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A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain.

Abstract：

:The dopamine transporter (DAT), located presynaptically on dopamine neurons, provides a marker for certain neurological diseases. In particular, the DAT is depleted in Parkinson's disease, and the extent of depletion correlates with the loss of dopamine. Herein we describe the design, synthesis, and biological evaluation of technepine, the first 99mTc-labeled SPECT imaging agent which targets the dopamine transporter in striatum. We have demonstrated that the DAT can accommodate a chelating unit attached to the 8-amine function of a tropane skeleton. Further, we have demonstrated for the first time that a molecule can be designed to carry the radionuclide 99mTc across the blood-brain barrier in sufficient quantity to obtain in vivo images of the striatum in monkeys. This advance will undoubtedly lead to the design of new receptor and transporter-mediated 99mTc agents which can label specific transporter and receptor targets in the central nervous system.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Meltzer PC,Blundell P,Jones AG,Mahmood A,Garada B,Zimmerman RE,Davison A,Holman BL,Madras BK

doi

10.1021/jm960868t

subject

Has Abstract

pub_date

1997-06-06 00:00:00

pages

1835-44

issue

12

eissn

0022-2623

issn

1520-4804

pii

jm960868t

journal_volume

40

pub_type

杂志文章

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