Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist

[Pyr(1)]apelin-13 is an endogenous vasodilator and inotrope but is downregulated in pulmonary hypertension and heart failure, making the apelin receptor an attractive therapeutic target. Agonists acting at the same G-protein-coupled receptor can be engineered to stabilize different conformational st...

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Bibliographic Details
Published in:	Hypertension (Dallas, Tex. 1979) Vol. 65; no. 4; p. 834
Main Authors:	Brame, Aimee L, Maguire, Janet J, Yang, Peiran, Dyson, Alex, Torella, Rubben, Cheriyan, Joseph, Singer, Mervyn, Glen, Robert C, Wilkinson, Ian B, Davenport, Anthony P
Format:	Journal Article
Language:	English
Published:	United States 01.04.2015
Subjects:	Animals Antipyretics Apelin Receptors Disease Models, Animal GTP-Binding Proteins - metabolism Humans Hypertension, Pulmonary - drug therapy Hypertension, Pulmonary - metabolism Hypertension, Pulmonary - physiopathology Intercellular Signaling Peptides and Proteins - pharmacology Male Rats Rats, Wistar Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism Research Design Saphenous Vein - drug effects Saphenous Vein - metabolism Saphenous Vein - physiopathology Vasodilation - drug effects pulmonary arterial hypertension [Pyr1]apelin-13 β-arrestin G-protein coupled receptors
ISSN:	1524-4563, 1524-4563
Online Access:	Get more information
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