Hutchings G, Deprest J, Nilius B, Roskams T, De Ridder D
Department of Obstetrics and Gynaecology, University Hospital Gasthuisberg, Leuven, Belgium.
Gynecol Obstet Invest. 2006;62(2):79-83. doi: 10.1159/000092530. Epub 2006 Apr 3.
C-kit receptor expressing interstitial cells generate and coordinate the electrical signals that control peristalsis in the gut. However, the function of interstitial cells in the myometrium is not known.
(1) Sections of rabbit myometrium were subjected to immunohistochemical staining for the c-kit receptor. (2) Spontaneously contracting myometrial strips from New Zealand White rabbits near term were mounted in an organ bath and attached to a tension-recording device. The effect of increased concentrations of the c-kit receptor antagonist imatinib mesylate on these contractions was observed. The main outcome measures were the change in frequency, amplitude and duration of contraction.
(1) Multipolar cells expressing c-kit were identified in the fibromuscular septum confirming the presence of interstitial cells in rabbit myometrium. (2) Imatinib decreased the amplitude of contractions by approximately 20% at 100 microM. No effect was seen at lower concentrations. No effect of imatinib on frequency or duration of contractions was observed at any of the concentrations studied.
In isolated rabbit myometrium, acute inhibition of the c-kit receptor by imatinib mesylate affects only the amplitude of spontaneous contractions at concentrations, the equivalent of x10-100 the normal therapeutic concentration.
表达C-kit受体的间质细胞产生并协调控制肠道蠕动的电信号。然而，间质细胞在子宫肌层中的功能尚不清楚。
（1）对兔子宫肌层切片进行C-kit受体免疫组化染色。（2）将接近足月的新西兰白兔的自发性收缩子宫肌条置于器官浴槽中，并连接到张力记录装置上。观察C-kit受体拮抗剂甲磺酸伊马替尼浓度增加对这些收缩的影响。主要观察指标为收缩频率、幅度和持续时间的变化。
（1）在纤维肌隔中鉴定出表达C-kit的多极细胞，证实兔子宫肌层中存在间质细胞。（2）在100微摩尔浓度下，伊马替尼使收缩幅度降低约20%。在较低浓度下未观察到影响。在任何研究浓度下，均未观察到伊马替尼对收缩频率或持续时间的影响。
在离体兔子宫肌层中，甲磺酸伊马替尼对C-kit受体的急性抑制仅在相当于正常治疗浓度10-100倍的浓度下影响自发性收缩的幅度。
