A novel vasorelaxant effect of clonixinate of L-lysine (Clx), analgesic and anti-inflammatory, was studied in rat aortic rings. 2. Clx completely relaxed aortic rings contracted by KCl 70 mM and together with its analog flunixin exhibited lesser potency but equal efficacy than verapamil. In comparison, indomethacin, which is a more potent cyclo-oxygenase inhibitor relaxed only about 40% of the maximal contraction of aortic rings. 3. Furthermore, Clx antagonized Ca2+ dependent aortic contraction and BAY K-8644 induced aortic contraction suggesting its calcium antagonist character. 4. From these results it can be concluded that the hypotensive effect seen in rats in vivo after Clx i.v. injection arises because of vasodilatory effect of Clx and gives further support to the proposal that the pharmacological mechanism of action of Clx should be calcium antagonism.
摘要
研究了L-赖氨酸氯尼辛酯（Clx）的一种新型血管舒张作用，它具有镇痛和抗炎作用，实验对象为大鼠主动脉环。2. Clx能使由70 mM氯化钾引起收缩的主动脉环完全舒张，与其类似物氟尼辛相比，效力较弱但疗效与维拉帕米相当。相比之下，更强效的环氧化酶抑制剂吲哚美辛仅能使主动脉环最大收缩幅度舒张约40%。3. 此外，Clx拮抗钙依赖性主动脉收缩和BAY K - 8644诱导的主动脉收缩，表明其具有钙拮抗剂特性。4. 从这些结果可以得出结论，静脉注射Clx后在大鼠体内观察到的降压作用是由于Clx的血管舒张作用，这进一步支持了Clx的药理作用机制应为钙拮抗作用的观点。
