The invention provides a method for controlling mammalian body weight using a compound of the formula or a non-toxic pharmaceutically acceptable salt thereof, wherein [E] is an estrogen and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier. Novel compositions for weight control comprising a compound of formula (I) or its salt are also disclosed. A preferred compound for use in the subject method and compositions is an estradiol derivative, namely, 17 .beta.-[(1-methyl-1,4-dihydro-3-pyridinyl)carbonyloxy]estra-1,3,5(10)-trie n-3-ol.

Centrally acting drug species are site-specifically/sustainedly delivered to the brain by administering to a patient in need of such treatment a therapeutically effective amount of the target drug species [D] tethered to a reduced, blood-brain barrier penetrating lipoidal form [D-DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type drug/carrier entity [D-QC].sup.+ prevents elimination thereof from the brain, while elimination from the general circulation is accelerated, and subsequent cleavage of the quaternary carrier/drug species results in sustained delivery of the drug [D] in the brain and facile elimination of the carrier moiety [QC].sup.+.