NORMAL DISTRIBUTION OF NICOTINIC ACETYLCHOLINE RECEPTORS IN NON-SMOKERS AND SMOKERS : 5IA-SPELT STUDY.

非吸烟者和吸烟者烟碱乙酰胆碱受体的正常分布：5IA-SPELT 研究。

• 批准号: 15591268
• 负责人: ISHIZU Koichi
• 金额: $ 1.66万
• 依托单位: KYOTO UNIVERSITY
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2003
• 资助国家: 日本
• 起止时间: 2003 至 2004
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-15591268/
• 关键词: 5IA; nicotine; SPECT; nAChR; quantitative; smoking; acetylcholine receptor; 受容体; 禁煙; 分布容積; アセチルコリン受容体; dynamic収集; 定量解析; 動脈血採血

We have demonstrated suitability of 123I-(S)-5-iodo-3-(2-azetidinylmethoxy) pyridine, 123I-5-iodo-A-85380(123I-5IA) to image in vivo nicotinic acetylcholine receptors in human brain. This distribution of 123I-5IA in normal volunteer was compatible with the known distribution of nicotinic receptors in humans. The present study was designed to demonstrate the in vivo temporal changes of high affinity nicotinic acetylcholine receptors (nAChR) in smokers before and after cigarette withdrawal using 123I-5IA. Subjects were four smokers free of any neurological diseases (1 female and 3 males, 26 to 30 yrs, mean 28.3+/-2.1). They underwent two dynamic SPECT (Picker, Prism 3000) studies, 4 hours after and 20 days after cigarette smoking withdrawal. All of them received a one-minute intravenous injection of approximately 150 MBq of 123I-5IA in both studies. Arterial input function was obtained for each subject and a two-compartment model was used to determine the kinetic parameters of 123I-5IA u … More sing data from 6 hours SPECT scan. The distribution volume (Vt)(ml/ml) of 123I-5IA, which is related to the number of unoccupied binding sites in the brain, was calculated and compared to previous results generated from normal non-smoker volunteers. The 123I-5IA Vt (ml/ml) values in the smokers are shown in Table 1. The highest Vt values were observed in thalamus and brain stem at both steps of the study. The Vt values were significantly higher after cigarette smoking withdrawal (p<0.01) as compared to the smoking study with 4 hours smoking withdrawal The Vt values from smokers were significant lower as compared to the values from normal non-smokers (p<0.05). No significant difference was observed between Vt values after cigarette smoking withdrawal. and those of the non-smokers. In conclusion, 123I-5IA-SPECT was valuable in assessing quantitative temporal changes of nAChR distribution in smoker's brain as measured before and after cigarette withdrawal. Up-regulation of nAChR was observed after 20 days cigarette withdrawal in the smokers. Less

我们已经证明了123 I-（S）-5-碘-3-（2-氮杂环丁烷甲氧基）吡啶，123 I-5-碘-A-85380（123 I-5IA）对人脑中烟碱乙酰胆碱受体的体内成像的适用性。正常志愿者中123 I-5IA的这种分布与人体中烟碱受体的已知分布一致。本研究旨在证明在体内的时间变化的高亲和力烟碱乙酰胆碱受体（nAChR）的吸烟者戒烟前后使用123 I-5IA。受试者为4名无任何神经系统疾病的吸烟者（1名女性和3名男性，26 - 30岁，平均28.3+/-2.1岁）。他们在戒烟后4小时和20天进行了两次动态SPECT（Picker，Prism 3000）研究。在两项研究中，所有患者均接受了1分钟静脉注射约150 MBq的123 I-5IA。获得了每例受试者的动脉输入函数，并采用二室模型确定了123 I-5IA u的动力学参数 ...更多信息 6小时SPECT扫描数据。计算123 I-5IA的分布体积（Vt）（ml/ml），其与脑中未占用结合位点的数量相关，并与正常非吸烟志愿者的先前结果进行比较。吸烟者的123 I-5IA Vt（ml/ml）值见表1。在研究的两个步骤中，在丘脑和脑干中观察到最高Vt值。戒烟后的Vt值显著高于戒烟4小时的吸烟研究（p<0.01）。吸烟者的Vt值显著低于正常非吸烟者的值（p<0.05）。戒烟后Vt值之间无显著差异。和那些不吸烟的人。总之，123 I-5IA-SPECT是有价值的，在评估定量的时间变化的nAChR分布在吸烟者的大脑中测量之前和之后戒烟。吸烟者戒烟20天后nAChR表达上调。少

项目成果

Quantification of human nicotinic acetylcholine receptors with 123I-5IA SPECT

使用 123I-5IA SPECT 定量人烟碱乙酰胆碱受体

• 发表时间: 2004
• 期刊: Journal of Nuclear Medicine 45(9)
• 作者: Marcelo Mamede;Koichi Ishizu;et al.
• 通讯作者: et al.

アセチルコリン受容体イメージングと痴呆性疾患

乙酰胆碱受体成像与痴呆疾病

• 发表时间: 2004
• 期刊: Cognition and Dementia 3
• 作者: Mamede M;Ishizu K;et al.;石津浩一
• 通讯作者: 石津浩一

5-[^<123>I]Iodo-A-85380 : assessment of pharmacological safety, radiation dosimetry and SPECT imaging of brain nicotinic receptors in healthy human subjects.

5-[^ 123 I]Iodo-A-85380：健康人类受试者中脑烟碱受体的药理学安全性、辐射剂量测定和SPECT成像的评估。

• 发表时间: 2004
• 期刊: Ann Nucl Med. 18(4)
• 作者: Ueda M;Iida Y;Mukai T;Mamede M;Ishizu K;Ogawa M;Magata Y;Konishi J;Saji H.
• 通讯作者: Saji H.

Quantification of human nicotinic acetylcholine receptors with ^<123>I-5IA SPECT.

用123 I-5IA SPECT定量人烟碱乙酰胆碱受体。

• 发表时间: 2004
• 期刊: Journal of Nuclear Medicine 45(9)
• 作者: Mamede M;Ishizu K;et al.
• 通讯作者: et al.

Asechirukorin jyuyoutai ime-jingu to chihouseisikkan

阿塞留科林十九大 伊神宫与Chihouseisikkan

• 发表时间: 2004
• 期刊: Congnitionand Dementia Vol.3
• 作者: Mamede M;Ishizu K;Ueda M;Mukai T;Iida Y;Fukuyama H;Saga T;Saji H.;Koichi Ishidu
• 通讯作者: Koichi Ishidu