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Small-molecule AT2 receptor agonists
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
Univ Florida, Coll Med, Dept Physiol & Funct Genom, Gainesville, FL 32611 USA.;McKnight Brain Inst, Gainesville, FL 32611 USA..
Univ Southern Denmark, Inst Mol Med, Dept Cardiovasc & Renal Res, POB 5230, Odense, Denmark..
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
2018 (English)In: Medicinal research reviews (Print), ISSN 0198-6325, E-ISSN 1098-1128, Vol. 38, no 2, p. 602-624Article, review/survey (Refereed) Published
Abstract [en]

The discovery of the first selective, small-molecule ATR receptor (AT2R) agonist compound 21 (C21) (8) that is now extensively studied in a large variety of in vitro and in vivo models is described. The sulfonylcarbamate derivative 8, encompassing a phenylthiofen scaffold is the drug-like agonist with the highest affinity for the AT2R reported to date (K-i = 0.4 nM). Structure-activity relationships (SAR), regarding different biaryl scaffolds and functional groups attached to these scaffolds and with a particular focus on the impact of various para substituents displacing the methylene imidazole group of 8, are discussed. Furthermore, the consequences of migration of the methylene imidazole group and presumed structural requirements for ligands that are aimed as AT2R agonists (e.g. 8) or AT2R antagonists (e.g. 9), respectively, are briefly addressed. A summary of the pharmacological actions of C21 (8) is also presented.

Place, publisher, year, edition, pages
John Wiley & Sons, 2018. Vol. 38, no 2, p. 602-624
Keywords [en]
angiotensin II, AT2 receptor, peptidomimetics, renin-angiotensin system
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-348314DOI: 10.1002/med.21449ISI: 000425027400006PubMedID: 28609561OAI: oai:DiVA.org:uu-348314DiVA, id: diva2:1201406
Funder
Swedish Research CouncilAvailable from: 2018-04-25 Created: 2018-04-25 Last updated: 2018-04-25Bibliographically approved

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Hallberg, MathiasHallberg, Anders

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