Prante O, Tietze R, Hocke C, Löber S, Hübner H, Kuwert T, Gmeiner P (2008)
Publication Type: Journal article
Publication year: 2008
Publisher: American Chemical Society
Book Volume: 51
Pages Range: 1800-1810
DOI: 10.1021/jm701375u
A series of fluoro-substituted analogs structurally derived from the aminomethyl-substituted pyrazolo[1,5-a]pyridine lead compounds 9 (FAUC 113) and 10 (FAUC 213) were synthesized and evaluated as high-affinity D4 receptor (D4R) ligands (3a-3h, Ki = 1.3-28 nM). The para-fluoroethoxy-substituted derivatives 3f and 3h revealed an outstanding D4 subtype selectivity of more than 3 orders of magnitude over both congeners D2 and D3 combined with inverse agonism at D4R. The corresponding 18F-labeled radioligands revealed high serum stability in vitro and log P values of 2-3. In vitro rat brain autoradiography showed specific binding of [18F]3h in distinct brain regions, including the gyrus dentate of the hippocampus, that were inhibited by both eticlopride (65-80%) and the selective D4R antagonist 10 (78-93%). The observed binding pattern was mainly consistent with the known D4R distribution in the rat brain. Thus, [18F]3h (FAUC F41) represents a potential radioligand for studying the D4R in vivo by positron emission tomography (PET). © 2008 American Chemical Society.
APA:
Prante, O., Tietze, R., Hocke, C., Löber, S., Hübner, H., Kuwert, T., & Gmeiner, P. (2008). Synthesis, Radiofluorination and In Vitro Evaluation of Pyrazolo[1,5-a]pyridine Based Dopamine D4 Receptor Ligands: Discovery of an Inverse Agonist Radioligand for PET. Journal of Medicinal Chemistry, 51, 1800-1810. https://doi.org/10.1021/jm701375u
MLA:
Prante, Olaf, et al. "Synthesis, Radiofluorination and In Vitro Evaluation of Pyrazolo[1,5-a]pyridine Based Dopamine D4 Receptor Ligands: Discovery of an Inverse Agonist Radioligand for PET." Journal of Medicinal Chemistry 51 (2008): 1800-1810.
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