St-Louis J
Pharmacology. 1982;25(6):327-37. doi: 10.1159/000137759.
The present experiments were designed to elucidate the pharmacological mechanism of the relaxing action of the ovarian hormone, relaxin, upon KCl-contracted rat uteri in vitro. Rat uterine segments were made to contract by superfusion with a physiological solution, in which 15% of the normal NaCl content had been replaced by an equimolar amount of KCl. The effect of relaxin, in reversing this contraction, was achieved in part by a direct action upon the tissue and in part (about 45% at the concentration of relaxin used) by the liberation of endogenous catecholamines which relax the uterus via beta-adrenergic activity. The effect of relaxin was reduced by propranolol, and it was not blocked by indomethacin, cimetidine or diphenhydramine. The effect of the ovarian peptide on uterine segments was potentiated in the presence of theophylline and indomethacin in the superfusing fluid. This effect of theophylline was shown to be insensitive to beta-adrenergic blockade. The results suggest that relaxin relaxes the KCl-contracted rat uterus in part by a direct inhibitory action upon the uterine muscle and in part by facilitating the release of intramural catecholamines. It is also suggested that relaxin may act via the production of cyclic AMP.
本实验旨在阐明卵巢激素松弛素对氯化钾收缩的大鼠离体子宫的舒张作用的药理机制。通过用生理溶液进行灌流使大鼠子宫段收缩,该生理溶液中15%的正常氯化钠含量已被等摩尔量的氯化钾替代。松弛素逆转这种收缩的作用部分是通过对组织的直接作用,部分(在所使用的松弛素浓度下约为45%)是通过内源性儿茶酚胺的释放,这些儿茶酚胺通过β-肾上腺素能活性使子宫舒张。普萘洛尔可降低松弛素的作用,而吲哚美辛、西咪替丁或苯海拉明不能阻断其作用。在灌流液中存在茶碱和吲哚美辛时,卵巢肽对子宫段的作用增强。茶碱的这种作用显示对β-肾上腺素能阻断不敏感。结果表明,松弛素使氯化钾收缩的大鼠子宫舒张,部分是通过对子宫肌的直接抑制作用,部分是通过促进壁内儿茶酚胺的释放。还表明松弛素可能通过环磷酸腺苷的产生发挥作用。