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Aminopeptidase A inhibitors as centrally acting antihypertensive agents.

Laurence Bodineau 1 Alain Frugière 1 Yannick Marc 1 Cédric Claperon 1 Catherine Llorens-Cortes 1, *
* Corresponding author
1 Neuropeptides centraux et régulations hydrique et cardiovasculaire
UPMC - Université Pierre et Marie Curie - Paris 6, INSERM - Institut National de la Santé et de la Recherche Médicale : U691, CIRB - Centre interdisciplinaire de recherche en biologie
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.
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https://www.hal.inserm.fr/inserm-00422692
Contributor : Catherine Llorens Cortes <>
Submitted on : Thursday, October 8, 2009 - 12:05:15 PM
Last modification on : Wednesday, September 23, 2020 - 4:33:33 AM

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Laurence Bodineau, Alain Frugière, Yannick Marc, Cédric Claperon, Catherine Llorens-Cortes. Aminopeptidase A inhibitors as centrally acting antihypertensive agents.. Heart Failure Reviews, Springer Verlag, 2008, 13 (3), pp.311-9. ⟨10.1007/s10741-007-9077-3⟩. ⟨inserm-00422692⟩

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