| Development and therapeutic indications of orally-active non-peptide vasopressin receptor antagonists. | |
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MedLine Citation:
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PMID: 11322860 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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, peripheral vascular disease and dysmenorrhea. 2) The blockade of V(2)-renal AVP receptors in the syndrome of inappropriate secretion of vasopressin, congestive hart failure, liver cirrhosis, nephrotic syndrome and any state of excessive retention of free water and subsequent dilutional hyponatraemia. 3) The blockade of V(3)-pituitary AVP receptors in ACTH-secreting tumours. This review examines the pharmacology of orally-active non-peptide AVP receptor antagonists and their clinical applications. |
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Authors:
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S B Paranjape; M Thibonnier |
Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Expert opinion on investigational drugs Volume: 10 ISSN: 1354-3784 ISO Abbreviation: Expert Opin Investig Drugs Publication Date: 2001 May |
Date Detail:
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Created Date: 2001-04-27 Completed Date: 2001-08-16 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9434197 Medline TA: Expert Opin Investig Drugs Country: England |
Other Details:
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Languages: eng Pagination: 825-34 Citation Subset: IM |
Affiliation:
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Case Western Reserve University School of Medicine and University Hospitals of Cleveland, 10900 Euclid Avenue, Cleveland, Ohio 44106-4951, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Diabetes Insipidus / drug therapy Dysmenorrhea / drug therapy Female Heart Failure / drug therapy Humans Hypertension / drug therapy Hyponatremia / drug therapy Receptors, Vasopressin / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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0/Receptors, Vasopressin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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