Pharmacology of vasopressin antagonists

Lisa C. Costello-Boerrigter; Guido Boerrigter; John C. Burnett

doi:10.1007/s10741-008-9108-8

Pharmacology of vasopressin antagonists

Lisa C. Costello-Boerrigter, Guido Boerrigter, John C. Burnett

Cardiovascular Medicine

Research output: Contribution to journal › Article › peer-review

31 Scopus citations

Abstract

Congestive heart failure (CHF) is characterized by fluid and water retention, which frequently is a therapeutic challenge. Most conventional diuretics act primarily as saluretics, i.e. they inhibit renal tubular electrolyte reabsorption, which due to osmotic pressure promotes excretion of isotonic fluid. Arginine vasopressin (AVP) via the V_1A receptor vasoconstricts and via the V₂ receptor promotes water reabsorption in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Novel V₂ receptor antagonists act as powerful aquaretics, i.e. they excrete free water. We review the pharmacology of non-selective V_1A/V₂ receptor antagonists and selective V₂ receptor antagonists currently in clinical development.

Original language	English (US)
Pages (from-to)	75-82
Number of pages	8
Journal	Heart Failure Reviews
Volume	14
Issue number	2
DOIs	https://doi.org/10.1007/s10741-008-9108-8
State	Published - 2009

Keywords

Aquaretic
Arginine vasopressin
Heart failure
Pharmacology

ASJC Scopus subject areas

Cardiology and Cardiovascular Medicine

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10.1007/s10741-008-9108-8

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title = "Pharmacology of vasopressin antagonists",

abstract = "Congestive heart failure (CHF) is characterized by fluid and water retention, which frequently is a therapeutic challenge. Most conventional diuretics act primarily as saluretics, i.e. they inhibit renal tubular electrolyte reabsorption, which due to osmotic pressure promotes excretion of isotonic fluid. Arginine vasopressin (AVP) via the V1A receptor vasoconstricts and via the V2 receptor promotes water reabsorption in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Novel V2 receptor antagonists act as powerful aquaretics, i.e. they excrete free water. We review the pharmacology of non-selective V1A/V2 receptor antagonists and selective V2 receptor antagonists currently in clinical development.",

keywords = "Aquaretic, Arginine vasopressin, Heart failure, Pharmacology",

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note = "Funding Information: Acknowledgment This work was supported by grants HL POI76611, HLR0136634 (JCB), HL07111 (GB), and the Mayo Foundation, Rochester, MN. Copyright: Copyright 2009 Elsevier B.V., All rights reserved.",

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N2 - Congestive heart failure (CHF) is characterized by fluid and water retention, which frequently is a therapeutic challenge. Most conventional diuretics act primarily as saluretics, i.e. they inhibit renal tubular electrolyte reabsorption, which due to osmotic pressure promotes excretion of isotonic fluid. Arginine vasopressin (AVP) via the V1A receptor vasoconstricts and via the V2 receptor promotes water reabsorption in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Novel V2 receptor antagonists act as powerful aquaretics, i.e. they excrete free water. We review the pharmacology of non-selective V1A/V2 receptor antagonists and selective V2 receptor antagonists currently in clinical development.

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Pharmacology of vasopressin antagonists

Abstract

Keywords

ASJC Scopus subject areas

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