Περίληψη:
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.
Συγγραφείς:
Vrachnis, Nikolaos
Malamas, Fotodotis M.
Sifakis, Stavros and
Deligeoroglou, Efthymios
Iliodromiti, Zoe
