The V2 receptor antagonist tolvaptan raises cytosolic calcium and prevents AQP2 trafficking and function: an in vitro and in vivo assessment

Tolvaptan, a selective vasopressin V2 receptor antagonist, is a new generation diuretic. Its clinical efficacy is in principle due to impaired vasopressin‐regulated water reabsorption via aquaporin‐2 (AQP2). Nevertheless, no direct in vitro evidence that tolvaptan prevents AQP2‐mediated water transp...

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Veröffentlicht in:	Journal of cellular and molecular medicine 2017-09, Vol.21 (9), p.1767-1780
Hauptverfasser:	Tamma, Grazia, Di Mise, Annarita, Ranieri, Marianna, Geller, Ari, Tamma, Roberto, Zallone, Alberta, Valenti, Giovanna
Format:	Artikel
Sprache:	eng
Schlagworte:	Aged, 80 and over Animals Antidiuretic Hormone Receptor Antagonists - pharmacology Antidiuretic Hormone Receptor Antagonists - therapeutic use Aquaporin 2 - metabolism Aquaporin 2 - urine aquaporin‐2 Benzazepines - pharmacology Calcium - metabolism Cell Membrane - drug effects Cell Membrane - metabolism Cell Membrane Permeability - drug effects Cyclic AMP - metabolism Cytosol - drug effects Cytosol - metabolism Dogs Endoplasmic Reticulum - drug effects Endoplasmic Reticulum - metabolism Female Fluorescence Resonance Energy Transfer Humans hyponatraemia Inappropriate ADH Syndrome - blood Inappropriate ADH Syndrome - drug therapy Kidney - drug effects Kidney - metabolism Madin Darby Canine Kidney Cells Male Mice, Knockout Middle Aged Original Osmosis Phosphorylation - drug effects PKD Protein Phosphatase 1 - metabolism Protein Transport - drug effects Receptors, Vasopressin - metabolism SIAD Sodium - blood tolvaptan vasopressin Water - metabolism
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