Abstract
Human chymase produces not only angiotensin II but also endothelin(ET)-1(1-31). We previously reported that ET-1(1-31) had several biological activities in vascular smooth muscle cells. In this study, we investigated the vasoconstrictor effect of ET-1(1-31) on the renal resistance vessels using in vitro microperfused rabbit afferent and efferent arterioles. ET-1(1-31) decreased the lumen diameter of the afferent and efferent arterioles dose-dependently. ET-1(1-31)-induced afferent arteriolar vasoconstriction was not affected by phosphoramidon, an ET converting enzyme inhibitor. ET-1(1-31)-induced renal arteriolar vasoconstriction was inhibited by BQ123, an ETA receptor inhibitor, but not by BQ788, an ETB receptor inhibitor. These results suggest that ET-1(1-31)-induced renal arteriolar vasoconstriction may be mediated by ETA-like receptors.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Arterioles / drug effects*
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Arterioles / ultrastructure
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Aspartic Acid Endopeptidases / antagonists & inhibitors
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Dose-Response Relationship, Drug
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Endothelin-1 / analogs & derivatives
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Endothelin-1 / chemical synthesis
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Endothelin-1 / pharmacology*
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Endothelin-Converting Enzymes
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Enzyme Inhibitors / pharmacology
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Glycopeptides / pharmacology
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Humans
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Kidney / blood supply*
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Male
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Metalloendopeptidases
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Muscle, Smooth, Vascular / drug effects*
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Oligopeptides / pharmacology
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Peptide Fragments / chemical synthesis
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Peptide Fragments / pharmacology*
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Peptides, Cyclic / pharmacology
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Perfusion
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Piperidines / pharmacology
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Rabbits
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Receptor, Endothelin A
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Receptors, Endothelin / drug effects
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Receptors, Endothelin / physiology
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Vascular Resistance / drug effects
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Vasoconstriction / drug effects*
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Vasoconstrictor Agents / pharmacology*
Substances
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Endothelin-1
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Enzyme Inhibitors
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Glycopeptides
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Oligopeptides
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Peptide Fragments
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Peptides, Cyclic
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Piperidines
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Receptor, Endothelin A
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Receptors, Endothelin
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Vasoconstrictor Agents
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endothelin-1 (1-31)
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BQ 788
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Aspartic Acid Endopeptidases
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Metalloendopeptidases
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Endothelin-Converting Enzymes
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cyclo(Trp-Asp-Pro-Val-Leu)
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phosphoramidon