Journal of Medicinal Chemistry 1980-07-01

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

J G Cannon, J A Perez, J P Pease, J P Long, J R Flynn, D B Rusterholz, S E Dryer

Index: J. Med. Chem. 23(7) , 745-9, (1980)

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Abstract

Three series of bicyclic, semirigid congeners of beta-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 derivateves, 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.