Renal adenylate cyclase activation by amino acylated vasopressin and oxytocin

Two series of neurohypophysial peptide amino-acylated derivatives were tested for their ability to activate plasma membrane adenylate cyclase prepared from pig or rat kidney. They were firstly [8-lysine]-vasopressin-related derivatives (N a[Glycyl-Cys] 1-[8-Lysine]-vasopressin and N a-[Glycyl-Glycyl...

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Veröffentlicht in:Molecular and cellular endocrinology 1975, Vol.2 (2), p.69-79
Hauptverfasser: Barth, Tomislav, Roy, Christian, Rajerison, Rabary, Jard, Serge
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container_title Molecular and cellular endocrinology
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creator Barth, Tomislav
Roy, Christian
Rajerison, Rabary
Jard, Serge
description Two series of neurohypophysial peptide amino-acylated derivatives were tested for their ability to activate plasma membrane adenylate cyclase prepared from pig or rat kidney. They were firstly [8-lysine]-vasopressin-related derivatives (N a[Glycyl-Cys] 1-[8-Lysine]-vasopressin and N a-[Glycyl-Glycyl-Glycyl-Cys] 1-[8-Lysine]-vasopressin) and secondly oxytocin-related derivatives (N a-[Glycyl-Cys] 1-oxytocin, N a-[Leucyl-Glycyl-Glycyl-Cys] 1-oxytocin, and N a-[Glycyl-Cys] 1-[2-O-methyl tyrosine]-oxytocin). The maximal adenylate cyclase activation induced by these peptides was lower than that induced by their respective parent hormones. After incubation of these analogues with plasma membranes obtained from the renal medulla, no significant release of parent hormones occurred. Good qualitative correlations were observed between relative antidiuretic activities measured in vivo and relative potencies in activating adenylate cyclase. It was concluded that direct action of the peptides tested on the kidney is at least partly responsible for their antidiuretic activity in vivo.
doi_str_mv 10.1016/0303-7207(75)90049-0
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They were firstly [8-lysine]-vasopressin-related derivatives (N a[Glycyl-Cys] 1-[8-Lysine]-vasopressin and N a-[Glycyl-Glycyl-Glycyl-Cys] 1-[8-Lysine]-vasopressin) and secondly oxytocin-related derivatives (N a-[Glycyl-Cys] 1-oxytocin, N a-[Leucyl-Glycyl-Glycyl-Cys] 1-oxytocin, and N a-[Glycyl-Cys] 1-[2-O-methyl tyrosine]-oxytocin). The maximal adenylate cyclase activation induced by these peptides was lower than that induced by their respective parent hormones. After incubation of these analogues with plasma membranes obtained from the renal medulla, no significant release of parent hormones occurred. Good qualitative correlations were observed between relative antidiuretic activities measured in vivo and relative potencies in activating adenylate cyclase. 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They were firstly [8-lysine]-vasopressin-related derivatives (N a[Glycyl-Cys] 1-[8-Lysine]-vasopressin and N a-[Glycyl-Glycyl-Glycyl-Cys] 1-[8-Lysine]-vasopressin) and secondly oxytocin-related derivatives (N a-[Glycyl-Cys] 1-oxytocin, N a-[Leucyl-Glycyl-Glycyl-Cys] 1-oxytocin, and N a-[Glycyl-Cys] 1-[2-O-methyl tyrosine]-oxytocin). The maximal adenylate cyclase activation induced by these peptides was lower than that induced by their respective parent hormones. After incubation of these analogues with plasma membranes obtained from the renal medulla, no significant release of parent hormones occurred. Good qualitative correlations were observed between relative antidiuretic activities measured in vivo and relative potencies in activating adenylate cyclase. 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subjects Adenylyl Cyclases - metabolism
amino-acylated neurohypophysial peptides
Animals
antidiuretic activity
Cell Membrane - drug effects
Cell Membrane - enzymology
Diuresis - drug effects
Dose-Response Relationship, Drug
Enzyme Activation
Kidney - enzymology
Kidney Medulla - drug effects
Kidney Medulla - enzymology
Kidney Medulla - metabolism
Kidney Medulla - ultrastructure
Oxytocin - analogs & derivatives
Oxytocin - metabolism
Oxytocin - pharmacology
Rats
renal adenylate cyclase
Swine
Vasopressins - analogs & derivatives
Vasopressins - pharmacology
title Renal adenylate cyclase activation by amino acylated vasopressin and oxytocin
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