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Homologous regulation of brain oxytocin receptors.
Abstract
Specific receptors for oxytocin have been identified in rat forebrain. Previous studies have demonstrated that in select regions, these receptors are dependent on heterologous induction by gonadal steroids. To investigate whether brain oxytocin receptors are homologously regulated by oxytocin, we measured oxytocin receptor binding after hypothalamic paraventricular nucleus lesions, repeated central injections of oxytocin, and continuous central infusion of oxytocin via osmotic minipump. Neither lesions of the paraventricular nucleus nor repeated oxytocin injections altered the binding of the selective oxytocin receptor ligand [125I]OTA [125I] d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH2(9)] ornithine vasotocin, as measured by in vitro receptor autoradiography. After 10 days of continuous oxytocin infusion by osmotic minipump, oxytocin receptor binding decreased in every target field by at least 50%. This decrease appeared to represent a down-regulation of receptors and not displacement by exogenous peptide, as it persisted for at least 24 h after pump removal, and binding remained reduced in the presence of a saturating concentration of [125I] OTA. Reduction of oxytocin receptors in response to increased oxytocin release may represent an important physiological mechanism for the regulation of central oxytocin neurotransmission.
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“Thus, intranasal administration of OXT might act to increase the concentration of OXT beyond endogenous levels in a normal-functioning brain resulting in desensitisation and hence, down-regulation of OXTRs.”
From Chronic and acute intranasal oxytocin produce divergent social effects in mice (2014) · cites this paper as Insel et al, 1992
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“Indeed, the oxytocin receptor is a G protein-coupled receptor and can undergo desensitisation and internalization after agonist application (Conti et al, 2009;Insel et al, 1992).”
From Chronic and acute intranasal oxytocin produce divergent social effects in mice (2014) · cites this paper as Insel et al, 1992
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Metadata
- Authors
- Insel, T. R., Winslow, J. T., & Witt, D. M.
- Affiliations
- National Institute of Mental Health (US)
- ORCID
- Insel, T R
- Venue
- Endocrinology
- Publisher
- The Endocrine Society
- Published
- 1992-05
- Volume
- 130
- Issue
- 5
- Pages
- 2602-2608
- ISSN
- 0013-7227 (ISSN-L)
- 1945-7170
- OpenAlex
- W2089520243
- Cited by
- 63
- References
- 18
- Citations by year
- 2025: 1 · 2023: 1 · 2022: 2 · 2021: 6 · 2020: 1 · 2019: 2 · 2018: 2 · 2017: 5 · 2016: 1 · 2015: 2 · 2014: 1 · 2013: 3 · 2012: 2
- FWCI
- 6.87
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrinology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Neuroendocrine regulation and behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Reproductive Medicine › Hypothalamic control of reproductive hormones
- Keywords
- oxytocin receptor, receptor down-regulation, paraventricular nucleus, forebrain, receptor binding, arginine vasotocin, hypothalamus
- MeSH terms
- Animals, Autoradiography, Brain, Cerebral Ventricles, Injections, Intraventricular, Iodine Radioisotopes, Male, Organ Specificity, Oxytocin, Paraventricular Hypothalamic Nucleus, Rats, Inbred Strains, Receptors, Angiotensin, Stereotaxic Techniques, Receptors, Oxytocin, Rats
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