• Open Access

REVIEW: Oxytocin: Crossing the Bridge between Basic Science and Pharmacotherapy

Authors

  • Cedric Viero,

    1.  Department of Cardiology, Wales Heart Research Institute, School of Medicine, Cardiff University, Cardiff, UK
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  • Izumi Shibuya,

    1.  Department of Veterinary Physiology, Tottori University, Tottori, Japan
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  • Naoki Kitamura,

    1.  Department of Veterinary Physiology, Tottori University, Tottori, Japan
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  • Alexei Verkhratsky,

    1.  Department of Cellular Neurophysiology, Institute of Experimental Medicine, Academy of Sciences of the Czech Republic, EU Centre of Excellence, Prague, Czech Republic
    2.  University of Manchester, School of Biological Sciences, Stopford Building, Oxford Road, Manchester M13 9PT, UK
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  • Hiroaki Fujihara,

    1.  Department of Physiology, School of Medicine, University of Occupational and Environmental Health, Kitakyushu, Japan
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  • Akiko Katoh,

    1.  Department of Physiology, School of Medicine, University of Occupational and Environmental Health, Kitakyushu, Japan
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  • Yoichi Ueta,

    1.  Department of Physiology, School of Medicine, University of Occupational and Environmental Health, Kitakyushu, Japan
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  • Hans H. Zingg,

    1.  Department of Pharmacology & Therapeutics, McGill University, Montreal, Quebec, Canada
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  • Alexandr Chvatal,

    1.  Department of Cellular Neurophysiology, Institute of Experimental Medicine, Academy of Sciences of the Czech Republic, EU Centre of Excellence, Prague, Czech Republic
    2.  Center for Cell Therapy and Tissue Repair, Charles University, Second Medical Faculty, Prague, Czech Republic
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  • Eva Sykova,

    1.  Center for Cell Therapy and Tissue Repair, Charles University, Second Medical Faculty, Prague, Czech Republic
    2.  Department of Neuroscience, Institute of Experimental Medicine, Academy of Sciences of the Czech Republic, EU Centre of Excellence, Prague, Czech Republic
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  • Govindan Dayanithi

    1.  Department of Cellular Neurophysiology, Institute of Experimental Medicine, Academy of Sciences of the Czech Republic, EU Centre of Excellence, Prague, Czech Republic
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Correspondence
Govindan Dayanithi, Directeur de Recherche au
CNRS, Laboratory of Physiology of Calcium
Signaling, Department of Cellular
Neurophysiology, Institute of Experimental
Medicine, Academy of Sciences of the Czech
Republic, v.v.i., Videnska, 1083, 142 20 Prague
4, Czech Republic.
Tel.: +420 241 062725;
Fax: +420 241 062732;
E-mail: gdaya@univ-montp2.fr;
gdaya@biomed.cas.cz

SUMMARY

Is oxytocin the hormone of happiness? Probably not. However, this small nine amino acid peptide is involved in a wide variety of physiological and pathological functions such as sexual activity, penile erection, ejaculation, pregnancy, uterus contraction, milk ejection, maternal behavior, osteoporosis, diabetes, cancer, social bonding, and stress, which makes oxytocin and its receptor potential candidates as targets for drug therapy. In this review, we address the issues of drug design and specificity and focus our discussion on recent findings on oxytocin and its heterotrimeric G protein-coupled receptor OTR. In this regard, we will highlight the following topics: (i) the role of oxytocin in behavior and affectivity, (ii) the relationship between oxytocin and stress with emphasis on the hypothalamo–pituitary–adrenal axis, (iii) the involvement of oxytocin in pain regulation and nociception, (iv) the specific action mechanisms of oxytocin on intracellular Ca2+ in the hypothalamo neurohypophysial system (HNS) cell bodies, (v) newly generated transgenic rats tagged by a visible fluorescent protein to study the physiology of vasopressin and oxytocin, and (vi) the action of the neurohypophysial hormone outside the central nervous system, including the myometrium, heart and peripheral nervous system. As a short nine amino acid peptide, closely related to its partner peptide vasopressin, oxytocin appears to be ideal for the design of agonists and antagonists of its receptor. In addition, not only the hormone itself and its binding to OTR, but also its synthesis, storage and release can be endogenously and exogenously regulated to counteract pathophysiological states. Understanding the fundamental physiopharmacology of the effects of oxytocin is an important and necessary approach for developing a potential pharmacotherapy.

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