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N-substituted phenyltropanes as in vivo binding ligands for rapid imaging studies of the dopamine transporter

✍ Scribed by Ursula Scheffel; John R. Lever; Philip Abraham; Karol R. Parham; William B. Mathews; Theresa Kopajtic; F. Ivy Carroll; Michael J. Kuhar

Publisher
John Wiley and Sons
Year
1997
Tongue
English
Weight
80 KB
Volume
25
Category
Article
ISSN
0887-4476

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✦ Synopsis

Variously substituted phenyltropanes are proven as superb binding ligands for the dopamine transporter (DAT). In this study, we examine four N-substituted phenyltropanes which are derivatives of RTI-55 as in vivo binding ligands in mice. In this series, the methyl group on the nitrogen was replaced by a propyl (RTI-310), an allyl (RTI-311), a butyl (RTI-312), or a fluoropropyl (RTI-313) group. The in vitro binding potencies of these compounds at rat striatal DAT varied somewhat but were about 1 nM. While these compounds did not display marked selectivity for the dopamine transporter, they were more selective than RTI-55. Injection of the radiolabeled compound into mice resulted in striatal-to-cerebellar ratios that varied from about 4.5-6.5. The ratios peaked most rapidly for RTI-311 and RTI-313, at about 20 min. Pharmacological inhibition studies indicated that these compounds were binding to DATs in the striatum, as expected. These findings suggest that some compounds of this type may be excellent in vivo binding ligands for rapid imaging studies of the DAT.

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