[3H]-DOB(4-bromo-2,5-dimethoxyphenylisopropylamine) and [3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor.
Molecular Pharmacology November 1, 1990 T. Branchek, N. Adham, M. Macchi et al. 77 citations
A single human 5-HT2 receptor gene, when expressed in monkey kidney or mouse fibroblast cells, produces both [3H]DOB and [3H]ketanserin binding sites that match those in brain tissue. Adding a GTP analog converts two-site agonist binding to a single low-affinity state and reduces high-affinity DOB sites by 50% without changing their affinity. These results demonstrate that DOB and ketanserin bind to different conformations of the same receptor protein, supporting the classical two-state model of agonist and antagonist affinity states over the hypothesis of a separate 5-HT2A receptor subtype.