Endogenous indoles as novel polyamine site ligands at the N-methyl-D-aspartate receptor complex

David R. Worthen, D. Alex Gibson, Dennis T. Rogers, Aimee K. Bence, May Fu, John M. Littleton, Peter A. Crooks

Research output: Contribution to journalArticlepeer-review

13 Scopus citations


High-throughput ligand displacement screens of a series of endogenous indoles revealed that tryptamine, serotonin and 5-methoxytryptamine readily displace [3H]spermidine and [3H]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [3H]MK-801 binding, suggest that certain endogenous indoles may act as ligands to one or more polyamine binding sites in the brain, including those on the N-methyl-D-aspartate receptor complex.

Original languageEnglish
Pages (from-to)343-346
Number of pages4
JournalBrain Research
Issue number2
StatePublished - Feb 2 2001

Bibliographical note

Funding Information:
This investigation was supported by National Institutes of Health, National Research Service award DA07304 from the National Institute on Drug Abuse, American Foundation for Pharmaceutical Education Fellowships (A.K.B. and D.R.W.) and National Institute of Alcohol Abuse and Alcoholism Grant AA12600.


  • CNS
  • Endogenous indole
  • N-Methyl-D-aspartate
  • Neuroprotection
  • Polyamine recognition domain

ASJC Scopus subject areas

  • Neuroscience (all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology


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