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- W2113017327 abstract "Abstract. The present study examined whether metabolism of the putative angiotensin-(1-7) receptor agonist and antagonist [angiotensin-(1-7) and D-alanine 7 angiotensin-(1-7), respectively] altered their ability to interact with angiotensin AT 1 , AT 2 , and AT 4 receptor subtypes. Both angiotensin-(1-7) and D-alanine 7 angiotensin-(1-7) competed with low affinity for 125 I-sarcosine 1 , isoleucine 8 angiotensin II binding to AT 1 and AT 2 receptors in rat liver and adrenal medulla membranes, respectively, and competed with low affinity for 125 I-angiotensin IV binding to AT 4 receptors in bovine kidney epithelial cell membranes. In vitro renal metabolism of the angiotensin-(1-7) receptor ligands (incubating peptides with rat cortical tissue homogenates) had minimal influence on low-affinity binding to AT 1 and AT 2 receptors, yet caused a significant and dramatic shift toward high-affinity binding for AT 4 receptors. Low-affinity angiotensin II binding to the AT 4 receptor was also shifted toward high-affinity binding following renal metabolism of the peptide. Conversely, angiotensins with high affinity for the AT 4 receptor ( e.g. , angiotensin IV) were shifted toward low-affinity binding states following peptide metabolism. Incubation of 125 I-angiotensin-(1-7) with rat cortical tissue generated the high-affinity AT 4 receptor ligand 125 I-angiotensin-(3-7), whereas the renal metabolism of 125 I-angiotensin II generated both 125 I-angiotensin-(3-7) and 125 I-angiotensin IV. These results reveal that renal metabolism of angiotensin-(1-7) receptor ligands and angiotensin II yields products that have high affinity for the AT 4 receptor and could potentially contribute to the biologic actions of the parent peptide in the kidney." @default.
- W2113017327 created "2016-06-24" @default.
- W2113017327 creator A5075187095 @default.
- W2113017327 date "2000-08-01" @default.
- W2113017327 modified "2023-10-03" @default.
- W2113017327 title "Metabolism Alters the Selectivity of Angiotensin-(1-7) Receptor Ligands for Angiotensin Receptors" @default.
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- W2113017327 doi "https://doi.org/10.1681/asn.v1181377" @default.
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