Imidazoline-modified benzylimidazolines as h5-HT1D/1B serotonergic ligands

Thomas Prisinzano, Ho Law, Malgorzata Dukat, Abdelmalik Slassi, Neil MaClean, Lidia Demchyshyn, Richard A. Glennon

Research output: Contribution to journalArticlepeer-review

29 Scopus citations


Sumatriptan, a h5-HT1D and h5-HT1B receptor agonist used clinically as a migraine-abortive, produces certain side effects thought to result from its affinity for h5-HT1B receptors. The present investigation extends our work with benzylimidazolines as novel non-tryptamine h5-HT1D/1B ligands. The effect of N-methylation, N-benzylation, ring-aromatization, and variation of the imidazoline ring on affinity both at h5-HT1D and h5-HT1B receptors was examined. Several compounds were identified with good affinity and enhanced (i.e., >100-fold) h5-HT1D versus h5-HT1B selectivity.

Original languageEnglish
Pages (from-to)613-619
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number3
StatePublished - 2001

ASJC Scopus subject areas

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


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