Hawkins P T, Reynolds D J, Poyner D R, Hanley M R
MRC Molecular Neurobiology Unit, MRC Centre, Cambridge, England.
Biochem Biophys Res Commun. 1990 Mar 16;167(2):819-27. doi: 10.1016/0006-291x(90)92099-l.
[3H]Inositol hexakisphosphate (InsP6) binds with a heterogeneous distribution to frozen sections of unfixed rat brain and is displaced by unlabelled InsP6. The pattern of binding correlates with binding to neuronal cell bodies. [3H]InsP6 binding to cerebellar membranes has been further characterised, is reversible, and saturable, and exhibits high specificity for inositol polyphosphates. The IC50 for competition by unlabelled InsP6 is approximately 100nM, whereas inositol 1,3,4,5,6 pentakisphosphate (Ins(13456)P5), inositol 1,3,4,5 tetrakisphosphate (Ins(1345)P4), and inositol 1,4,5 trisphosphate (Ins(145)P3) bind with an affinity at least one order of magnitude lower. [3H]InsP6 binding is clearly distinct from previously characterised Ins(145)P3 (ref. 1, 2) and Ins(1345)P4 (ref. 3) binding, both in terms of pharmacology and brain distribution.
[3H]肌醇六磷酸(InsP6)以异质性分布与未固定大鼠脑的冰冻切片结合,并可被未标记的InsP6取代。结合模式与神经元细胞体的结合相关。[3H]InsP6与小脑膜的结合已得到进一步表征,具有可逆性和饱和性,并且对肌醇多磷酸表现出高度特异性。未标记的InsP6竞争的IC50约为100nM,而肌醇1,3,4,5,6-五磷酸(Ins(13456)P5)、肌醇1,3,4,5-四磷酸(Ins(1345)P4)和肌醇1,4,5-三磷酸(Ins(145)P3)的结合亲和力至少低一个数量级。[3H]InsP6结合在药理学和脑部分布方面均明显不同于先前表征的Ins(145)P3(参考文献1、2)和Ins(1345)P4(参考文献3)结合。