Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin
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We investigated the mechanisms that regulate the efficacy of agonists in the arginine-vasopressin (AVP)/oxytocin (OT) receptor system. In this paper, we present evidence that AVP, a full agonist of the vasopressin receptors, acts as a partial agonist on the oxytocin receptor. We also found that AVP becomes a full agonist when two aromatic residues of the oxytocin receptor are replaced by the residues present at equivalent positions in the vasopressin receptor subtypes. Our results indicate that these two residues modulate the response of the oxytocin receptor to the partial agonist AVP.
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A host of evidence reveals significant OT and V1aR crosstalk in other model species.
“A host of evidence reveals significant OT and V1aR crosstalk in other model species, including pharmacological studies (Gimpl and Fahrenholz, 2001; Gruber et al., 2012), physiological studies (Chini et al., 1996; Meyer-Lindenberg et al., 2011), and neuropeptide binding and behavioral changes (Loyens et al., 2012; Schorscher-Petcu et al., 2010; Song et al., 2014).”
From Neuropeptide diversity and the regulation of social behavior in New World primates (2016) · cites this paper as Chini et al., 1996
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- Authors
- Chini, B., Mouillac, B., Balestre, M.-N., Trumpp-Kallmeyer, S., Hoflack, J., Hibert, M., Andriolo, M., Pupier, S., Jard, S., & Barberis, C.
- Affiliations
- Inserm (FR)
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1996-11-18
- Volume
- 397
- Issue
- 2-3
- Pages
- 201-206
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2062583603
- Cited by
- 117
- References
- 40
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 2 · 2022: 3 · 2021: 5 · 2020: 5 · 2019: 6 · 2018: 5 · 2017: 2 · 2016: 4 · 2015: 2 · 2014: 6 · 2013: 9 · 2012: 4
- FWCI
- 2.02
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- FEBS Letters (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Institut National de la Santé et de la Recherche Médicale
- Centre National de la Recherche Scientifique
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Social Sciences › Psychology › Social Psychology › Neuroendocrine regulation and behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- oxytocin receptor, vasopressin, partial agonists, agonist efficacy, aromatic residues, vasopressin receptor, G protein-coupled receptors
- MeSH terms
- Amino Acid Sequence, Animals, Arginine Vasopressin, Cell Line, Cloning, Molecular, Computer Simulation, Humans, Models, Molecular, Molecular Sequence Data, Oxytocin, Vasotocin, Mutagenesis, Site-Directed, Receptors, Oxytocin
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