The preliminary biocharacteristic study of a potential dopamine D_3 receptor imaging agent, ~(125) I-7-OH-PIPAT

Z. Tulassay, A. Kryszewski, P. Dítě, D. Kleczkowski, J. Rudzinski, Z. Bartuzi, G. Hasselgren, A. Larko
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Abstract

Objective To study the biocharacteristics of a potential dopamine D 3 receptor imaging agent, 125 I 7 hydroxy 2 [ N propyl N (3′ iodo 2′ propenyl) amino]tetralin (7 OH PIPAT) which was synthesized in this lab. Methods 125 I 7 OH PIPAT was used as a radioactive tracer to study the biodistribution of 125 I 7 OH PIPAT in rats and in particular, in the brain regions, and autoradiography was used to study the binding sites of 125 I 7 OH PIPAT in rat brain slices. Results The uptake of 125 I 7 OH PIPAT in the whole brain reached to 1%, and autoradiography showed that 125 I 7 OH PIPAT was accumulated at olfactory tubercle and limbic regions of rat brain. Conclusions 125 I 7 OH PIPAT is able to penetrate the brain blood barrier, and has the affinity to dopamine D 3 receptors. It has the potential activity to be a dopamine D 3 receptor imaging agent.
一种潜在的多巴胺D_3受体显像剂~(125)I-7-OH-PIPAT的生物特性初步研究
目的研究本实验室合成的一种潜在的多巴胺d3受体显像剂125 I 7羟基2 [N丙基N(3′碘2′丙烯基)氨基]四氢化萘(7 OH PIPAT)的生物学特性。方法采用125 I 7 OH PIPAT作为放射性示踪剂,研究125 I 7 OH PIPAT在大鼠体内特别是脑区的生物分布,并采用放射自显影技术研究125 I 7 OH PIPAT在大鼠脑片中的结合位点。结果125i7 OH PIPAT在全脑内的摄取达到1%,放射自显像显示125i7 OH PIPAT在大鼠脑嗅结节和边缘区有积累。结论125i7oh PIPAT能穿透脑血屏障,与多巴胺d3受体具有亲和力。它具有作为多巴胺d3受体显像剂的潜在活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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