Comparison of biological effects of N-alkylated congeners of .beta.-phenethylamine derived from 2-aminotetralin, 2-aminoindan, and 6-aminobenzocycloheptene

Abstract

Three series of bicyclic, semirigid congeners of .beta.-phenethylamine were prepared for evaluation of the effect of ring size (and of concomitant conformational variation) on biological activity in a variety of assays [exploratory activity, circling behavior and hot-plate analgesia] for adrenergic and dopaminergic actions in mice and rats. Pharmacologic activity was associated with 2-aminotetralin and 2-aminoindan derivatives, but was not found with 6-aminobenzocycloheptene derivatives. Several aminotetralins and aminoindans increase the hot-plate reaction time without eliciting dopaminergic effects. This action was not blocked by pretreatment with naloxone.