The effect of relaxin on the oxytocin receptor in human uterine smooth muscle cells

Oct 24, 2006Regulatory peptides

Relaxin’s effect on oxytocin receptors in human uterine muscle cells

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Abstract

Prolonged relaxation hormone (RLX) incubation inhibited 30-40% of oxytocin receptor (OTR) binding in human uterine smooth muscle cells.

OTR mRNA expression decreased by about 50% following RLX treatment.
OTR protein expression was down regulated by approximately 35%.
Binding affinity of OTR remained unchanged despite the decrease in binding.
The findings suggest that high local concentrations of RLX may contribute to uterine quiescence during pregnancy by reducing OTR levels.

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EXPERIMENTAL OBJECTIVES: Activation of the oxytocin receptor (OTR) induces phospholipase C induced PIP(2) turnover in the human uterus. Relaxin (RLX), a polypeptide hormone produced in the corpus luteum of pregnancy as well as in the placenta and decidua inhibits PIP(2) turnover and subsequent signaling in human myometrium. The purpose of this study was to evaluate a possible effect of RLX on OTR regulation in human uterine smooth muscle cells. Primary cultures of myometrium from term pregnant women undergoing elective caesarean section were incubated for different time periods (0-96 h) and with different concentrations of RLX [10 pg/ml-20 microg/ml]. The effects on OTR binding, mRNA and protein expression were evaluated by means of (125)I-OVT binding assay, RT-PCR and flow cytometry.

RESULTS: Prolonged RLX incubation was able to inhibit 30-40% of OTR binding while binding affinity remained unchanged. Oxytocin receptor mRNA and protein expression were down regulated by RLX about 50% and 35% respectively.

CONCLUSION: We report for the first time an effect of RLX on OTR regulation in human uterine myometrial cells. The above results indicate that high local uterine RLX concentrations may be involved in uterine quiescence during human pregnancy by down regulating the OTR.

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The effect of relaxin on the oxytocin receptor in human uterine smooth muscle cells

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