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蝌蚪中阿法沙龙/阿法多龙和甲己炔巴比妥的压力逆转:全身麻醉不同分子位点的证据

Pressure reversal of alphaxalone/alphadolone and methohexitone in tadpoles: evidence for different molecular sites for general anaesthesia.

作者信息

Halsey M J, Wardley-Smith B, Wood S

出版信息

Br J Pharmacol. 1986 Oct;89(2):299-305. doi: 10.1111/j.1476-5381.1986.tb10260.x.

Abstract

Tadpoles were used to study quantitative interactions between high pressure and two intravenous anaesthetics, alphaxalone/alphadolone and methohexitone. The potencies of the two agents were decreased by high pressure but to different extents. The maximum effect was seen in the pressure range 70-130 atmospheres absolute (ATA). The increases in the normobaric anaesthetizing concentration (ED50) required at 100 ATA were alphaxalone/alphadolone:405 +/- 5 (s.d.)%; methohexitone:658 +/- 80 (s.d.)%. For both alphaxalone/alphadalone and methohexitone, the curves obtained when the increase in ED50 was plotted against increasing pressure showed plateaux at pressures above 70 ATA. These data support the concept of the two intravenous drugs causing general anaesthesia by the occupation of separate molecular 'sites' with different but finite capacities.

摘要

蝌蚪被用于研究高压与两种静脉麻醉剂(α-羟孕酮/α-孕烷二酮和甲己炔巴比妥)之间的定量相互作用。两种药物的效能均因高压而降低,但程度不同。在绝对压力70-130个大气压(ATA)范围内观察到最大效应。在100 ATA时所需的常压麻醉浓度(ED50)增加量为:α-羟孕酮/α-孕烷二酮:405±5(标准差)%;甲己炔巴比妥:658±80(标准差)%。对于α-羟孕酮/α-孕烷二酮和甲己炔巴比妥,当将ED50的增加量与压力增加量作图时得到的曲线在压力高于70 ATA时显示出平台期。这些数据支持了这两种静脉药物通过占据具有不同但有限容量的单独分子“位点”而导致全身麻醉的概念。

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Molecular mechanisms of general anaesthesia.全身麻醉的分子机制
Nature. 1982 Dec 9;300(5892):487-93. doi: 10.1038/300487a0.

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