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等张和等长记录测量的效应比较:II. 生理性拮抗剂的浓度-效应曲线

A comparison of effects measured with isotonic and isometric recording: II. Concentration-effect curves for physiological antagonists.

作者信息

Barlow R B, Bond S M, Grant C, McQueen D S, Yaqoob Z

机构信息

Department of Neuroscience, 1 George Square, Edinburgh EH8 9JZ, Scotland, UK.

出版信息

Br J Pharmacol. 2001 Aug;133(7):1087-95. doi: 10.1038/sj.bjp.0704169.

Abstract

If one drug, B, antagonizes another, A, by producing the opposite physiological effect, the antagonist concentration-effect curves should be affected by the recording system, which limits the range of agonist responses. With pieces of isolated guinea-pig ileum taken from adjacent parts of the same animal, one recorded isotonically, the other isometrically with the same load, the isotonic IC(50) values for (-)isoprenaline opposing carbachol or histamine were lower than the isometric values (P<0.01) but there was a significant correlation between them (P<0.01): the isotonic curves were steeper (P<0.01) and there were wider shifts in IC(50) before increasing the agonist reduced the maximum relaxation. In similar experiments with pieces of rat uterus in oestrus from the same animal, the concentration-effect curves for carbachol opposed by increasing concentrations of (-)isoprenaline or (-)adrenaline had slightly lower EC(50) values with isometric recording but there was a significant correlation (P<0.01) with isotonic values. The antagonist effect (ratio of the EC(50) relative to that for the control) was higher with isotonic recording (P<0.01 for (-)isoprenaline, P<0.025 for (-)adrenaline) and all (27) curves were steeper than the corresponding isometric curve (P<0.001). The influence of the method of recording on the results is expected from the narrower operational window and smaller upper limit to relaxation with isotonic recording. A way of obtaining measurements of IC(50) against a standard agonist effect is suggested in an Appendix.

摘要

如果一种药物B通过产生相反的生理效应拮抗另一种药物A,那么拮抗剂浓度-效应曲线应该会受到记录系统的影响,因为记录系统会限制激动剂反应的范围。用取自同一只动物相邻部位的豚鼠离体肠段,一段进行等张记录,另一段在相同负荷下进行等长记录,(-)异丙肾上腺素对抗卡巴胆碱或组胺的等张IC50值低于等长记录的值(P<0.01),但二者之间存在显著相关性(P<0.01):等张曲线更陡(P<0.01),在增加激动剂降低最大舒张之前,IC50的变化幅度更大。在对同一只处于发情期的大鼠子宫进行的类似实验中,随着(-)异丙肾上腺素或(-)肾上腺素浓度增加,卡巴胆碱的浓度-效应曲线在等长记录时的EC50值略低,但与等张记录的值存在显著相关性(P<0.01)。等张记录时拮抗剂效应(EC50相对于对照的比值)更高((-)异丙肾上腺素为P<0.01,(-)肾上腺素为P<0.025),所有(27条)曲线都比相应的等长曲线更陡(P<0.001)。由于等张记录的操作窗口更窄且舒张的上限更小,所以可以预期记录方法会对结果产生影响。附录中提出了一种针对标准激动剂效应获得IC50测量值的方法。

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