Heart Failure Reviews

, 13:311

Aminopeptidase A inhibitors as centrally acting antihypertensive agents

  • Laurence Bodineau
  • Alain Frugière
  • Yannick Marc
  • Cédric Claperon
  • Catherine Llorens-Cortes
Article

DOI: 10.1007/s10741-007-9077-3

Cite this article as:
Bodineau, L., Frugière, A., Marc, Y. et al. Heart Fail Rev (2008) 13: 311. doi:10.1007/s10741-007-9077-3

Abstract

Among the main bioactive peptides of the brain renin–angiotensin system, angiotensin (Ang) II and AngIII exhibit the same affinity for the type 1 and type 2 Ang receptors. Both peptides, injected intracerebroventricularly, cause similar increase in blood pressure (BP). Because AngII is converted in vivo to AngIII, the identity of the true effector is unknown. This review summarized recent insights into the predominant role of brain AngIII in the central control of BP underlining the fact that brain aminopeptidase A (APA), the enzyme forming central AngIII, could constitute a putative central therapeutic target for the treatment of hypertension. This led to the development of potent, systematically active APA inhibitors, such as RB150, as a prototype of a new class of centrally acting antihypertensive agents for the treatment of certain forms of hypertension.

Keywords

Angiotensin IIIAminopeptidase A inhibitorArterial blood pressureBrain renin–angiotensin systemHypertensionZinc metalloproteases

Copyright information

© Springer Science+Business Media, LLC 2007

Authors and Affiliations

  • Laurence Bodineau
    • 1
    • 2
    • 3
  • Alain Frugière
    • 1
    • 2
    • 3
  • Yannick Marc
    • 1
    • 2
    • 3
  • Cédric Claperon
    • 1
    • 2
    • 3
  • Catherine Llorens-Cortes
    • 1
    • 2
    • 3
  1. 1.U 691InsermParis Cedex 05France
  2. 2.U 691Collège de FranceParis Cedex 05France
  3. 3.U 691Université Pierre et Marie Curie-Paris 6Paris Cedex 05France