Quantitative structure-activity relationship of antidepressant agents. Derivatives of cis- and trans-1-amino-4-aryltetralin.

The quantitative structure-activity relationship (QSAR) was studied for monoamine uptake inhibition of cis- and trans-1-amino-4-aryltetralins. The physicochemical parameters, electronic (sigma), hydrophobic (pi), and molar refraction (MR) were found to be significantly correlated with 5-hydroxytryptamine (5-HT) uptake inhibition activity in corpus striatum of rat brain in both series of compounds. The norepinephrine (NE) uptake inhibition activity in hypothalamus and dopamine (DA) uptake inhibition activity in corpus striatum, however, yielded poor correlations in either set of compounds. However, the selectivity ratios, - log [IC50 (DA)/IC50 (5-HT)] and - log [IC50 (NE)/IC50 (5-HT)] described statistically sound correlations with properly chosen physicochemical parameters in cis- and trans-1-amino-4-aryltetralins.