Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban

2005 ◽  
Vol 11 (10) ◽  
pp. 593-608 ◽  
Author(s):  
Maurice Manning ◽  
Ling Ling Cheng ◽  
Stoytcho Stoev ◽  
Nga Ching Wo ◽  
W. Y Chan ◽  
...  
Keyword(s):  
Oxytocin Receptor ◽  
Oxytocin Antagonists

scholarly journals The Oxytocin-Oxytocin Receptor System and Its Antagonists as Tocolytic Agents

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Nikolaos Vrachnis ◽  
Fotodotis M. Malamas ◽  
Stavros Sifakis ◽  
Efthymios Deligeoroglou ◽  
Zoe Iliodromiti
Keyword(s):  
Preterm Labor ◽  
Oxytocin Receptor ◽  
Uterine Contractility ◽  
Receptor Antagonists ◽  
Receptor System ◽  
Main Pathway ◽  
Intracellular Ca ◽  
Oxytocin Antagonists ◽  
Tocolytic Agents ◽  
G Protein Coupled

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+2and 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.

Regulation of the Oxytocin Receptor in Bovine Reproductive Tissues and the Role of Steroids

2000 ◽  
Vol 35 (3-4) ◽  
pp. 134-141 ◽  
Author(s):  
R Ivell ◽  
A-R Fuchs ◽  
R Bathgate ◽  
G Tillmann ◽  
T Kimura
Keyword(s):  
Oxytocin Receptor ◽  
Reproductive Tissues

1422: Oxytocin Receptor and Caveolin-1 Expression in the Prostate of Young and Aging Male

2005 ◽  
Vol 173 (4S) ◽  
pp. 385-386
Author(s):  
Gregor Bötticher ◽  
Zsófia Herbert ◽  
Erdogan Sendemir ◽  
Andreas Aschoff ◽  
Gustav Friedrich Jirikowski ◽  
...  
Keyword(s):  
Oxytocin Receptor ◽  
Aging Male ◽  
Caveolin 1
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