Preparation of a technetium-99m SPECT agent for imaging the sigma-2 receptor status of solid tumors
✍ Scribed by Robert H. Mach; Kenneth T. Wheeler; Suwanna Blair; Biao Yang; Cynthia S. Day; Joseph B. Blair; Seok-Rye Choi; Hank F. Kung
- Publisher
- John Wiley and Sons
- Year
- 2001
- Tongue
- French
- Weight
- 156 KB
- Volume
- 44
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.516
No coin nor oath required. For personal study only.
✦ Synopsis
The synthesis and in vitro binding of a novel 99m Tc-labeled radiotracer for imaging the sigma-2 (s 2 ) receptor status of breast tumors is described. Structural characterization and in vitro binding studies were conducted using the corresponding rhenium surrogate, Re-2. X-ray crystallographic studies revealed that the complexation reaction gave exclusively the syn isomer. In vitro binding studies indicated that this complex has a high affinity for s 2 (K i ¼ 13:7 nM) versus s 1 receptors (K i ¼ 1125 nM). These data indicate that