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Crankshaw, DJ,Pistilli, MJ,O'Brien, YM,Sweeney, EM,Dockery, P,Holloway, AC,Morrison, JJ
2013
August
Reproductive Sciences
The Effects of Extracellular Calcium-Sensing Receptor Ligands on the Contractility of Pregnant Human Myometrium In Vitro
Published
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calcium-sensing receptors calhex-231 calindol cinacalcet human myometrium tocolysis SMOOTH-MUSCLE-CELLS CA2+-SENSING RECEPTOR EXPRESSION ARTERY IDENTIFICATION KERATINOCYTES CALHEX-231 CHANNELS DRUGS
20
882
890
Ligands for extracellular calcium-sensing (CaS) receptors inhibit oxytocin-induced contractions of the rat's uterus. In this study, we investigated whether the CaS receptor ligands calindol, cinacalcet, and calhex 231 have similar effects on pregnant human myometrium. We compared their effects to those of the calcium-channel blocker nifedipine. In conventional concentration-effect experiments, both the mean contractile force (MCF) and the maximum amplitude of contractions induced by 1 nmol/L oxytocin were inhibited by nifedipine. Calindol and cinacalcet were ineffective as inhibitors, while calhex-231 produced partial inhibition. When single 10 mol/L doses were applied calhex-231 produced a slowly developing inhibition, reducing the MCF to 38%, and amplitude to 34%, of vehicle controls after 1 hour. In similar experiments, calindol was ineffective while cinacalcet weakly inhibited only the amplitude. Immunohistochemistry revealed sparse expression of CaS receptors in pregnant human myometrium.
DOI 10.1177/1933719112468949
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