Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters

Guangrong Zheng, David B. Horton, Agripina G. Deaciuc, Linda P. Dwoskin, Peter A. Crooks

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

A series of des-keto lobeline analogs has been synthesized and evaluated for their ability to inhibit the dopamine transporter (DAT) and serotonin transporter (SERT) function and for their affinity for the synaptic vesicle monoamine transporter (VMAT2), as well as for α4β2* and α7* neuronal nicotinic acetylcholine receptors (nAChRs). The enantiomers 8R-hydroxylobel-9-ene (3a) and 10S-hydroxylobel-7-ene (3c) exhibited high potency and selectivity at SERT and DAT, respectively.

Original languageEnglish
Pages (from-to)5018-5021
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number19
DOIs
StatePublished - Oct 1 2006

Bibliographical note

Funding Information:
This research was supported by NIH Grant DA 13519.

Keywords

  • Dopamine transporter
  • Lobeline
  • Serotonin transporter
  • Vesicular monoamine transporter

ASJC Scopus subject areas

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

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