体内的催产素拮抗剂的活动在大鼠子宫活动。
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安TG,韩寒SJ,曹y, Pak SC, Flouret G
体内的催产素拮抗剂的活动在大鼠子宫活动。
体内。2004;11 - 12月18 (6):763 - 6。
- PubMed ID
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15646817 (在PubMed]
- 文摘
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催产素拮抗剂(OTA), tt - 235,是由我们组和显示抑制自发或oxytocin-induced灵长类动物的子宫收缩。本研究的目的是确定的时间tt - 235块oxytocin-induced发情大鼠子宫收缩。在实验1中,三个在线旅行社的时间响应子宫收缩性检查。老鼠在颈静脉麻醉和套管被注入车辆(无菌生理盐水),Antag我Antag二世和tt - 235。子宫活动监控通过水balloon-tipped套管放在子宫角。子宫收缩活动确定的综合区域10分钟。每个在线旅行社管理作为单个丸注入5 microg,紧随其后的是100亩催产素5分钟后,也作为一个丸。催产素注射相同剂量的重复每小时5小时。实验2确定三个在线旅行社的影响子宫催产素受体数量(Rn)和亲和力(Kd)。老鼠接受在线旅行社或车辆被牺牲在受体分析0.5和4个小时。 In Experiment 1, Antag I, Antag II and TT-235 inhibited the integrated uterine response to oxytocin at 5 minutes by 76%, 77% and 80%, respectively, compared to controls (p<0.05). Two hours after injecting Antag I, inhibition of uterine contractility was 55% lower than controls (p<0.05). At 3 hours, uterine contractility was no longer affected in rats treated with Antag I compared with controls. The suppressive uterine activity with Antag II continued up to 3 hours. However, uterine contractility remained lower (53%) in rats treated with TT-235 5 hours later. In Experiment 2, TT-235 induced a significant decrease (p<0.05) in oxytocin receptor number and binding affinity at both 0.5 and 4 hours compared with controls. Antag I and Antag II did not alter oxytocin receptor number or binding affinity significantly at each time point studied compared with controls. In conclusion, TT-235 may inhibit the uterine response to oxytocin by decreasing oxytocin receptor numbers and oxytocin binding affinity, which might explain the prolonged oxytocin antagonist activity of TT-235.