A study has been made of the relationship between the structure of phenylalkylamines and potential correlates of their psychotomimetic activity. Optimum activity is associated with (a) an isopropylamine side chain, with a R-(-) configuration at the carbon atom a to the amino group, and (b) 2,5-dimethoxy substitution, together with an alkyl or halo group at position 4 that is probably limited in bulk to n-propyl or bromo. The activity of compounds in producing hyperthermia in rabbits provides good quantitative correlation with reported psychotomimetic activitiesin man.
