核化学与放射化学
覈化學與放射化學
핵화학여방사화학
HE HUAXUE YU FANGSHE HUAXUE
2010年
2期
99-105
,共7页
李艳%贾红梅%Deuther-Conrad Winnie%Brust Peter%Steinbach Joerg%刘伯里
李豔%賈紅梅%Deuther-Conrad Winnie%Brust Peter%Steinbach Joerg%劉伯裏
리염%가홍매%Deuther-Conrad Winnie%Brust Peter%Steinbach Joerg%류백리
吲哚类配体%σ受体%~(99)Tc~m%~(123)I
吲哚類配體%σ受體%~(99)Tc~m%~(123)I
신타류배체%σ수체%~(99)Tc~m%~(123)I
Indole%σ receptors%~(99)Tc~m%~(123)I
设计了~(123)I和~(99)Tc~m标记的吲哚类σ_2受体肿瘤放射性示踪剂,合成了其稳定化合物 (Indole-I和Indole-MAMA-Re) 和标记前体(Indole-MAMA).体外受体结合分析结果表明,化合物Indole-I对σ1和σ_2受体的抑制常数K_i值分别为(0.574±0.355) μmol/L和(0.162±0.030) μmol/L(n=3),Indole-MAMA-Re对σ1和σ_2受体的抑制常数K_i值分别为(3.75±2.22) μmol/L和(7.83±4.87) μmol/L(n=3).成功制备了~(99)Tc~m-Indole-MAMA,纯化后经高效液相色谱法(HPLC)分析其放化纯大于90%.今后可在本文化合物的基础上通过结构优化,设计合成对σ_2受体具有高亲和力和选择性的吲哚类SPECT肿瘤显像剂.
設計瞭~(123)I和~(99)Tc~m標記的吲哚類σ_2受體腫瘤放射性示蹤劑,閤成瞭其穩定化閤物 (Indole-I和Indole-MAMA-Re) 和標記前體(Indole-MAMA).體外受體結閤分析結果錶明,化閤物Indole-I對σ1和σ_2受體的抑製常數K_i值分彆為(0.574±0.355) μmol/L和(0.162±0.030) μmol/L(n=3),Indole-MAMA-Re對σ1和σ_2受體的抑製常數K_i值分彆為(3.75±2.22) μmol/L和(7.83±4.87) μmol/L(n=3).成功製備瞭~(99)Tc~m-Indole-MAMA,純化後經高效液相色譜法(HPLC)分析其放化純大于90%.今後可在本文化閤物的基礎上通過結構優化,設計閤成對σ_2受體具有高親和力和選擇性的吲哚類SPECT腫瘤顯像劑.
설계료~(123)I화~(99)Tc~m표기적신타류σ_2수체종류방사성시종제,합성료기은정화합물 (Indole-I화Indole-MAMA-Re) 화표기전체(Indole-MAMA).체외수체결합분석결과표명,화합물Indole-I대σ1화σ_2수체적억제상수K_i치분별위(0.574±0.355) μmol/L화(0.162±0.030) μmol/L(n=3),Indole-MAMA-Re대σ1화σ_2수체적억제상수K_i치분별위(3.75±2.22) μmol/L화(7.83±4.87) μmol/L(n=3).성공제비료~(99)Tc~m-Indole-MAMA,순화후경고효액상색보법(HPLC)분석기방화순대우90%.금후가재본문화합물적기출상통과결구우화,설계합성대σ_2수체구유고친화력화선택성적신타류SPECT종류현상제.
Novel indole radiotracers for ~(123)I and ~(99)Tc~m labeling were designed. The corresponding reference compounds (Indole-I and Indole-MAMA-Re) and the precursor (Indole-MAMA) for ~(99)Tc~m labeling were synthesized. Competition binding assays in vitro show that the K_i values successfully prepared. The radio-chemical purity (RCP) of ~(99)Tc~m-Indole-MAMA after purification was higher than 90% by HPLC analysis. The compounds reported in this paper may be used as lead compounds for further structural modification to develop indole SPECT tumor imaging agents with high affinity and selectivity for σ_2 receptors.
