Radioiodinated (—)-2-[4-(3‐iodophenyl) piperidino] cyclohexanol: A potential radioligand for mapping presynaptic cholinergic neurons
Radioiodinated (—)-2-[4-(3‐iodophenyl) piperidino] cyclohexanol: A potential radioligand for mapping presynaptic cholinergic neurons
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放射性碘标记的 (—)-2-[4-(3-碘苯基)哌啶基]环己醇：用于绘制突触前胆碱能神经元的潜在放射性配体
DOI：
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发表时间：
1996
影响因子：
1.5
通讯作者：
A. Ichikawa
中科院分区：
文献类型：
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作者：
K. Shiba;H. Mori;H. Matsuda;A. Ichikawa
我们合成了放射性碘标记的2-[4-(3-碘苯基)哌啶]环己醇((-)-[125I]-m-碘代氨基酚[(-)-[125I]MIV])的(-)-对映体，并研究了其与大鼠脑内维沙米考受体的体内结合特异性和亲和力。(-)-MIV量显著增加(∼为注射剂量的3%)，滞留时间延长。未标记维沙米考(0.5Mol·kg-1)给药前后，(-)-[125I]-MIV在脑内的蓄积明显减少。体内阻断和置换研究表明，(-)-[125I]MIV与维沙米考受体的结合亲和力很高，而与其他受体的结合亲和力很低。放射自显影研究表明，(-)-[125I]-MIV和(-)-[~3H]维沙米考在大鼠脑冠状切片上的放射性分布相似。结果表明，(-)-[125I]MIV在大鼠脑内结合部位的特性与体外相似。放射性碘标记(-)-MIV可能对研究脑内突触前胆碱能神经元有潜在的帮助。
SummaryWe synthesized the (—)-enantiomer of radioiodinated 2-[4-(3-iodophenyl)piperidino] cyclohexanol ((—)-[125I]-m-iodovesamicol [(—)-[125I]mIV]) and evaluated its in vivo binding specificity and affinity for the vesamicol receptor in the rat brain. Significant amounts (∼ 3% of the injected dose) of (—)-mIV accumulated and retention was prolonged. The accumulation of (—)-[125I]mIV in the brain was significantly reduced by the pre- and post-administration of unlabelled vesamicol (0.5 μmol kg-1). Blocking and displacement studies in vivo showed that the binding affinity of (—)-[125I]mIV for the vesamicol receptor was very high, but that for other receptors was very low. Autoradiographic studies showed that the regional distribution of radioactivity, as revealed by coronal sections of the rat brain, was similar for both (—)-[125I]mIV and (—)-[3H]vesamicol. The results demonstrated that the characteristics of (—)-[125I]mIV for binding sites in rat brain were similar in vivo and in vitro. Radioiodinated (—)-mIV may potentially be useful for studying presynaptic cholinergic neurons in the brain.