钙拮抗剂TMB-8抑制BHQ,NE和KCl引起的培养乳牛基底动脉单个平滑肌细胞内游离钙的升高

• 作 者: 王斌 张孝清 王金唏 杨思军 肖继皋
• 机 构: 南京医科大学药理教研室,南京大学配位化学国家重点实验室
• 出 处: 药学学报
• 发表日期: 1997年11期
• 关键词: 基底动脉 NE KCl TMB-8 内游离钙 平滑肌细胞 钙拮抗剂 细胞外钙 二乙胺 肌浆网

用ＡＲＣＭＭＩＣ阳离子测定系统，测量单个细胞内游离钙浓度（［Ｃａ２＋］ｉ），研究８（Ｎ，Ｎ二乙胺）ｎ辛基３，４，５三甲氧基苯甲酸酯（ＴＭＢ８）对培养乳牛基底动脉平滑肌［Ｃａ２＋］ｉ的作用。在细胞外钙浓度为１３ｍｍｏｌ·Ｌ－１时，ＴＭＢ８（３０μｍｏｌ·Ｌ－１）可明显抑制ＢＨＱ，ＮＥ及ＫＣｌ引起［Ｃａ２＋］ｉ的升高。在细胞外钙为零＋ＥＧＴＡ０１ｍｍｏｌ·Ｌ－１时，ＴＭＢ８（１０，３０及１００μｍｏｌ·Ｌ－１）可浓度依赖性地降低静息［Ｃａ２＋］ｉ，ＴＭＢ８（３０μｍｏｌ·Ｌ－１）可几乎完全阻断ＢＨＱ及ＮＥ引起［Ｃａ２＋］ｉ的增加。研究表明ＴＭＢ８降低培养乳牛基底动脉平滑肌［Ｃａ２＋］ｉ的机制，主要是抑制肌浆网Ｃａ２＋的释放，或增加肌浆网对Ｃａ２＋的摄入，并由此间接地抑制细胞外钙的内流。

AR  CM  MCIC cation measurement system, measuring intracellular free calcium concentration ([Ca2] i), the study 8  (N, N  diethyl)  n  octyl  3,4,5  trimethoxy Effect of TMB8 on [Ca2 +] i in cultured basilar artery smooth muscle of dairy cattle. TMB 8 (30μmol·L-1) significantly inhibited the increase of [Ca2 +] i induced by BHQ, NE and KCl when the extracellular calcium concentration was 13mmol·L-1. TMB 8 (10, 30 and 100 μmol·L-1) decreased the concentration of resting [Ca2 +] i, TMB8 (30 μmol·L-1) in a concentration-dependent manner when the extracellular calcium was zero + EGTA01 mmol·L- 1) can almost completely block the increase of [Ca2 +] i caused by BHQ and NE. Studies have shown that the mechanism of TMB-8 lowering cultured [Ca2 +] i in basilar artery of dairy cow is mainly to inhibit the release of Ca2 + in sarcoplasmic reticulum, or to increase the uptake of Ca2 + by sarcoplasmic reticulum and thereby indirectly inhibit the extracellular calcium flow.