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Synthesis and in vitro evaluation of iodine labelled pyrazolo[1,5‐ a ]pyridines as highly selective dopamine D4 receptor ligands by O. Prante; S. Löber; H. Hübner; P. Gmeiner; T. Kuwert is a Medicine article available to read on EtoBox.

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## 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.

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

Author

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

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0022-2135)

Published

2001

Language

EN

Field

Medicine (Life Sciences)