STRUCTURE ACTIVITY RELATIONSHIP OF TC-99M COMPLEXES OF PHENYLENEDIAMINE THIOL THIOETHER LIGANDS (PHAT) TO BRAIN UPTAKE IN RATS

被引：13

作者：

MCBRIDE, BJ ^{[1
]}

BALDWIN, RM ^{[1
]}

KERR, JM ^{[1
]}

WU, JL ^{[1
]}

SCHULTZE, LM ^{[1
]}

SALAZAR, NE ^{[1
]}

CHINITZ, JM ^{[1
]}

BYRNE, EF ^{[1
]}

机构：

[1] MEDIPHYS INC,RES & DEV LAB,EMERYVILLE,CA 94608

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 01期

关键词：

D O I：

10.1021/jm00053a010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of ligands, phenylenediamine-thiol-thioether (PhAT), was synthesized, and their Tc-99m complexes were evaluated for potential use as a functional brain imaging agent. The ligands reacted with (NaTcO4)-Tc-99m and SnCl2 to form single, stable, neutral, and lipophilic Te-99m complexes. Several of these complexes showed significant brain uptake and retention in rats. In particular, the S-ethyl, allyl, and propargyl derivatives had high initial brain uptake (0.88, 0.99, and 0.82% dose/g at 5 min, respectively) and good retention (0.71, 0.75, and 0.67% dose/g at 30 min). The structure-activity relationship of alkyl, alkenyl, and alkynyl thioether derivatives is reported.

引用

页码：81 / 86

页数：6

共 25 条

[1] NEUTRAL TECHNETIUM(V) COMPLEXES WITH AMIDE THIOL THIOETHER CHELATING LIGANDS [J].