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以锗和砷靶材生产无载体添加的硒-73的化学工艺以及L-2-氨基-4-([73Se]甲基硒代)丁酸(L-[73Se]硒代蛋氨酸)的合成。

Chemical processing for production of no-carrier-added selenium-73 from germanium and arsenic targets and synthesis of L-2-amino-4-([73Se]methylseleno) butyric acid (L-[73Se]selenomethionine).

作者信息

Plenevaux A, Guillaume M, Brihaye C, Lemaire C, Cantineau R

机构信息

Cyclotron Research Center, Liège University, Belgium.

出版信息

Int J Rad Appl Instrum A. 1990;41(9):829-38. doi: 10.1016/0883-2889(90)90060-t.

Abstract

The Ge(4He, xn) and 75As(p, 3n) reactions were compared as the best potential routes for routine production of selenium-73 (73Se) for medical applications. With 26 MeV alpha particles, available with compact cyclotrons, the first reaction required an enriched 70Ge target of sodium metagermanate to give a production yield of 1 mCi/microAh (0.037 GBq/microAh) in a 105 mg/cm2 target. With 55 MeV protons the As(p, 3n) reaction on natural arsenic yielded 20 mCi/microAh (0.74 GBq/microAh) in a 685 mg/cm2 target. A simple method was developed and optimized for both targets in order to isolate and purify the no-carrier-added selenium in the elemental form with a radiochemical yield greater than 75% in less than 90 min. An automated radiochemical processing unit has been designed for the routine production of 100-150 mCi (3.7-5.5 GBq) batches of carrier-free 73Se ready for radiopharmaceutical labeling. 30 mCi (1.11 GBq) (EOS) of L-2-amino-4-([73Se]methylseleno) butyric acid (L-[73Se]selenomethionine) ready for injection with a specific activity of 5 Ci/mmol (185 GBq/mmol) (EOS) were obtained through a fast chemical synthesis. Radiation absorbed dose estimates for L-[73Se]selenomethionine have been determined. A value of 0.70 rem/mCi (0.19 mSv/MBq) administered was calculated for the risk from irradiation in man. The first human PET investigation with [73Se]selenomethionine showed a very good delineation between liver and pancreas.

摘要

对用于医学应用的硒 - 73((^{73}Se))常规生产而言,比较了(Ge(^{4}He, xn))和(^{75}As(p, 3n))反应作为最佳潜在途径。使用紧凑型回旋加速器可获得的26兆电子伏的α粒子,第一个反应需要偏锗酸钠的富集(^{70}Ge)靶,在(105 mg/cm^{2})的靶中产生的产率为1毫居里/微安(0.037吉贝可/微安)。使用55兆电子伏的质子,天然砷上的(As(p, 3n))反应在(685 mg/cm^{2})的靶中产生20毫居里/微安(0.74吉贝可/微安)。针对这两种靶开发并优化了一种简单方法,以便以大于75%的放射化学产率在不到90分钟内分离并纯化元素形式的无载体添加硒。已设计了一个自动化放射化学处理单元,用于常规生产100 - 150毫居里(3.7 - 5.5吉贝可)无载体(^{73}Se)批次,用于放射性药物标记。通过快速化学合成获得了30毫居里(1.11吉贝可)(有效截止状态)可供注射的L - 2 - 氨基 - 4 - ([ (^{73}Se) ]甲基硒代)丁酸(L - [ (^{73}Se) ]硒代蛋氨酸),比活度为5居里/毫摩尔(185吉贝可/毫摩尔)(有效截止状态)。已确定了L - [ (^{73}Se) ]硒代蛋氨酸的辐射吸收剂量估计值。计算出人体照射风险为每注射1毫居里(0.19毫希沃特/兆贝可)0.70雷姆。首次使用[ (^{73}Se) ]硒代蛋氨酸的人体正电子发射断层扫描研究显示肝脏和胰腺之间的界限非常清晰。

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