ArticleThe Journal of pharmacology and experimental therapeutics2013
Selective and potent agonists and antagonists for investigating the role of mouse oxytocin receptors.
Article in The Journal of pharmacology and experimental therapeutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.
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Who cites it
52 citing papers in PubMed, 101 citations in OpenAlex.
- Oxytocin supports the barrier integrity of brain endothelial cells via oxytocin receptors.Journal of neuroendocrinology · 2026Article
- Ethological Constraints and Welfare-Related Bias in Laboratory Mice: Implications of Housing, Lighting, and Social Environment.Animals : an open access journal from MDPI · 2026Review
- Acute administration of Manning compound during the spawning period reduces reproductive success in female zebrafish.Frontiers in endocrinology · 2026Article
- Fluorescent Peptide Tracers for Simultaneous Oxytocin Receptor Activation and Visualization.Angewandte Chemie (International ed. in English) · 2025Article
- Vasopressin and oxytocin excite BNST neurons via oxytocin receptors, which reduce anxious arousal.Cell reports · 2025Article
- Oxytocin in neurodevelopmental disorders: Autism spectrum disorder and Prader-Willi syndrome.Pharmacology & therapeutics · 2024Review
- Neuropeptide therapeutics to repress lateral septum neurons that disable sociability in an autism mouse model.Cell reports. Medicine · 2024Article
- Article
- Leveraging the unique social organization of California mice to study circuit-specific effects of oxytocin on behavior.Hormones and behavior · 2024Review
- A genetically encoded sensor measures temporal oxytocin release from different neuronal compartments.Nature biotechnology · 2023Article
- Oxytocin mediated excitation of hypoglossal motoneurons: implications for treating obstructive sleep apnea.Sleep · 2023Article
- Vasopressin V1a receptor and oxytocin receptor regulate murine sperm motility differently.Life science alliance · 2023Article
- Rethinking the Architecture of Attachment: New Insights into the Role for Oxytocin Signaling.Affective science · 2022Review
- Paraventricular Nucleus VPhysiology & behavior · 2022Article
- Sex-specific and social experience-dependent oxytocin-endocannabinoid interactions in the nucleus accumbens: implications for social behaviour.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2022Review
- Oxytocin via oxytocin receptor excites neurons in the endopiriform nucleus of juvenile mice.Scientific reports · 2022Article
- Oxytocin receptor behavioral effects and cell types in the bed nucleus of the stria terminalis.Hormones and behavior · 2022Article
- On the Utility of Chemical Strategies to Improve Peptide Gut Stability.Journal of medicinal chemistry · 2022Article
- Oxytocin and vasopressin: Signalling, behavioural modulation and potential therapeutic effects.British journal of pharmacology · 2022Review
- Social experience alters oxytocinergic modulation in the nucleus accumbens of female prairie voles.Current biology : CB · 2022Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 3 countries.
Funding
Abstract
The neuropeptides oxytocin (OT) and vasopressin (AVP) have been shown to play a central role in social behaviors; as a consequence, they have been recognized as potential drugs to treat neurodevelopmental and psychiatric disorders characterized by impaired social interactions. However, despite the basic and preclinical relevance of mouse strains carrying genetic alterations in the OT/AVP systems to basic and preclinical translational neuroscience, the pharmacological profile of mouse OT/AVP receptor subtypes has not been fully characterized. To fill in this gap, we have characterized a number of OT and AVP agonists and antagonists at three murine OT/AVP receptors expressed in the nervous system as follows: the oxytocin (mOTR) and vasopressin V1a (mV1aR) and V1b (mV1bR) subtypes. These three receptors were transiently expressed in vitro for binding and intracellular signaling assays, and then a homology model of the mOTR structure was constructed to investigate how its molecular features compare with human and rat OTR orthologs. Our data indicate that the selectivity profile of the natural ligands, OT and AVP, is conserved in humans, rats, and mice. Furthermore, we found that the synthetic peptide [Thr(4)Gly(7)]OT (TGOT) is remarkably selective for the mOTR and, like the endogenous OT ligand, activates Gq and Gi and recruits β-arrestins. Finally, we report three antagonists that exhibit remarkably high affinities and selectivities at mOTRs. These highly selective pharmacological tools will contribute to the investigation of the specific physiologic and pathologic roles of mOTR for the development of selective OT-based therapeutics.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.