Synthesis and <sup>125</sup> I labeling of a precursor for imaging nicotinic acetylcholine receptors

LIU Yuxia LIU Ning YANG Yuanyou ZAN Liangbiao LIAO Jiali JIN Jiannan

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Synthesis and ¹²⁵ I labeling of a precursor for imaging nicotinic acetylcholine receptors

更新时间：2021-03-12

- Synthesis and ¹²⁵ I labeling of a precursor for imaging nicotinic acetylcholine receptors
- NUCLEAR TECHNIQUES Issue 8, (2006)
- 作者机构：
  
  1. 四川大学原子核科学技术研究所辐射物理及技术教育部重点实验室
  2. 四川大学原子核科学技术研究所辐射物理及技术教育部重点实验室,成都,610064
- 作者简介：
- 基金信息：
  
  国家自然科学基金资助项目(20071023)
- DOI：
  CLC： R817
- Published：01 August 2006
- 稿件说明：
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[1]刘钰霞,刘宁,杨远友,昝亮彪,廖家莉,金建南.一种烟碱乙酰胆碱受体(nAChRs)显像前体化合物的合成与~(125)I标记研究[J].核技术,2006(08):592-596.

LIU Yuxia LIU Ning YANG Yuanyou ZAN Liangbiao LIAO Jiali JIN Jiannan. Synthesis and ¹²⁵ I labeling of a precursor for imaging nicotinic acetylcholine receptors[J]. Nuclear techniques, 2006, (8): 592-596.
[1]刘钰霞,刘宁,杨远友,昝亮彪,廖家莉,金建南.一种烟碱乙酰胆碱受体(nAChRs)显像前体化合物的合成与~(125)I标记研究[J].核技术,2006(08):592-596. DOI：

LIU Yuxia LIU Ning YANG Yuanyou ZAN Liangbiao LIAO Jiali JIN Jiannan. Synthesis and ¹²⁵ I labeling of a precursor for imaging nicotinic acetylcholine receptors[J]. Nuclear techniques, 2006, (8): 592-596. DOI：

摘要

本文介绍一种可用于125／123I标记的A-85380类前体化合物——（S）-5-（三丁基锡烷基）-3-[[1-（叔丁氧基羰基）-2-甲氧基]氮杂环丁基]吡啶的设计、合成及125I标记研究。实验以2-糠胺和（S）-氮杂环丁基甲酸为起始物

先合成（S）-5-（三丁基锡烷基）-3-[[1-（叔丁氧基羰基）-2-氮杂环丁基]甲氧基]吡啶前体化合物

再用125I标记

制得5-[125I]I-A-85380。整个放射性标记的时间为50-55min

标记率大于30％。5-[125I]I-A-85380在室温下放置3天

其放化纯度仍在95％以上

表明其在体外具有较高的稳定性。

Abstract

Nicotinic Acetylcholine Receptors （nAChRs） are involved in various pharmacological effects or diseases

such as Alzheimer’s Disease

Parkinson’s Disease and tobacco addiction. It will be very appealing to image nAChRs in vivo

diagnose and treat the above diseases

and probe the mechanism of nAChRs in tobacco addiction if the suitable radioactive labeled compound can be synthesized. In this study

（s）-5-（tri-butylstannyl）-3{[1-（tert-butoxycarbonyl）-2- azetidinyl]methoxy}pyridine

a precursor for imaging nAChRs

was synthesized with commercial 2-furfurylamine and （s）-2-azetidinecarboxylic acid as starting materials

and was further labeled with 125/123I.The whole procedure for radiosynthesis needs 50 - 55 min and more than 30% of the 125I are found in the purified 5-[125I]-A-85380. Even staying for 3 days at room temperature in vitro

the purified 5-[125I]-I-85380 can maintain its stability

with a radiochemical purity of more than 95%.

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Synthesis and 125 I labeling of a precursor for imaging nicotinic acetylcholine receptors

DOI：

摘要

Abstract

关键词

Keywords

references

Synthesis and ¹²⁵ I labeling of a precursor for imaging nicotinic acetylcholine receptors