Inhibition of synaptosomal accumulation of l-norepinephrine. I: N-arylalkyl and N-aryloxyalkyl dl-amphetamines and related compounds.

The ability of a group of systematically modified amphetamines to inhibit the accumulation of l-norepinephrine by nonstriatal synaptosomes was investigated. N-Substitution by the proper bulky hydrophobic groups can be well tolerated. Structure-activity relationships generate a qualitative picture of the inhibitor-carrier interaction site.