Superiority of pulmonary administration of mepenzolate bromide over other routes as treatment for chronic obstructive pulmonary disease.
Superiority of pulmonary administration of mepenzolate bromide over other routes as treatment for chronic obstructive pulmonary disease.
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DOI：
10.1038/srep04510
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发表时间：
2014-03-28
影响因子：
4.6
通讯作者：
Mizushima T
中科院分区：
文献类型：
--
作者：
Tanaka K;Kurotsu S;Asano T;Yamakawa N;Kobayashi D;Yamashita Y;Yamazaki H;Ishihara T;Watanabe H;Maruyama T;Suzuki H;Mizushima T
我们最近提出，由于其抗炎和支气管扩张活性，甲苯唑酸盐溴化（甲苯唑酸盐）可能是治疗慢性阻塞性肺疾病（COPD）的有效药物。在这项研究中，我们研究了不同给药途径对小鼠的益处和副作用。口服甲哌唑酯不仅能引起支气管扩张，而且能降低弹性酶所致肺气肿的严重程度；然而，与气管内给药方式相比，达到这一效果所需的剂量约高5000倍。静脉注射或直肠注射甲哌唑酸盐也显示出这些药理作用。气管内给药，而不是其他途径，对弹性酶诱导的肺损伤和支气管扩张有保护作用，剂量远低于影响排便和心率的剂量。这些结果表明，肺途径给药美苯唑酸可能优于其他途径（口服、静脉或直肠内）治疗COPD患者。
We recently proposed that mepenzolate bromide (mepenzolate) would be therapeutically effective against chronic obstructive pulmonary disease (COPD) due to its both anti-inflammatory and bronchodilatory activities. In this study, we examined the benefits and adverse effects associated with different routes of mepenzolate administration in mice. Oral administration of mepenzolate caused not only bronchodilation but also decreased the severity of elastase-induced pulmonary emphysema; however, compared with the intratracheal route of administration, about 5000 times higher dose was required to achieve this effect. Intravenously or intrarectally administered mepenzolate also showed these pharmacological effects. The intratracheal route of mepenzolate administration, but not other routes, resulted in protective effects against elastase-induced pulmonary damage and bronchodilation at a much lower dose than that which affected defecation and heart rate. These results suggest that the pulmonary route of mepenzolate administration may be superior to other routes (oral, intravenous or intrarectal) to treat COPD patients.
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组蛋白脱乙酰基酶2介导的糖皮质激素受体的脱乙酰基化可以抑制NF-kappab。
影响因子：
15.3
作者：
Ito, Kazuhiro;Yamamura, Satoshi;Essilfie-Quaye, Sarah;Cosio, Borja;Ito, Misako;Barnes, Peter J;Adcock, Ian M
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Adcock, Ian M
DOI：
10.1164/rccm.2103118
发表时间：
2002-08-15
影响因子：
24.7
作者：
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通讯作者：
Yoshida, M
DOI：
10.1124/jpet.111.179051
发表时间：
2011-09-01
影响因子：
3.5
作者：
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影响因子：
120.1
作者：
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影响因子：
4.3
作者：
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通讯作者：
Schols, AMWJ