Cho T M, Cho J S, Loh H H
Proc Natl Acad Sci U S A. 1978 Feb;75(2):784-8. doi: 10.1073/pnas.75.2.784.
The concentrations of nicotinic drugs required to effect a 50% transfer of triphosphol[3H]isositide from an aqueous phase to a nonaqueous phase closely approximated their concentrations for both in vivo neuromuscular blocking activity and binding to purified nicotinic receptors, and correlated well (correlation coefficient = 0.95)) with their biological activities measured by other workers in an Electrophorus electroplax preparation. The triphospho[3H]inositide transfer induced by nicotinic ligands was dependent on the lipid concentration and was potentiated by Ca2+. The affinity constants of 45Ca2+ for triphosphoinositide were similar to those for the purified nicotinic receptor. These and other findings suggest the possibility that triphosphoinositide (phosphatidylinositol bisphosphate) is a binding site of the nicotinic receptor.
使三磷酸[3H]肌醇磷脂从水相转移至非水相达到50%转移率所需的烟碱类药物浓度，与它们在体内的神经肌肉阻断活性以及与纯化烟碱受体结合的浓度非常接近，并且与其他研究人员在电鳗电板制备实验中测得的它们的生物学活性具有良好的相关性（相关系数 = 0.95）。烟碱配体诱导的三磷酸[3H]肌醇磷脂转移依赖于脂质浓度，并受到Ca2+的增强。45Ca2+对三磷酸肌醇的亲和常数与对纯化烟碱受体的亲和常数相似。这些及其他发现提示三磷酸肌醇磷脂（磷脂酰肌醇二磷酸）可能是烟碱受体的一个结合位点。
