Abstract: High density lipoprotein (HDL) levels in serum cholesterol are increased by orally administering phenylethylamine derivatives having the structural formula ##STR1## wherein R.sub.1 is a member selected from the group consisting of --CH(CH.sub.3).sub.2, --C(CH.sub.3).sub.3 and ##STR2## R.sub.2 is a member selected from the group consisting of --OH and --CH.sub.2 OH; and R.sub.3 and R.sub.4, respectively, are members selected from the group consisting of --H and --OH.