U46619、前列腺素F2α、拉坦前列素和曲伏前列素在离体猪睫状动脉中的血管活性反应

Vasoactive responses of U46619, PGF2alpha, latanoprost, and travoprost in isolated porcine ciliary arteries.

作者信息

Vysniauskiene Ineta, Allemann Reto, Flammer Josef, Haefliger Ivan O

机构信息

Laboratory of Pharmacology and Physiology, University Eye Clinic, Basel, Switzerland.

出版信息

Invest Ophthalmol Vis Sci. 2006 Jan;47(1):295-8. doi: 10.1167/iovs.05-0760.

DOI:10.1167/iovs.05-0760

PMID:16384976

Abstract

PURPOSE

To compare the vasoactive properties of the prostanoids U46619 (thromboxane A2 analogue), prostaglandin F(2alpha) (PGF(2alpha)), latanoprost free acid, and travoprost free acid in isolated porcine ciliary arteries.

METHODS

In a myograph system (isometric force measurement), quiescent vessels were exposed (cumulatively) to U46619, PGF(2alpha), latanoprost, or travoprost (0.1 nM-0.1 mM). Experiments were also conducted in the presence of SQ 29548 (TP-receptor antagonist; 3-10 microM) or AL-8810 (FP-receptor antagonist; 3-30 microM). Contractions were expressed as the percentage of 100 mM potassium chloride-induced contractions.

RESULTS

In quiescent vessels, contractions (concentration-response curves) induced by (0.1 mM) PGF(2alpha) (87.9% +/- 3.5%), U46619 (66.7% +/- 4.1%), and latanoprost (62.9% +/- 3.6%) were more pronounced (P < or = 0.001) than those induced by travoprost (23.0% +/- 4.4%). Concentration-response curves for PGF(2alpha), latanoprost, and travoprost were preceded by a smaller contraction peak (0.1 microM) that was higher (P < or = 0.05) for travoprost (24.4% +/- 2.8%) than for PGF(2alpha) (12.9% +/- 4.6%), but not different (P = 0.58) from latanoprost (22.0% +/- 3.0%). The 50% maximal contraction (PD50: negative log M concentration) of U46619 (-8.05 +/- 0.13) was lower (P < or = 0.001) than those of latanoprost (-5.65 +/- 0.10), PGF(2alpha) (-5.49 +/- 0.14), and travoprost (-5.12 +/- 0.52). Contractions were inhibited (P < or = 0.05-0.001) either by SQ 29548 or AL-8810.

CONCLUSIONS

In isolated porcine ciliary arteries, all prostanoids tested induced contractions. Among them, travoprost appeared to be the least potent and U46619 the most efficient.

摘要

目的

比较前列腺素U46619（血栓素A2类似物）、前列腺素F(2α)（PGF(2α)）、雷珠单抗游离酸和曲伏前列素游离酸在离体猪睫状动脉中的血管活性特性。

方法

在肌动描记系统（等长力测量）中，将静态血管（累积地）暴露于U46619、PGF(2α)、雷珠单抗或曲伏前列素（0.1 nM - 0.1 mM）。实验也在存在SQ 29548（TP受体拮抗剂；3 - 10 μM）或AL - 8810（FP受体拮抗剂；3 - 30 μM）的情况下进行。收缩以100 mM氯化钾诱导收缩的百分比表示。

结果

在静态血管中，（0.1 mM）PGF(2α)（87.9% ± 3.5%）、U46619（66.7% ± 4.1%）和雷珠单抗（62.9% ± 3.6%）诱导的收缩（浓度 - 反应曲线）比曲伏前列素（23.0% ± 4.4%）诱导的收缩更明显（P ≤ 0.001）。PGF(2α)、雷珠单抗和曲伏前列素的浓度 - 反应曲线之前有一个较小的收缩峰值（0.1 μM），曲伏前列素（24.4% ± 2.8%）的该峰值高于PGF(2α)（12.9% ± 4.6%）（P ≤ 0.05），但与雷珠单抗（22.0% ± 3.0%）无差异（P = 0.58）。U46619的50%最大收缩（PD50：负对数M浓度）（-8.05 ± 0.1）低于雷珠单抗（-5.65 ± 0.10）、PGF(2α)（-5.49 ± 0.14）和曲伏前列素（-5.12 ± 0.52）（P ≤ 0.001）。收缩被SQ 29548或AL - 8810抑制（P ≤ 0.05 - 0.001）。