Non-peptide AT2-receptor agonists

U Steckelings; Mats Larhed; Anders Hallberg; Robert Widdop; Emma Jones; Charlotta Wallinder; Pawel Namsolleck; Bjorn Dahlof; Thomas Unger

doi:10.1016/j.coph.2010.11.002

Non-peptide AT2-receptor agonists

U Steckelings, Mats Larhed, Anders Hallberg, Robert Widdop, Emma Jones, Charlotta Wallinder, Pawel Namsolleck, Bjorn Dahlof, Thomas Unger

Pharmacology

Research output: Contribution to journal › Article › Research › peer-review

92 Citations (Scopus)

Abstract

The renin-angiotensin-system harbours two main receptor subtypes binding angiotensin II which are the AT1-receptor and the AT2-receptor. While the AT1-receptor has been a drug target in cardiovascular disease for many years, the AT2-receptor was only a subject of academic interest. This has changed with the design and synthesis of a first non-peptide, orally active AT2-receptor agonist, compound 21 (C21). First data using C21 revealed tissue protective effects and functional improvement after myocardial infarction and in hypertension-induced end organ damage, notably in a blood-pressure independent way. In all of these models, AT2-receptor mediated anti-inflammation seemed an important underlying mechanism. C21 is awaited to enter a phase I clinical study in 2011.

Original language	English
Pages (from-to)	187 - 192
Number of pages	6
Journal	Current Opinion in Pharmacology
Volume	11
Issue number	2
DOIs	https://doi.org/10.1016/j.coph.2010.11.002
Publication status	Published - 2011

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10.1016/j.coph.2010.11.002

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abstract = "The renin-angiotensin-system harbours two main receptor subtypes binding angiotensin II which are the AT1-receptor and the AT2-receptor. While the AT1-receptor has been a drug target in cardiovascular disease for many years, the AT2-receptor was only a subject of academic interest. This has changed with the design and synthesis of a first non-peptide, orally active AT2-receptor agonist, compound 21 (C21). First data using C21 revealed tissue protective effects and functional improvement after myocardial infarction and in hypertension-induced end organ damage, notably in a blood-pressure independent way. In all of these models, AT2-receptor mediated anti-inflammation seemed an important underlying mechanism. C21 is awaited to enter a phase I clinical study in 2011.",

author = "U Steckelings and Mats Larhed and Anders Hallberg and Robert Widdop and Emma Jones and Charlotta Wallinder and Pawel Namsolleck and Bjorn Dahlof and Thomas Unger",

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T1 - Non-peptide AT2-receptor agonists

AU - Steckelings, U

AU - Larhed, Mats

AU - Hallberg, Anders

AU - Widdop, Robert

AU - Jones, Emma

AU - Wallinder, Charlotta

AU - Namsolleck, Pawel

AU - Dahlof, Bjorn

AU - Unger, Thomas

PY - 2011

Y1 - 2011

N2 - The renin-angiotensin-system harbours two main receptor subtypes binding angiotensin II which are the AT1-receptor and the AT2-receptor. While the AT1-receptor has been a drug target in cardiovascular disease for many years, the AT2-receptor was only a subject of academic interest. This has changed with the design and synthesis of a first non-peptide, orally active AT2-receptor agonist, compound 21 (C21). First data using C21 revealed tissue protective effects and functional improvement after myocardial infarction and in hypertension-induced end organ damage, notably in a blood-pressure independent way. In all of these models, AT2-receptor mediated anti-inflammation seemed an important underlying mechanism. C21 is awaited to enter a phase I clinical study in 2011.

AB - The renin-angiotensin-system harbours two main receptor subtypes binding angiotensin II which are the AT1-receptor and the AT2-receptor. While the AT1-receptor has been a drug target in cardiovascular disease for many years, the AT2-receptor was only a subject of academic interest. This has changed with the design and synthesis of a first non-peptide, orally active AT2-receptor agonist, compound 21 (C21). First data using C21 revealed tissue protective effects and functional improvement after myocardial infarction and in hypertension-induced end organ damage, notably in a blood-pressure independent way. In all of these models, AT2-receptor mediated anti-inflammation seemed an important underlying mechanism. C21 is awaited to enter a phase I clinical study in 2011.

UR - http://www.sciencedirect.com/science/article/pii/S147148921000175X

U2 - 10.1016/j.coph.2010.11.002

DO - 10.1016/j.coph.2010.11.002

M3 - Article

SN - 1471-4892

VL - 11

SP - 187

EP - 192

JO - Current Opinion in Pharmacology

JF - Current Opinion in Pharmacology

IS - 2

ER -

Non-peptide AT2-receptor agonists

Abstract

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