3H-DOB (4-bromo-2,5-dimethoxyphenylisopropylamine) labels a guanyl nucleotide-sensitive state of cortical 5-HT2 receptors.
Molecular Pharmacology February 1, 1987 R. A. Lyon, K. Davis, M. Titeler 106 citations
A radiolabeled compound, 3H-DOB, was used to label a subset of serotonin 5-HT2 receptors in rat frontal cortex tissue. It bound with high affinity and saturability, marking a population of receptors that made up only about 5% of the total 5-HT2 receptors labeled by another compound, 3H-ketanserin. Agonists showed 10- to 100-fold higher affinity for the 3H-DOB-labeled sites than for the 3H-ketanserin-labeled sites, while antagonists did not discriminate between the two subsets. Binding was potently inhibited by nonhydrolyzable GTP derivatives but not by ATP derivatives, suggesting these sites are coupled to G proteins.