Potent agonist activity of DOB at 5-HT2 receptors in guinea pig trachea

William A. Heller, Jay M. Baraban

Research output: Contribution to journalArticlepeer-review

Abstract

DOB, 4-bromo-2,5-dimethyloxyamphetamine, a potent hallucinogen, displays high affinity for the 5-HT2 receptor in binding assays. Since 5-HT contractile responses in guinea pig trachea are mediated by 5-HT2 receptors, we assessed the activity of DOB and related analogs in this preparation. DOB acts as a partial 5-HT agonist with an EC50=25 nM and is blocked by the potent selective 5-HT2 receptor antagonists ketanserin, pirenperone and LY 53857, as is 5-HT. These findings indicate that DOB may be useful agent in characterizing 5-HT2 receptor responses.

Original languageEnglish (US)
Pages (from-to)115-117
Number of pages3
JournalEuropean Journal of Pharmacology
Volume138
Issue number1
DOIs
StatePublished - Jun 12 1987

Keywords

  • 5-HT receptors
  • DOB
  • Hallucinogens
  • Trachea

ASJC Scopus subject areas

  • Pharmacology

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