The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents
Oxytocin, a hormone involved in numerous physiologic processes, plays a central role in the mechanisms of parturition and lactation. It acts through its receptor, which belongs to the G-protein-coupled receptor superfamily, while Gq/phospholipase C (PLC)/inositol 1,4,5-triphosphate (InsP3) is the ma...
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| Format: | Article |
| Language: | English |
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Wiley
2011-01-01
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| Series: | International Journal of Endocrinology |
| Online Access: | http://dx.doi.org/10.1155/2011/350546 |
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| author | Nikolaos Vrachnis Fotodotis M. Malamas Stavros Sifakis Efthymios Deligeoroglou Zoe Iliodromiti |
| author_facet | Nikolaos Vrachnis Fotodotis M. Malamas Stavros Sifakis Efthymios Deligeoroglou Zoe Iliodromiti |
| author_sort | Nikolaos Vrachnis |
| collection | DOAJ |
| description | Oxytocin, a hormone involved in numerous physiologic processes, plays a central role in the mechanisms of parturition and lactation. It acts through its receptor, which belongs to the G-protein-coupled receptor superfamily, while Gq/phospholipase C (PLC)/inositol 1,4,5-triphosphate (InsP3) is the main pathway via which it exerts its action in the myometrium. Changes in receptor levels, receptor desensitization, and locally produced oxytocin are factors that influence the effect of oxytocin on uterine contractility in labor. Activation of oxytocin receptor causes myometrial contractions by increasing intracellular Ca+2 and production of prostaglandins. Since oxytocin induces contractions, the inhibition of its action has been a target in the management of preterm labor. Atosiban is today the only oxytocin receptor antagonist that is available as a tocolytic. However, the quest for oxytocin receptor antagonists with a better pharmacological profile has led to the synthesis of peptide and nonpeptide molecules such as barusiban, retosiban, L-368,899, and SSR-126768A. Many of these oxytocin receptor antagonists are used only as pharmacological tools, while others have tocolytic action. In this paper, we summarize the action of oxytocin and its receptor and we present an overview of the clinical and experimental data of oxytocin antagonists and their tocolytic action. |
| format | Article |
| id | doaj-art-dc4235fbfc0f42c3a5afbe1c54e5ba5b |
| institution | Kabale University |
| issn | 1687-8337 1687-8345 |
| language | English |
| publishDate | 2011-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | International Journal of Endocrinology |
| spelling | doaj-art-dc4235fbfc0f42c3a5afbe1c54e5ba5b2025-02-03T06:15:13ZengWileyInternational Journal of Endocrinology1687-83371687-83452011-01-01201110.1155/2011/350546350546The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic AgentsNikolaos Vrachnis0Fotodotis M. Malamas1Stavros Sifakis2Efthymios Deligeoroglou3Zoe Iliodromiti42nd Department of Obstetrics and Gynecology, Aretaieio Hospital, University of Athens Medical School, 11526 Athens, Greece1st Department of Obstetrics and Gynecology, Alexandra Hospital, University of Athens Medical School, 11526 Athens, GreeceDepartment of Obstetrics and Gynaecology, University Hospital of Heraklion, 71110 Heraklion, Crete, Greece2nd Department of Obstetrics and Gynecology, Aretaieio Hospital, University of Athens Medical School, 11526 Athens, Greece2nd Department of Obstetrics and Gynecology, Aretaieio Hospital, University of Athens Medical School, 11526 Athens, GreeceOxytocin, a hormone involved in numerous physiologic processes, plays a central role in the mechanisms of parturition and lactation. It acts through its receptor, which belongs to the G-protein-coupled receptor superfamily, while Gq/phospholipase C (PLC)/inositol 1,4,5-triphosphate (InsP3) is the main pathway via which it exerts its action in the myometrium. Changes in receptor levels, receptor desensitization, and locally produced oxytocin are factors that influence the effect of oxytocin on uterine contractility in labor. Activation of oxytocin receptor causes myometrial contractions by increasing intracellular Ca+2 and production of prostaglandins. Since oxytocin induces contractions, the inhibition of its action has been a target in the management of preterm labor. Atosiban is today the only oxytocin receptor antagonist that is available as a tocolytic. However, the quest for oxytocin receptor antagonists with a better pharmacological profile has led to the synthesis of peptide and nonpeptide molecules such as barusiban, retosiban, L-368,899, and SSR-126768A. Many of these oxytocin receptor antagonists are used only as pharmacological tools, while others have tocolytic action. In this paper, we summarize the action of oxytocin and its receptor and we present an overview of the clinical and experimental data of oxytocin antagonists and their tocolytic action.http://dx.doi.org/10.1155/2011/350546 |
| spellingShingle | Nikolaos Vrachnis Fotodotis M. Malamas Stavros Sifakis Efthymios Deligeoroglou Zoe Iliodromiti The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents International Journal of Endocrinology |
| title | The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents |
| title_full | The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents |
| title_fullStr | The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents |
| title_full_unstemmed | The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents |
| title_short | The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents |
| title_sort | oxytocin oxytocin receptor system and its antagonists as tocolytic agents |
| url | http://dx.doi.org/10.1155/2011/350546 |
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