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Synthesis and in vitro evaluation of iodine labelled pyrazolo[1,5-a]pyridines as highly selective dopamine D4 receptor ligands

✍ Scribed by O. Prante; S. Löber; H. Hübner; P. Gmeiner; T. Kuwert

Publisher
John Wiley and Sons
Year
2001
Tongue
French
Weight
122 KB
Volume
44
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Two ^131^I‐labelled radioligands, namely 3‐(4‐[^131^I]iodophenylpiperazin‐1‐ylmethyl)‐pyrazolo[1,5‐a]pyridine and 3‐(4‐chlorophenylpiperazin‐1‐ylmethyl)‐7‐[^131^I]iodopyrazolo[1,5‐a]pyridine, which are required for studies or binding of these ligands to the D4 receptor, have been synthesized in 80% and 32% radiochemical yields, respectively; the radiochemical purity in each case was >97%. For the second radioligand a kit preparation, based on iododestannylation followed by solid‐phase extraction, was possible. In vitro characterization using CHO‐cells expressing different dopamine receptor subtypes gave K~i~ values of 3.1 and 2.6 nM. Both radioligands are highly selective for the D4 subtype as compared to other dopamine subtypes. Copyright © 2001 John Wiley & Sons, Ltd.

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