chalon, Kjell Någren, Denis Guilloteau, Christer Halldin

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [3H]5-methyl-6-nitroquipazine was found to have a Kd=51±7 pM. The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography.

Original languageEnglish (US)
Pages (from-to)3611-3613
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number24
DOIs
StatePublished - Dec 2002

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter'. Together they form a unique fingerprint.

Cite this