Effect of molecular size on 5-hydroxytryptamine receptor agonist activity of 8-hydroxy-2-(alkylamino)tetralins and adrenal cortical 11 beta-hydroxylase inhibition potency of metyrapone analogues.

A quantitative structure-activity relationship has been established between 5-hydroxytryptamine receptor agonist activity of 8-hydroxy-2-(alkylamino)tetralins (I) and adrenal cortical 11 beta-hydroxylase inhibition potency of metyrapone derivatives (II) and the van der Waals volume, Vw, of the compounds. In both examples the size of the molecules has been significantly correlated with the inhibitory potencies of the compounds.