The design and synthesis of novel derivatives of the dopamine uptake inhibitors GBR 12909 and GBR 12935. High-affinity dopaminergic ligands for conjugation with highly fluorescent cadmium selenide/zinc sulfide core/shell nanocrystals
✍ Scribed by Ian D Tomlinson; John Mason; Jon N Burton; Randy Blakely; Sandra J Rosenthal
- Publisher
- Elsevier Science
- Year
- 2003
- Tongue
- French
- Weight
- 243 KB
- Volume
- 59
- Category
- Article
- ISSN
- 0040-4020
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✦ Synopsis
There is a growing demand for compounds with very high affinities for the dopamine transporter protein (DAT) that can be conjugated to fluorescent markers such as cadmium selenide/zinc sulfide core/shell nanocrystals. This paper describes the design and synthesis of two derivatives of the DAT antagonists GBR 12935 and GBR 12909. These compounds have a high biological affinity for DAT and may be conjugated to nanocrystals via a thiol linkage without a significant reduction in their biological activity. Such conjugates may be used in fluorescent imaging studies.