Comparison of Biological Effects of N-Alkylated Congeners of β-Phenylethylamine Derived from 2-Aminotetralin, 2-Aminoindan, and 6-Aminobenzocycloheptene

Article abstract of DOI:10.1021/jm00181a009

Three series of bicyclic, semirigid congeners of β-phenethylamine have been prepared for evaluation of the effect of ring size (and of concomitant conformational variation) on biological activity in a variety of assays for adrenergic and dopaminergic actions.Pharmacologic activity was associated with 2-aminotetralin and 2-aminoindan derivatives, but was not found with 6-aminobenzocycloheptene derivatives.Noteworthy is the ability of several aminotetralins and aminoindans to increase the hot-plate reaction time without eliciting dopaminergic effects.This action was not blocked by pretreatment with naloxone.