Pharmacological Characterization of Aprocitentan, a Dual Endothelin Receptor Antagonist, Alone and in Combination with Blockers of the Renin Angiotensin System, in Two Models of Experimental Hypertension.


Journal

The Journal of pharmacology and experimental therapeutics
ISSN: 1521-0103
Titre abrégé: J Pharmacol Exp Ther
Pays: United States
ID NLM: 0376362

Informations de publication

Date de publication:
03 2019
Historique:
received: 24 09 2018
accepted: 27 12 2018
pubmed: 10 1 2019
medline: 2 11 2019
entrez: 10 1 2019
Statut: ppublish

Résumé

The endothelin (ET) system has emerged as a novel target for hypertension treatment where a medical need persists despite availability of several pharmacological classes, including renin angiotensin system (RAS) blockers. ET receptor antagonism has demonstrated efficacy in preclinical models of hypertension, especially under low-renin conditions and in hypertensive patients. We investigated the pharmacology of aprocitentan (

Identifiants

pubmed: 30622171
pii: jpet.118.253864
doi: 10.1124/jpet.118.253864
doi:

Substances chimiques

Antihypertensive Agents 0
Endothelin Receptor Antagonists 0
Pyrimidines 0
Sulfonamides 0
Desoxycorticosterone Acetate 6E0A168OB8
aprocitentan MZI81HV01P

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

462-473

Informations de copyright

Copyright © 2019 The Author(s).

Auteurs

Frederic Trensz (F)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Céline Bortolamiol (C)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Markus Kramberg (M)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Daniel Wanner (D)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Hakim Hadana (H)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Markus Rey (M)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Daniel S Strasser (DS)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Stéphane Delahaye (S)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Patrick Hess (P)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Enrico Vezzali (E)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Ulrich Mentzel (U)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Joël Ménard (J)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Martine Clozel (M)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland.

Marc Iglarz (M)

Drug Discovery Department, Idorsia Pharmaceuticals Ltd., Allschwil, Switzerland marc.iglarz@idorsia.com.

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Classifications MeSH