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首页> 外文期刊>Life sciences >Effects of methylecgonidine on acetylcholine-induced bronchoconstriction and indicators of lung injury in guinea pigs.
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Effects of methylecgonidine on acetylcholine-induced bronchoconstriction and indicators of lung injury in guinea pigs.

机译：甲基乙草胺对乙酰胆碱诱导的豚鼠支气管收缩的影响和肺损伤指标。

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The fumarate salt of methylecgonidine (MEG; anhydroecgonine methylester), a pyrolysis product of cocaine, has previously been shown to antagonize contractions of guinea pig isolated trachea induced by acetylcholine (ACh) and other spasmogenics. We determined the effects of MEG fumarate on ACh-induced bronchoconstriction in vivo. Specific airway conductance (SGaw) was measured in guinea pigs receiving 30-300 mg/kg s.c. MEG fumarate and exposed one hour later to nebulized ACh (0.2-3.2%; by inhalation). MEG fumarate did not induce any changes in SGaw; neither did it antagonize dose-dependent decreases in SGaw induced by ACh. However, tremors, salivation, startle and increased numbers of fecal boli were observed after MEG administration. Thus, unlike antagonism of ACh-induced contractions of guinea pig isolated trachea observed in vitro, MEG fumarate does not antagonize ACh-induced bronchoconstriction in vivo, even at doses which induced changes in grossly-observable behavior. Inhalation of a condensation aerosol of MEG base induced lung damage as evidenced by the presence of blood and higher levels of protein and lactate dehydrogenase in the lung lavage fluid of MEG-treated animals than of control animals. Aerosols of MEG fumarate, on the other hand, did not induce lung damage when inhaled. These results extend previous observations that MEG base may contribute to detrimental pulmonary effects of crack smoking.
机译：以前已显示可卡因的热解产物甲基乙草胺的富马酸盐（MEG;脱水乙草胺甲酯）可拮抗乙酰胆碱（ACh）和其他引起痉挛的豚鼠分离出的气管收缩。我们确定了富马酸MEG对ACh诱导的体内支气管收缩的影响。在接受30-300 mg / kg s.c.的豚鼠中测量比气道电导（SGaw）。 MEG富马酸酯，一小时后暴露于雾化的ACh（0.2-3.2％;吸入）。富马酸MEG不会引起SGaw的任何改变;它也没有拮抗ACh诱导的SGaw剂量依赖性下降。然而，MEG给药后观察到震颤，流涎，惊吓和粪便数量增加。因此，与在体外观察到的ACh诱导的豚鼠离体气管收缩的拮抗作用不同，即使在一定剂量下，MEG富马酸酯在体内也不会拮抗ACh诱导的支气管收缩，即使在引起可观察到的行为改变的剂量下也是如此。吸入MEG碱的凝结气溶胶可引起肺损伤，这是通过MEG处理动物的肺灌洗液中血液的存在以及蛋白质和乳酸脱氢酶的水平高于对照动物来证明的。另一方面，MEG富马酸酯的气雾剂在吸入时不会引起肺损伤。这些结果扩展了以前的观察结果，即MEG碱可能对裂解烟的肺部有害作用。

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