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Cited by 306Neuroendocrine regulation and behaviorNeuropeptides and Animal PhysiologyChemical Synthesis and Analysis

The DOI matches its Crossref record; 263 of the 265 references it cites were found in a registry or an index.

Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents☆

MANNING, M, STOEV, S, CHINI, B, DURROUX, T, MOUILLAC, B, GUILLON, G·2008·Progress in Brain Research
DOI 10.1016/s0079-6123(08)00437-8
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Abstract

Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)? (vasodilating) receptor. This presentation will summarize some highlights of the recent progress, in the design and synthesis of selective peptide agonists, antagonists, radioiodinated ligands, fluorescent ligands and bivalent ligands for these receptors. Here we present published and unpublished pharmacological data on the most widely used agonists, antagonists and labelled ligands. The pharmacological properties of promising new selective OT antagonists and V(1b) agonists are also presented. This review should serve as a useful guide for the selection of the most appropriate ligand for a given study. The current status of non-peptide OT and AVP antagonists and agonists is also summarized. The relative merits of peptide and non-peptide AVP and OT agonists and antagonists as: (1) research tools and (2) therapeutic agents will be evaluated. Many of the receptor selective peptide agonists and antagonists from this and other laboratories are far more widely used as pharmacological tools for studies on the peripheral and central effects of OT and AVP than their non-peptide counterparts. In addition to OT and to a lesser extent AVP (pitressin), a number of OT and AVP analogues; such as carbetocin (OT agonist) dDAVP (desmopressin, V(2) agonist), terlipressin (V(1a) agonist), felypressin (V(1a) agonist) and atosiban (Tractocile OT antagonist) are also in clinical use. Despite much early promise, no non-peptide V(1a) or OT antagonists are currently in clinical trials. While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v. administration), for the treatment of euvolemic and hypervolemic hyponatremia in hospitalized patients. Promising new non-peptide V(1b) and OT antagonists, as well as non-peptide V(2) and OT agonists are now in pre-clinical development.

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Metadata

Authors
MANNING, M., STOEV, S., CHINI, B., DURROUX, T., MOUILLAC, B., & GUILLON, G.
Affiliations
  • University of Toledo (US)
  • Centre National de la Recherche Scientifique (FR)
Corresponding author
MANNING, M
ORCID
Venue
Progress in Brain Research
Publisher
Elsevier
Published
2008
Volume
170
Pages
473-512
ISSN
0079-6123 (ISSN-L)
DOI
10.1016/s0079-6123(08)00437-8
OpenAlex
W1523553171
Cited by
296
References
265
Citations by year
2026: 7 · 2025: 7 · 2024: 8 · 2023: 5 · 2022: 14 · 2021: 23 · 2020: 10 · 2019: 15 · 2018: 19 · 2017: 23 · 2016: 15 · 2015: 29 · 2014: 23 · 2013: 20 · 2012: 25
FWCI
46.73
Type
book chapter
Language
en
Open access
closed
Locations
  • Progress in brain research (publishedVersion)
  • PubMed (publishedVersion)
Funders
National Institute of General Medical Sciences (GM25280, R01GM025280)
Topics
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Neuroendocrine regulation and behavior
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
  • Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
Keywords
vasopressin, oxytocin, vasopressin V1a receptor, vasopressin V1b receptor, V2 receptor, oxytocin receptor, peptide agonists, peptide antagonists, non-peptide agonists, non-peptide antagonists, radioiodinated ligands, fluorescent ligands, bivalent ligands, desmopressin, terlipressin, felypressin, atosiban, vasopressin receptor antagonists, conivaptan
MeSH terms
Terlipressin, Animals, Benzazepines, Clinical Trials as Topic, Deamino Arginine Vasopressin, Female, Humans, Hyponatremia, Lypressin, Oligopeptides, Oxytocin, Peptides, Structure-Activity Relationship, Uterus, Vasodilator Agents, Vasopressins, Receptors, Vasopressin, Receptors, Oxytocin, Antidiuretic Agents, Rats, Antidiuretic Hormone Receptor Antagonists

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