Uses
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages -arrestins while blocking G-protein signaling[1]. TRV120027inducesacutecatecholaminesecretionthrough cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for theacute decompensated heart failure (ADHF) treatment[2].
References
[1] Boerrigter G, et al. TRV120027, a novel β-arrestin biased ligand at the angiotensin II type I receptor, unloads the heart and maintains renal function when added to furosemide in experimental heart failure.Circ Heart Fail. 2012 Sep 1;5(5):627-34. Epub 2012 Aug 13. DOI:
10.1161/CIRCHEARTFAILURE.112.969220[2] Liu CH, et al. Arrestin-biasedAT1RagonisminducesacutecatecholaminesecretionthroughTRPC3coupling.Nat Commun.2017 Feb 9;8:14335. DOI:
10.1038/ncomms14335
