NITRIC OXIDE-ASSOCIATED VASORELAXING EFFECT OF AN ANTIULCER AGENT, BENEXATE HYDROCHLORIDE BETADEX
NITRIC OXIDE-ASSOCIATED VASORELAXING EFFECT OF AN ANTIULCER AGENT, BENEXATE HYDROCHLORIDE BETADEX
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DOI：
10.1002/ddr.430360103
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发表时间：
1995-09-01
影响因子：
3.8
通讯作者：
MATSUNAGA, K
中科院分区：
文献类型：
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作者：
IWASAKI, T;MATSUNAGA, K
在有内皮和无内皮的大鼠胸主动脉环中检测了盐酸贝奈克酯倍他环糊精（BHB）的血管舒张作用。1 - 100 μM的BHB在苯肾上腺素（1 μM）预收缩的有内皮和去内皮的主动脉中均引起浓度依赖性的血管舒张，其在有内皮的主动脉中的舒张作用明显更强。BHB这种部分内皮依赖性血管舒张被一氧化氮（NO）合酶抑制剂N - ω - 硝基 - L - 精氨酸甲酯（100 μM）和NO清除剂血红蛋白（10 μM）显著抑制，但不被环氧化酶抑制剂吲哚美辛（5 μM）抑制。用BHB（30 μM）处理的有内皮主动脉中NO的第二信使c - GMP的含量较对照水平显著增加约两倍。100 μM的BHB处理后的NO合酶（NOS）活性增加到与10 μM的L - 精氨酸处理后大致相同的水平。综上所述，这些结果表明BHB的血管舒张作用部分与内皮的NO合成和释放有关，而与前列腺素系统无关。BHB引起内皮NO合成和释放的机制可能是通过作为NOS的底物发挥作用从而激活NOS。（C）1995威利 - 利斯公司
The vasorelaxing effect of benexate hydrochloride betadex (BHB) was examined in rat thoracic aortic ring with and without endothelium. BHB at 1 similar to 100 mu M caused concentration-dependent vasorelaxation in both endothelium-intact and -denuded aortas precontracted with phenylephrine (1 mu M), with its relaxing effect being significantly more potent in the endothelium-intact aorta. This partial endothelium-dependent vasorelaxation by BHB was significantly inhibited by N-omega-nitro-L-arginine methylester (100 mu M), an inhibitor of nitric oxide (NO) synthase, and hemoglobin (10 mu M), an NO scavenger, but not by indomethacin (5 mu M), an inhibitor of cyclooxygenase. The content of c-GMP, a second messenger of NO, in endothelium-intact aorta treated with BHB (30 mu M) significantly increased by about twofold of the control level. NO synthase (NOS) activity by the treatment of BHB at 100 mu M increased to about the same level by the treatment of L-arginine at 10 mu M. Taken together, these results suggest that the vasorelaxing effect of BHB is, in part, associated with NO synthesis and release from the endothelium but not with the prostaglandin system. The mechanism of NO synthesis and release from the endothelium by BHB might be NOS activation by the effect as a substrate of NOS. (C) 1995 Wiley-Liss, Inc.