Development and therapeutic indications of orally-active non-peptide vasopressin receptor antagonists

Expert Opinion on Investigational Drugs
S B Paranjape, M Thibonnier

Abstract

Vasopressin (AVP) is a cyclic nonapeptide hormone that exhibits many physiological effects including free water reabsorption, vasoconstriction, cellular proliferation and adrenocorticotrophic hormone (ACTH) secretion. In a healthy organism, AVP plays an important role in the homeostasis of fluid osmolality and volume status. However, in several diseases or conditions such as the syndrome of inappropriate secretion of AVP (SIADH), congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome, dysmenorrhoea and ocular hypertension, AVP may play an important role in their pathophysiology. Recently, orally-active non-peptide AVP receptor antagonists were developed by random screening of chemical entities and optimisation of lead compounds. These include agents specific for the V(1)-vascular and V(2)-renal AVP receptor subtypes. Dual V(1)/V(2) AVP receptor antagonists are also being studied. Some of these non-peptide receptor antagonists have been studied extensively, while others are currently under investigation. Potential therapeutic indications for AVP receptor antagonists comprise: 1) The blockade of V(1)-vascular AVP receptors in arterial hypertension, congestive heart failure, Raynaud's syndrome, periph...Continue Reading

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Citations

Dec 4, 2003·Current Opinion in Pharmacology·Marc Thibonnier
Mar 21, 2006·Proceedings of the National Academy of Sciences of the United States of America·Werner G PurschkeSven Klussmann
May 20, 2004·Bioorganic & Medicinal Chemistry Letters·Min Amy XiangMona Patel
May 6, 2004·Bioorganic & Medicinal Chemistry Letters·Min Amy XiangMona Patel
Apr 20, 2007·Biology of Reproduction·Travis M HagedornBruce D Schultz
Jun 12, 2003·Bioorganic & Medicinal Chemistry Letters·Fuk Wah SumTrina Saunders
Nov 22, 2005·Bioorganic & Medicinal Chemistry Letters·Amedeo A FailliC H Park

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