The effect of the oxytocin antagonists, CAP 476 and F327, on calcium mobilisation in single cultured human myometrial cells

Br J Obstet Gynaecol. 1993 Jun;100(6):581-6. doi: 10.1111/j.1471-0528.1993.tb15314.x.

Abstract

Objective: To investigate the mechanism of action of the oxytocin (OT) antagonists, CAP 476 and F327.

Design: A prospective descriptional study.

Subjects: Women undergoing caesarean section at term or hysterectomy.

Interventions: Myometrial cells were cultured from uterine biopsies.

Main outcome measures: Intracellular calcium ([Ca2+]i), determined in single cells.

Results: Application of OT caused a transient increase in [Ca2+]i. CAP 476 abolished and F327 reduced the response to OT but neither reduced the [Ca2+]i transient induced by cell depolarisation with 120 mmol K+. CAP 476 did not reduce transients caused by prostaglandin E2. F327 reduced the frequency of repetitive [Ca2+]i transients occurring during continuous application of OT.

Conclusions: The results demonstrate that the antagonists reduce the effect of OT and that their action is relatively specific. Their mechanism of action as clinical tocolytic agents is discussed.

MeSH terms

  • Calcium / metabolism*
  • Calcium Channels / drug effects
  • Calcium Channels / metabolism
  • Cesarean Section
  • Female
  • Humans
  • Hysterectomy
  • Myometrium / drug effects
  • Myometrium / metabolism*
  • Oxytocin / analogs & derivatives*
  • Oxytocin / metabolism*
  • Oxytocin / pharmacology
  • Pregnancy
  • Prospective Studies
  • Vasotocin / analogs & derivatives*
  • Vasotocin / pharmacology

Substances

  • Calcium Channels
  • atosiban
  • F 327
  • Oxytocin
  • Calcium
  • Vasotocin