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Synthesis and in vitro Evaluation of Iodine Labelled Pyrazolo[1,5-a]pyridines as Highly Selective Dopamine D4 Receptor Ligands

Löber S, Gmeiner P, Hübner H (2001)

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Publication Type: Journal article

Publication year: 2001

Journal

Publisher: Wiley-Blackwell

Book Volume: 44

Pages Range: 849-858

DOI: 10.1002/jlcr.508

Abstract

Two ¹³¹I-labelled radioligands, namely 3-(4-[¹³¹1]iodophenylpiperazin-1-ylmethyl)-pyrazolo[1,5-a]pyridine and 3-(4-chlorophenylpiperazin-1-ylmethyl)-7-[ ¹³¹I]iodopyrazolo[1,5-a]pyridine, which are required tor 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 Ki values of 3.1 and 2.6nM. 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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How to cite

APA:

Löber, S., Gmeiner, P., & Hübner, H. (2001). Synthesis and in vitro Evaluation of Iodine Labelled Pyrazolo[1,5-a]pyridines as Highly Selective Dopamine D4 Receptor Ligands. Journal of Labelled Compounds & Radiopharmaceuticals, 44, 849-858. https://doi.org/10.1002/jlcr.508

MLA:

Löber, Stefan, Peter Gmeiner, and Harald Hübner. "Synthesis and in vitro Evaluation of Iodine Labelled Pyrazolo[1,5-a]pyridines as Highly Selective Dopamine D4 Receptor Ligands." Journal of Labelled Compounds & Radiopharmaceuticals 44 (2001): 849-858.

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