Berg G, Andersson R G, Rydén G
Am J Obstet Gynecol. 1985 Feb 1;151(3):392-6. doi: 10.1016/0002-9378(85)90310-2.
The concentration of available beta-adrenoceptors has been studied in the myometrium of women treated with terbutaline for premature uterine contractions and in an untreated control group. Myometrial strips were taken at cesarean section from the lower uterine segment and the uterine fundus. The concentration of beta-adrenoceptors was determined with a radioligand binding assay. In untreated women we found no difference in the concentration of beta-adrenoceptors in the uterine fundus compared to that in the lower uterine segment. The cyclic adenosine monophosphate production after beta-adrenoceptor agonist stimulation in vitro was equal in both locations. In the terbutaline-treated women, the binding site concentrations in both the fundus and lower uterine segment were lower compared to those in the control group. The decrease was most pronounced in the fundus where receptor concentration was only half that found in the control group. The results suggest that treatment with beta-mimetics causes a desensitization in the beta-adrenoceptor system of human myometrium during pregnancy. This desensitization may partly explain the limited duration of the relaxant effect of beta-mimetics often seen in the treatment of preterm labor.
已对用特布他林治疗子宫过早收缩的女性子宫肌层以及未治疗的对照组子宫肌层中可用β-肾上腺素能受体的浓度进行了研究。在剖宫产时从子宫下段和子宫底部获取子宫肌条。用放射性配体结合试验测定β-肾上腺素能受体的浓度。在未治疗的女性中,我们发现子宫底部β-肾上腺素能受体的浓度与子宫下段相比没有差异。体外β-肾上腺素能受体激动剂刺激后环磷酸腺苷的产生在两个部位是相等的。在接受特布他林治疗的女性中,子宫底部和子宫下段的结合位点浓度均低于对照组。这种降低在子宫底部最为明显,其受体浓度仅为对照组的一半。结果表明,β-拟交感神经药治疗会导致孕期人子宫肌层β-肾上腺素能受体系统脱敏。这种脱敏可能部分解释了在早产治疗中经常看到的β-拟交感神经药松弛作用持续时间有限的现象。