The effects of alkyl substituents at the 6-position of cocaine analogues on dopamine transporter binding affinity and dopamine uptake inhibition

Stacey A. Lomenzo, Sari Izenwasser, Jonathan L. Katz, Mark L. Trudell

Research output: Contribution to journalArticle

4 Scopus citations

Abstract

A series of 6-alkyl-3β-benzyl-2-(methoxycarbonylmethyl)tropane analogues were synthesized and evaluated as cocaine binding-site ligands at the dopamine transporter (DAT). The in vitro inhibition of [3H]dopamine and the DAT binding affinity (K(i), [3H]WIN 35,428) were measured in rat caudate putamen tissue. Generally, substitution at the 6-position was found to reduce ligand potency.

Original languageEnglish (US)
Pages (from-to)35-42
Number of pages8
JournalMedicinal Chemistry Research
Volume8
Issue number1-2
StatePublished - Jan 1 1998

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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