The oxytocin receptor system: structure, function, and regulation.

  title={The oxytocin receptor system: structure, function, and regulation.},
  author={Gerald Gimpl and Falk Fahrenholz},
  journal={Physiological reviews},
  volume={81 2},
The neurohypophysial peptide oxytocin (OT) and OT-like hormones facilitate reproduction in all vertebrates at several levels. The major site of OT gene expression is the magnocellular neurons of the hypothalamic paraventricular and supraoptic nuclei. In response to a variety of stimuli such as suckling, parturition, or certain kinds of stress, the processed OT peptide is released from the posterior pituitary into the systemic circulation. Such stimuli also lead to an intranuclear release of OT… 

Figures and Tables from this paper

Oxytocin--anatomy and functional assignments: a minireview.

Oxytocin (OXY) is a very abundant neuropeptide exerting a wide spectrum of central and peripheral effects as neurohormone, neurotransmitter, or neuromodulator as well as in peripheral tissues, including uterus, placenta, amnion, corpus luteum, testis, and heart.

Conditional oxytocin receptor knockout mice: targeting the forebrain to understand behavior.

  • J. Amico
  • Biology, Psychology
  • 2008
The development of a conditional knockout (KO) of the OTR in selected forebrain regions of the mouse is reported, and the physiological and behavioral consequences of this genetic manipulation are reported.

Oxytocin and Estrogen Receptor β in the Brain: An Overview

A role for OT is found in this estrogen receptor β-mediated anxiolytic effect and further research is needed to identify modulators of OT signaling and the pathways utilized to allow better therapeutic manipulations of this system in patient populations.

Regulation of oxytocin receptors and oxytocin receptor signaling.

The current knowledge of the complex regulation of OTR transcription in the myometrium and the intracellular signaling mechanisms through which OT mediates its potent stimulatory effects are summarized.

Molecular regulation of the oxytocin receptor in peripheral organs.

Findings taken together indicate that the oxytocin receptor is regulated in a very complicated manner, and the transcriptional regulatory elements critical for this regulation should be investigated further.

Computer aided study of the oxytocin - receptor complex binding sites

The aim of this investigation is to construct a three dimensional model of the oxytocin receptor, to be used to define the binding sites between oxytoc in and its receptor, as a prerequisite for further search for oxytocIn receptor antagonists.

Neural Functions of Hypothalamic Oxytocin and its Regulation

Brain functions of OT and their underlying neural mechanisms as well as the perspectives of their clinical usage are presented.

Complementary Role of Oxytocin and Vasopressin in Cardiovascular Regulation

The inappropriate regulation of oxytocin and vasopressin secretion during ischemia, hypoxia/hypercapnia, inflammation, pain, and stress may play a significant role in the pathogenesis of cardiovascular diseases.



Oxytocin Receptors in the Central Nervous System

The distribution of OT receptors in the adult rat brain is first reported; then, their development in the same species; and moreover, differences in their localization among species.

Central Nervous System Effects of the Neurohypophyseal Hormones and Related Peptides

It appears that adequate amounts of vasopressin and oxytocin to induce these effects are released at the appropriate sites of action, and norepinephrine, dopamine, serotonin, and glutamate are the neurotransmitters involved in the influence of the neurohypophyseal hormones and related neuropeptides on brain function.

Structural bases of vasopressin/oxytocin receptor function.

Recent studies suggest that the vasopressin V1b receptor may serve additional and unknown functions in the brain and at the periphery, and a great number of molecular probes have been developed, including agonists and antagonists, and radiolabelled, fluorescent or photosensitive ligands.

Ricin‐Cytotoxin Conjugate Administration Reveals a Physiologically Relevant Role for Oxytocin in the Control of Gonadotropin Secretion a

It is now apparant that the OT can exert physiologically relevant actions within the anterior pituitary gland to stimulate prolactin (PRL)2J and corticotropin (ACTHr secretion) and to potentiate hypothalamic drive exerted by other releasing factors and, in some unique situations, be the primary releasing factor.

Structure, characterization, and expression of the rat oxytocin receptor gene.

To study the molecular mechanisms underlying OTR regulation, recombinant bacteriophage lambda EMBL3 genomic clones containing the rat OTR gene are isolated and characterized using sequence information derived from a human myometrial OTR cDNA, supporting the notion that interleukins may mediate labor induction via transcriptional activation of the O TR gene.

The role of sex steroids in the oxytocin hormone system

Oxytocin receptor messenger ribonucleic acid: characterization, regulation, and cellular localization in the rat pituitary gland.

Northern blot analysis, reverse transcriptase-polymerase chain reaction, and in situ hybridization analysis indicated a dramatic increase in pituitary OTR gene expression at the end of gestation and after estrogen treatment, suggesting the role of OT as a hypothalamic PRL-releasing factor may so far have been underestimated.

Oxytocin and male reproductive function.

In the male mammal, the small peptide hormone oxytocin is produced in similar quantities within the hypothalamo-pituitary magnocellular system as in the female, yet for the male little is known about

The oxytocin receptor.

  • T. KimuraR. Ivell
  • Biology, Chemistry
    Results and problems in cell differentiation
  • 1999
The oxytocin receptor was first identified using a pharmacological ligandbinding assay in the rat myometrium in the 1970s and, amongst eutherian mammals, arginine8-vasopressin (AVP), though having its own specific receptors, was shown to bind to the oxytocIn receptor with almost as high affinity as oxytoc in itself.