摘要
目的比较和分析不同类型有效浓度的β受体拮抗剂对肾上腺素的拮抗作用。方法用氚（Ｈ３）标记的环磷酸腺苷（ａｄｅｎｏｓｉｎｅ３′，Ｓ′－ｍｏｎｏｐｈｏｓｈａｔｅ，ｃＡＭＰ），以蛋白竞争结合法测定细胞内ｃＡＭＰ的含量。结果（１）撤除１０－５ｍｏｌ／Ｌ非选择性β受体拮抗剂噻吗心安（ｔｉｍｏｌｏｌ）后，５小时内肾上腺素对小梁细胞ｃＡＭＰ的作用无明显恢复。撤除１０－６ｍｏｌ／Ｌ噻吗心安后５小时内，肾上腺素的作用仅部分恢复。（２）撤除选择性β２受体拮抗剂ＩＣＩ１１８，５５１（１０－５ｍｏｌ／Ｌ，１０－６ｍｏｌ／Ｌ）后，５小时肾上腺素的作用部分恢复。（３）撤除１０－５ｍｏｌ／Ｌ选择性β１受体拮抗剂比索洛尔（ｂｉｓｏｐｒｏｌｏｌ）后，１５分钟肾上腺素的作用即有明显恢复。结论噻吗心安和ＩＣＩ１１８，５５１对肾上腺素的拮抗作用强，时间持久；比索洛尔对肾上腺素的拮抗作用弱，持续时间短。根据实验结果推测牛眼小梁细胞上存在β受体，且以β２受体为主。
Objective To compare and assay the effects of various β adrenergic antagonists at effective concentrations on epinephrine (EPI). Method Cyclic adenosine 3′,5′ monophosphate (cAMP) in trabecular cells was measured by protein binding assay with 3H cAMP. Results (1) The effect of EPI increasing cAMP in bovine trabecular cells (BTC) in vitro did not obviously recover at the fifth hour after the removal of 10 -5 mol/L timolol, and partly recovered at the fifth hour after the removal of 10 -6 mol/L timolol. (2) There was only part recovery for the effect of EPI at the fifth hour after the removal of ICI 118, 551 (10 -5 mol/L, and 10 -6 mol/L). (3) There was an obvious recovery for the effect of EPI at the fiftenth minute after the removal of 10 -5 mol/L bisoprolol. Conclusion The effect of timolol and ICI 118, 551 for blocking EPI is strong and sustained; bisoprolol produces a smaller blockade to the effect of EPI, lasting a short time. Our results also presume that BTC contains β adrenergic receptors, and β 2 adrenergic receptors are dominant.
出处
《中华眼科杂志》
CAS
CSCD
北大核心
1997年第5期373-375,共3页
Chinese Journal of Ophthalmology
