Support for 5-HT2C receptor functional selectivity in vivo utilizing structurally diverse, selective 5-HT2C receptor ligands and the 2,5-dimethoxy-4-iodoamphetamine elicited head-twitch response model

► 5-HT2C agonists and antagonists attenuate the HTR in C57Bl/6 mice elicited by DOI. ► 5-HT2C agonists and antagonists differentially alter locomotion after DOI treatment. ► 5-HT2A and 2C ligand selectivity is conserved from human to mouse receptors. ► 5-HT2C agonists diminish the functional efficacy of DOI at mouse 5-HT2C receptors. ► 5-HT2C agonists may display functional selectivity for 5-HT2C receptors in vivo.