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

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.