磷酸二酯酶4（PDE4）选择性抑制剂单独及与β2-拟似剂同时给药对催产素诱导的妊娠子宫肌层收缩的子宫舒张作用。

Utero-relaxant effect of PDE4-selective inhibitor alone and in simultaneous administration with beta2-mimetic on oxytocin-induced contractions in pregnant myometrium.

作者信息

Franova Sona, Janicek Frantisek, Visnovsky Jozef, Dokus Karol, Zubor Pavol, Sutovska Martina, Nosalova Gabriela

机构信息

Department of Pharmacology, Jessenius Faculty of Medicine, Comenius University, Martin, Slovakia.

出版信息

J Obstet Gynaecol Res. 2009 Feb;35(1):20-5. doi: 10.1111/j.1447-0756.2008.00839.x.

DOI:10.1111/j.1447-0756.2008.00839.x

PMID:19215543

Abstract

BACKGROUND

The objective of the study was to observe the effect of rolipram, the prototype phosphodiesterase 4 selective inhibitor, on oxytocin-induced contractions of human term myometrial strips, and compare the effect with salbutamol, beta(2)-adrenergic agonist, in single and the simultaneous application.

METHODS

Human myometrium was obtained from pregnant women in term that had a term delivery by the caesarian section. Myometrial strips were excised from the lower uterine segment and placed into an organ-bath with Krebs-Henseleit buffer. The mean peak amplitude of contraction (mN) of the myometrial smooth muscle to the doses of oxytocin (10(-6) mmol/L(-1)) with subsequent single administration of rolipram (10(-4) mmol/L(-1)), salbutamol (10(-4) mmol/L(1)) and simultaneous administration of rolipram and salbutamol (both 10(-4) mmol/L(-1)), was used as a parameter of myometrial reactivity.

RESULTS

Rolipram alone decreased the oxytocin-induced contractile amplitude to 47.98%, single salbutamol application resulted in amplitudinal decrease to 56.07%, and the combination of both compounds in their simultaneous administration resulted in the decrease of oxytocin-induced contractile amplitude to 29.1%.

CONCLUSION

Our data are consistent with previous studies of the enhanced efficiency of the beta(2)-adrenergic agonist, when administered together with the phosphodiesterase 4-inhibitor. Moreover we have shown that rolipram alone has a more profound effect on oxytocin-induced contractions than salbutamol alone.

摘要

背景

本研究的目的是观察磷酸二酯酶4选择性抑制剂原型咯利普兰对催产素诱导的足月人子宫肌条收缩的影响，并比较其与β2肾上腺素能激动剂沙丁胺醇单独及联合应用时的效果。

方法

从足月剖宫产的孕妇获取人子宫肌层。从子宫下段切取子宫肌条，置于含Krebs-Henseleit缓冲液的器官浴槽中。以子宫肌条平滑肌对催产素（10⁻⁶ mmol/L⁻¹）剂量的平均收缩峰值幅度（mN），随后单独给予咯利普兰（10⁻⁴ mmol/L⁻¹）、沙丁胺醇（10⁻⁴ mmol/L¹）以及联合给予咯利普兰和沙丁胺醇（均为10⁻⁴ mmol/L⁻¹）后的平均收缩峰值幅度作为子宫肌反应性的参数。