Clear progress has been made in our understanding of the role of ACE2 in the brain. The many beneficial effects of this carboxypeptidase on the central regulation of cardiovascular function could be independent or at least partially result from the modification of angiotensin peptides. The potential therapeutic implications of ACE2 suggest that it could be used to treat hypertension, heart failure, and other cardiovascular diseases. Increasing brain ACE2 by stimulating endogenous ACE2 activity and/or expression, or administration of exogenous ACE2 may provide beneficial effects in some pathologic conditions and this could be a new strategy for future development of novel therapeutic agents. Further understanding of its role in the central nervous system is needed because it would lead to the exploration of novel therapies for neurogenic hypertension and other cardiovascular as well as neurologic diseases.