张毅, 叶益新, 乔小英. 羟苯氨酮对心肌肌钙蛋白C与Ca2+亲和力的影响J. 药学学报, 1999, 34(9): 658-661.
引用本文: 张毅, 叶益新, 乔小英. 羟苯氨酮对心肌肌钙蛋白C与Ca2+亲和力的影响J. 药学学报, 1999, 34(9): 658-661.
Zhang Yi, Ye Yixin , Qiao Xiaoying, . EFFECT OF OXYPHENAMONE ON CA2+ AFFNITY OF CARDIAC TROPONIN CJ. Acta Pharmaceutica Sinica, 1999, 34(9): 658-661.
Citation: Zhang Yi, Ye Yixin , Qiao Xiaoying, . EFFECT OF OXYPHENAMONE ON CA2+ AFFNITY OF CARDIAC TROPONIN CJ. Acta Pharmaceutica Sinica, 1999, 34(9): 658-661.

羟苯氨酮对心肌肌钙蛋白C与Ca2+亲和力的影响

EFFECT OF OXYPHENAMONE ON CA2+ AFFNITY OF CARDIAC TROPONIN C

  • 摘要: 目的:探讨羟苯氨酮(oxyphenam one , Oxy) 的钙增敏机理。方法:从牛心肌组织中提取cTn C,采用荧光探针标记法观察Oxy 对c Tn C与Ca2+ 亲和力的影响,并和已知的钙增敏剂 MCI-154 、磺甲唑(sulmazole , Sul) 作比较。结果: Oxy 显著增加cTn C和Ca2+ 的亲和力,且呈剂量与效应相关。而50 μm ol·L-1 MCI-154 或Sul 对cTn C和Ca2+亲和力曲线均无显著影响。结论: Oxy 的钙增敏机理可能与直接增加cTn C与Ca2+ 的亲和力有关。

     

    Abstract: AIM: To explore the molecular mechanism of the calcium sensitizing effect of oxyphenamone(Oxy). METHODS: Cardiac troponin C(cTn C) was purified from cattle cardiac muscle and labeled with fluorescent probe, dansyl chloride. The effect of Oxy on the affinity of cTn C to Ca2+ was studied and compared with those of MCI 154 and sulmazole(Sul). RESULTS: Oxy was shown to improve the affinity of Ca2+ dose dependently. Oxy 10 μmol·L -1 slightly shifted the cTn C—Ca 2+ affinity curve to the left, but showed no significance while Oxy 25 μmol·L-1 significantly shifted the curve to the left. Oxy 50 μmol·L-1 showed more potent action, shifting the affinity curve to the left by 0.2 pCa unit. In contrast, MCI 154 or Sul 50 μmol·L-1 showed no significant influence on the affinity curve. CONCLUSION: These results suggest that the positive inotropic action of Oxy on cardiac muscle is, at least, partially mediated by increasing the sensitivity of cTn C to Ca2+, the calcium sensitizing effect of MCI-154 and Sul may be mediated otherwise besides directly increasing the affinity of cTn C to Ca2+.

     

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