Lobelane analogues as novel ligands for the vesicular monoamine transporter-2

Guangrong Zheng, Linda P. Dwoskin, Agripina G. Deaciuc, Jun Zhu, Marlon D. Jones, Peter A. Crooks

Research output: Contribution to journalArticlepeer-review

35 Scopus citations


A series of lobelane analogues has been synthesized and their structure-activity relationships at the vesicular monoamine transporter-2 (VMAT2) have been evaluated. The most potent analogues in this series were the cis-2,6-piperidino analogues, 25b, 27b, 28b, and 30b, with Ki values ranging from 430 to 580 nM.

Original languageEnglish
Pages (from-to)3899-3909
Number of pages11
JournalBioorganic and Medicinal Chemistry
Issue number12
StatePublished - Jun 2 2005

Bibliographical note

Funding Information:
This research was supported by NIH grants DA 00399 and DA 13519. The authors also gratefully acknowledge the generous gift of [ 3 H]DTBZ from Dr. Michael R. Kilbourn (supported by NIH Grant MH 47611). The authors also thank Mr. Robert King of the Environmental Research and Training Laboratory, University of Kentucky for performing the elemental analyses. For purposes of full disclosure, the University of Kentucky holds patents on lobeline and lobeline analogues, which have been licensed by Yaupon Therapeutics Inc. (Lexington, KY). A potential royalty stream to G.Z., L.P.D., M.D.J., and P.A.C. may occur consistent with University of Kentucky policy. Both L.P.D. and P.A.C. are founders of, and have financial interest in Yaupon Therapeutics Inc.


  • Lobeline
  • Methamphetamine
  • Structure-activity relationships
  • Vesicular monoamine transporter

ASJC Scopus subject areas

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


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