2-Iodo-LSD, a radiolabeled analogue of 2-iodo-LSD, has been used as a radioligand for serotonin 5-HT2 receptors. In addition, radiolabeled derivatives of 2-iodo-LSD, such as 1-methyl-2-iodo-LSD and 1-ethyl-2-iodo-LSD, have been developed for use as presumably non-hallucinogenic agents in imaging of serotonin receptors.