阿片受体：在脑切片中观察到的结合协同性。
Opiate receptor: cooperativity of binding observed in brain slices.
作者信息
Davis M E, Akera T, Brody T M, Watson L
出版信息
Proc Natl Acad Sci U S A. 1977 Dec;74(12):5764-6. doi: 10.1073/pnas.74.12.5764.
Abstract
Kinetic constants for binding of 3H-labeled morphine and naloxone were determined from Hill plot analyses and from experiments in which the concentration of tritiated drug was constant and that of nonlabeled drug varied. With brain slices, the binding of either drug exhibited strong positive cooperativity (Hill slope greater than 3); this was not observed in brain homogenates. Thus, in slices the relationship between opiate binding site and ligand may be more relevant physiologically and pharmacologically.
摘要
通过希尔图分析以及氚标记药物浓度恒定而非标记药物浓度变化的实验，测定了³H标记的吗啡和纳洛酮结合的动力学常数。对于脑切片，两种药物的结合均表现出强正协同性（希尔斜率大于3）；而在脑匀浆中未观察到这种情况。因此，在切片中，阿片类药物结合位点与配体之间的关系在生理和药理方面可能更具相关性。
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本文引用的文献
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