SPECT imaging of the benzodiazepine receptor in non-human primate brain with [123I]Ro 16-0154.
SPECT imaging of the benzodiazepine receptor in non-human primate brain with [123I]Ro 16-0154.
复制标题
使用 [123I]Ro 16-0154 对非人灵长类动物脑中苯二氮卓受体进行 SPECT 成像。
DOI：
10.1016/0014-2999(91)90043-p
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发表时间：
1991
影响因子：
5
通讯作者：
Charney,D
中科院分区：
文献类型：
--
作者：
Innis,R;Zoghbi,S;Johnson,E;Woods,S;al-Tikriti,M;Baldwin,R;Seibyl,J;Malison,R;Zubal,G;Charney,D
我们在非人类灵长类动物中使用SPECT（单光子发射计算机断层扫描）成像来检查123i标记的Ro 16-0154作为苯二氮卓类受体的体内探针的时间过程和药理学特异性。最大脑摄取在静脉注射放射配体后约70分钟达到，约占注射剂量的10%。放射性密度的区域分布与已知的苯二氮卓受体在灵长类动物脑内的分布一致，最高的吸收区域位于枕区。放射性的冲洗相对缓慢，在放射性峰值后每小时的速率为3%。注射苯二氮卓类拮抗剂ro15 -1788 （0.2 ~ 0.3 mg/kg静脉注射）可使脑放射性迅速下降90%以上。综上所述，[123I] ro16 -0154是一种很有前景的苯二氮卓类受体体内SPECT放射配体，具有高脑摄取、稳定的峰值放射性周期、适当的区域分布以及被其他苯二氮卓类受体药物取代的能力。
We have used SPECT (single photon emission computed tomography) imaging in non-human primates to examine the time course and pharmacological specificity of123I-labeled Ro 16-0154 as an in vivo probe of the benzodiazepine receptor. Maximal brain uptake was reached approximately 70 min post i.v. administration of the radioligand and represented approximately 10% of the injected dose. The regional distribution of radioactive densities was consistent with the known distribution of benzodiazepine receptor in primate brain, with highest uptake localized over the occipital area. Washout of radioactivity was relatively slow with a rate of 3% per hour after the time of peak radioactivity. Injection of the benzodiazepine antagonist Ro 15-1788 (0.2–0.3 mg/kg i.v.) caused a rapid decrease of more than 90% of radioactivity from brain. In summary, [123I]Ro 16-0154 is a promising in vivo SPECT radioligand for the benzodiazepine receptor, with high brain uptake, a stable period of peak radioactivity, appropriate regional distribution, and ability to be displaced by other benzodiazepine receptor agents.