Radioligands for the study of the 5-HT transporter in vivo

Peter Brust, Ursula Scheffel, Zsolt Szabo

Research output: Contribution to journalReview article

Abstract

Loss of 5-HT transporter (SERT) sites has been implicated in various neurodegenerative diseases and users of some amphetamine derivatives such as MDMA. Therefore, the development of suitable radioligands for neuroimaging of the SERT in the human brain is important. A large number of drugs have been labeled with 11C, 18F or 123I over the last ten years in order to achieve such radioligands. Despite these attempts most of the compounds were found unsuitable because of low target-to-nontarget ratios. Some cocaine- derived radioligands allow SERT imaging of the human brain using positron emission tomography (PET) although they have a limited selectivity. Among the various specific 5-HT uptake inhibitors only [123I]iodonitroquipazine for single photon emission computed tomography (SPECT) and [11C](+)McN5652 for PET appear to meet the criteria of a useful radioligand. There is still a need for the development of new radioligands for SERT imaging. Advances in tracer synthetic methodologies may bring further progress in this field.

Original languageEnglish (US)
Pages (from-to)129-145
Number of pages17
JournalIDrugs
Volume2
Issue number2
StatePublished - Feb 19 1999

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ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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