Psychedelic 5-HT2A receptor agonists are emerging as rapid acting antidepressants. GM-2505, is a novel 5-HT2A/5-HT2C receptor agonist with 5-HT releasing activity. The PK/PD relationships for 5-HT2A receptor occupancy and changes in quantitative EEG were overlaid with efficacy in a rat model for antidepressant activity.