The Basic and Clinical Pharmacology of Nonpeptide Vasopressin Receptor Antagonists
Abstract
The neurohypophysial hormone arginine vasopressin (AVP) is a cyclic nonpeptide whose actions are mediated by the stimulation of specific G protein–coupled membrane receptors pharmacologically classified into V 1-vascular (V 1 R), V 2-renal (V 2 R) and V 3-pituitary (V 3 R) AVP receptor subtypes. The random screening of chemical compounds and optimization of lead compounds recently resulted in the development of orally active nonpeptide AVP receptor antagonists. Potential therapeutic uses of AVP receptor antagonists include (a) the blockade of V 1-vascular AVP receptors in arterial hypertension, congestive heart failure, and peripheral vascular disease; (b) the blockade of V 2-renal AVP receptors in the syndrome of inappropriate vasopressin secretion, congestive heart failure, liver cirrhosis, nephrotic syndrome and any state of excessive retention of free water and subsequent dilutional hyponatremia; (c) the blockade of V 3-pituitary AVP receptors in adrenocorticotropin-secreting tumors. The pharmacological and clinical profile of orally active nonpeptide vasopressin receptor antagonists is reviewed here.
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AVP has similar affinity for OTRs, V1aRs, and V1bRs, whereas OT may have a higher affinity for OTRs than for V1aRs or V1bRs.
“AVP has a similar affinity for OTRs, V1aRs, and V1bRs while OT may have a higher affinity for OTRs than V1aRs or V1bRs [28; 29; 30; 31; 32; 33].”
From Cross-talk among oxytocin and arginine-vasopressin receptors: Relevance for basic and clinical studies of the brain and periphery (2018) · cites this paper as [32]
There can be differences of around 10-100 fold in the selectivity of OTRs and AVP receptors for OT and AVP.
“Nevertheless, it appears that there can be differences of around 10–100 fold in the selectivity of OTRs and AVP receptors for OT and AVP.”
From Cross-talk among oxytocin and arginine-vasopressin receptors: Relevance for basic and clinical studies of the brain and periphery (2018) · cites this paper as [32]
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- Authors
- Thibonnier, M., Coles, P., Thibonnier, A., & Shoham, M.
- Affiliations
- University Hospitals of Cleveland (US)
- ORCID
- Thibonnier, M
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 2001-04
- Volume
- 41
- Issue
- 1
- Pages
- 175-202
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2104748479
- Cited by
- 146
- References
- 2
- Citations by year
- 2026: 1 · 2024: 2 · 2022: 4 · 2021: 3 · 2020: 3 · 2019: 5 · 2018: 2 · 2017: 5 · 2016: 4 · 2015: 7 · 2014: 8 · 2013: 7 · 2012: 7
- FWCI
- 2.25
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Annual Review of Pharmacology and Toxicology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Electrolyte and hormonal disorders
- Health Sciences › Medicine › Surgery › Cardiovascular, Neuropeptides, and Oxidative Stress Research
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- vasopressin receptor antagonists, vasopressin, V1 receptor, V2 receptor, G protein-coupled receptors, syndrome of inappropriate antidiuretic hormone secretion, hyponatremia, hypertension, congestive heart failure, drug development
- MeSH terms
- Amino Acid Sequence, Animals, Arginine Vasopressin, Humans, Molecular Sequence Data, Receptors, Vasopressin, Antidiuretic Hormone Receptor Antagonists
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