Sodium-dependent high-affinity binding of [3H]hemicholinium-3 in the rat brain: a potentially selective marker for presynaptic cholinergic sites.
Sodium-dependent high-affinity binding of [3H]hemicholinium-3 in the rat brain: a potentially selective marker for presynaptic cholinergic sites.
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大鼠脑中 [3H]hemicholinium-3 的钠依赖性高亲和力结合：突触前胆碱能位点的潜在选择性标记。
DOI：
10.1016/0024-3205(84)90525-3
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发表时间：
1984
期刊：
影响因子：
6.1
通讯作者：
Yamamura,HI
中科院分区：
文献类型：
--
作者：
Vickroy,TW;Roeske,WR;Yamamura,HI
本文报道了胆碱能神经末梢选择性钠依赖高亲和力胆碱摄取(SDHACU)抑制剂[~3H]-半胱氨酸-3([~H]HC-3)的膜结合特性。在所描述的测定条件下，[~3H]HC-3与一个可饱和的高亲和力(表观Kd=1.9nM)的中枢神经系统膜结合，其区域分布如下：纹状体⪢海马体；大脑皮层；小脑。高亲和力的[~3H]HC-3结合完全依赖于氯化钠的存在(EC50=35-50 mM)，当其他钠盐或一价离子被取代时，结合明显减少。胆碱(Ki=6μM)和乙酰胆碱(Ki=35μM)对HC-3结合有抑制作用，但对其他胆碱能药物和代谢抑制剂的敏感性明显降低。鉴于[~3H]HC-3结合和SDHACU具有相似的离子依赖性、区域分布和药理学特性，密切相关的位点可能参与了这两个过程。
This report describes the membrane binding properties of [3H] hemicholinium-3 ([3H]HC-3), a selective inhibitor of sodium-dependent high-affinity choline uptake (SDHACU) in cholinergic nerve terminals. Under the described assay conditions, [3H]HC-3 binds with a saturable population of high-affinity (apparent Kd=1.9 nM) CNS membrane sites having the regional distribution: striatum ⪢ hippocampus > cerebral cortex > cerebellum. High-affinity [3H]HC-3 binding is entirely dependent upon the presence of sodium chloride (EC50=35–50 mM) and is markedly reduced when other salts of sodium or monovalent ions are substituted. [3H]HC-3 binding is inhibited by choline (Ki=6μM) and acetylcholine (Ki=35μM) but markedly less sensitive to other cholinergic agents and metabolic inhibitors. In light of the similar ionic dependencies, regional distributions and pharmacological specificities of [3H]HC-3 binding and SDHACU, closely associated sites may be involved in both processes.