Oxytocin is used widely for the induction and augmentation of labour, but t
here is little information about the dynamics of oxytocin receptors in huma
n myometrium during parturition, and the possible effect of oxytocin infusi
on. This information is important because G protein-coupled receptors, such
as the oxytocin receptor, undergo desensitization after prolonged or repea
ted stimulation. The concentration of myometrial oxytocin receptors and the
steady state of its mRNA were measured in patients undergoing Caesarean se
ctions before or during spontaneous or induced labour. The concentration of
receptors before labour was 477 (175-641) fmol mg(-1) protein (median, qua
rtile range), and decreased to 140 (72-206; P < 0.05) and 118 (69-75; P < 0
.01) fmol mg(-1) protein during prolonged oxytocin-augmented and oxytocin-i
nduced labour, respectively. The corresponding oxytocin receptor mRNA conce
ntrations decreased by 60- and 300-fold, respectively. The decrease in rece
ptor binding and mRNA in women receiving oxytocin infusion indicates that h
omologous receptor desensitization occurs in vivo.