| 大鼠体内硝基精氨酸的手性代谢动力学 |
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| 引用本文： | 辛艳飞,童睿,方扬,周向军,王永祥.大鼠体内硝基精氨酸的手性代谢动力学[J].中国药理学通报,2005,21(1):38-41. |
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| 作者姓名： | 辛艳飞 童睿 方扬 周向军 王永祥 |
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| 作者单位： | 上海交通大学药学院分子药理学实验室,上海,200030 |
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| 摘 要： | 目的 应用毛细管电色谱 (CEC)对大鼠体内的硝基精氨酸手性转化和代谢动力学进行研究。方法 采用手性配体交换法检测大鼠血浆中D型硝基精氨酸 (D NNA)和L型硝基精氨酸(L NNA)的浓度,应用非房室模型对所获得的血药浓度-时间数据进行拟合,计算药动学参数。结果 D NNA和L NNA在大鼠体内代谢具有明显的异构体选择性,清除率分别为(0 46±0 02)ml·h-1·kg-1和(0 17±0 03)ml·h-1·kg-1 (P<0 05 );T1 /2分别为 ( 1 44±0 28 )h和(3 48±0 41)h(P<0 05)。D NNA到L NNA的单项手性转化率为(50 03±8 5)%。结论 D NNA和L NNA在大鼠体内的代谢有明显的异构体选择性 (其差异可能主要源于D NNA到L NNA的单向手性转化)。
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| 关 键 词： | DNNA LNNA 毛细管电色谱 手性转化 手性动力学 |
| 文章编号： | 1001-1978(2005)01-0038-04 |
| 修稿时间： | 2004年8月18日 |
Chiral pharmacokinetics and inversion of NG-nitro-arginine in rats |
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| XIN Yan-fei,TONG Rui,FANG Yang,ZHOU Xiang-jun,WANG Yong-xiang.Chiral pharmacokinetics and inversion of NG-nitro-arginine in rats[J].Chinese Pharmacological Bulletin,2005,21(1):38-41. |
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| Authors: | XIN Yan-fei TONG Rui FANG Yang ZHOU Xiang-jun WANG Yong-xiang |
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| Abstract: | Aim To explore pharmacokinetics of NG-nitro-D -arginine (D-NNA)and NG-nitro-L-arginine (L-NNA)in conscio us rats. Methods The plasma concentration of D-NNA and L -NNA were determined by chiral ligand exchange method with capillary electroc hromatography (CEC). Pharmacokinetic parameters were obtained using non-compart ment model and were fitted using a computer program DAS. Results The metabolism of D-NNA and L-NNA exhibited significant isomeric sel ectivity. The CL and T 1/2 of D-NNA and D-NNA were(0.46±0. 02) ml·h -1·kg -1 vs (0.17±0.03) ml· h -1·kg -1( P<0.05)and (1.44±0.28) h vs (3.48±0.41) h (P<0.05), respect ively. Unidirectional chiral conversion rate of D-NNA to L-NNA was (50 .03±8.5)%. Conclusion The stereoselective pharmacokinetics of NG-nitro-arginine observed maybe due to the unidirectional chiral inversion of D-NNA to L-NNA. |
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| Keywords: | D-NNA L-NNA |
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