的临床前药理学GW280430A (AV430A)在恒河猴和猫:mivacurium做了对比。
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Savarese JJ,贝尔蒙特先生,Hashim妈,Mook RA Jr,米堡EE, Samano V, Patel党卫军,费尔德曼PL,舒尔茨是的,McNulty M,斯皮策T,科恩DL,摩根P Wastila世行
的临床前药理学GW280430A (AV430A)在恒河猴和猫:mivacurium做了对比。
麻醉学。2004年4月,100 (4):835 - 45。
- PubMed ID
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15087618 (在PubMed]
- 文摘
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背景:没有替代琥珀酰胆碱是可用的。GW280430A (AV430A)是一个代表一个新类的去极化神经肌肉阻断药物称为不对称mixed-onium chlorofumarates。它经历了快速降解在等离子体化学水解和失活的半胱氨酸内收,结果在很短的时间效应。心血管,神经肌肉和自主药理学与mivacurium GW280430A比这里。方法:成年雄性恒河猴和成年雄性猫和一氧化二氮麻醉oxide-oxygen-halothane chloralose-pentobarbital,分别。GW280430A的神经肌肉阻断性质和mivacurium比较刺激的速率的0.15赫兹的脚伸肌肌腱牵向前(猴子)和胫骨前(猫)。交感神经反应化验在瞬膜制备、猫和迷走神经的影响进行评估通过观察猫的心搏徐缓的反应刺激后颈迷走神经。结果:GW280430A和mivacurium均等的猴子在每种情况下(ED95 0.06毫克/公斤)。GW280430A mivacurium一半强大的猫。行动的总持续时间mivacurium GW280430A是不到一半的猴子; recovery slopes were more than twice as rapid. The 25-75% recovery index of GW280430A did not vary significantly after various bolus doses or infusions, averaging 1.4-1.8 min in the monkey, significantly shorter than the same time interval (4.8-5.7 min) for mivacurium. Dose ratios for autonomic versus neuromuscular blocking properties in the cat were greater than 25 for both GW280430A and mivacurium. The ratio ED Hist:ED95 Neuromuscular Block in the monkey was significantly greater (approximately 53 vs. 13) for GW280430A, indicating approximately four times less relative prominence of the side effects of skin flushing and decrease of blood pressure, which are associated with release of histamine. CONCLUSIONS: These experiments show a much shorter neuromuscular blocking effect and much-reduced side effects in the case of GW280430A vis-a-vis mivacurium. These results, together with the novel chemical degradation of GW280430A, suggest further evaluation in human subjects.
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- 药物