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首页> 外文期刊>Brain research >Cytisine binds with similar affinity to nicotinic alpha4beta2 receptors on the cell surface and in homogenates.
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Cytisine binds with similar affinity to nicotinic alpha4beta2 receptors on the cell surface and in homogenates.

机译：半胱氨酸与细胞表面和匀浆中的烟碱α4β2受体具有相似的亲和力。

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摘要

Cytisine and nicotine bound to specific sites in homogenates prepared from HEK 293 cells which stably express human neuronal nicotinic alpha4 and beta2 subunits. The number of sites was the same for both ligands and nicotine was a full competitive inhibitor of cytisine binding. However, when binding was done to intact cells the number of binding sites per cell for nicotine was approximately 4-fold the number of sites for cytisine. Nicotine fully blocked cytisine binding, but cytisine only partially blocked nicotine binding to intact cells. When cells were permeabilized with saponin, the number of sites for nicotine was unchanged, while the number of sites for cytisine was increased, and cytisine was able to fully block nicotine binding. These data indicate that cytisine binds only to surface receptors on intact cells. The apparent affinity of cytisine for surface receptors (K(d)=0.8 nM) was not significantly different from that for receptors in the cell homogenate (0.3 nM).
机译：半胱氨酸和尼古丁与HEK 293细胞制备的匀浆中的特定位点结合，HEK 293细胞稳定表达人神经元烟碱α4和β2亚基。对于两个配体而言，位点的数目是相同的，并且尼古丁是完全的竞争性胞嘧啶结合抑制剂。然而，当完成与完整细胞的结合时，每个细胞对尼古丁的结合位点的数目大约是对胱氨酸的位点数目的4倍。尼古丁完全阻断了胱氨酸的结合，但胱氨酸仅部分阻断了尼古丁与完整细胞的结合。当用皂苷透化细胞时，烟碱的位点数目没有变化，而胱氨酸的位点数目却增加了，并且胱氨酸可以完全阻断烟碱的结合。这些数据表明，半胱氨酸仅与完整细胞上的表面受体结合。半胱氨酸对表面受体的表观亲和力（K（d）= 0.8 nM）与细胞匀浆中对受体的表观亲和力（0.3 nM）没有显着差异。

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