Maloteaux J M, Gossuin A, Pauwels P J, Laduron P M
FEBS Lett. 1983 May 30;156(1):103-7. doi: 10.1016/0014-5793(83)80257-9.
A rapid carbachol-induced disappearance of muscarinic cell surface receptors was shown using [3H]methyl scopolamine as ligand on intact 108CC15 hybrid cells or rat cerebellar cells. This phenomenon is temperature-dependent, correlated to agonist stimulation and reversible. In these short time periods (less than or equal to 30 min), no change was observed in the total receptor amount measured on membrane preparations. This disappearance of cell surface receptors could represent the first event in cell desensitization which could be followed by receptor recycling in physiological conditions or by receptor degradation if the stimulation by agonists persists, as in long-term regulation.
使用[3H]甲基东莨菪碱作为配体,在完整的108CC15杂交细胞或大鼠小脑细胞上,显示了卡巴胆碱诱导的毒蕈碱细胞表面受体的快速消失。这种现象是温度依赖性的,与激动剂刺激相关且可逆。在这些短时间内(小于或等于30分钟),在膜制剂上测得的总受体量没有变化。细胞表面受体的这种消失可能代表细胞脱敏的第一个事件,在生理条件下可能随后是受体再循环,或者如果激动剂持续刺激,如在长期调节中,则是受体降解。