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Your search keyword '"Sibley, David R."' showing total 7 results
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7 results on '"Sibley, David R."'

1. Characterization of the Binding Pocket for a Novel Positive Allosteric Modulator of the D1 Dopamine Receptor

Author

Hanson, John N., primary, Nilson, Ashley N., additional, Cohen, Eve, additional, Wang, Feijun, additional, Rayadurgam, Jayachandra, additional, Goldberg, Alexander, additional, Xie, Bing, additional, Luderman, Kathryn, additional, Free, R. Benjamin, additional, Shi, Lei, additional, Frankowski, Kevin, additional, and Sibley, David R., additional

Published
2024
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2. Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the D3 Dopamine Receptor

Author

Snyder, Kir K., primary, Moritz, Amy E., additional, Madaras, Nora, additional, Wang, Feijun, additional, Kelley, Amber, additional, Gandhi, Disha, additional, Akano, Emmanuel, additional, Inbody, Laura, additional, Lee, Kuo, additional, Free, R. Benjamin, additional, Shi, Lei, additional, Frankowski, Kevin, additional, and Sibley, David R., additional

Published
2024
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3. Enhancing Ligand Pharmacokinetics While Retaining Dopamine D4 Receptor Potency and Selectivity via Bioisosteric Substitution of Amide Linkers with 1,2,3-Triazoles

Author

Alkhatib, Mohammad, primary, Nilson, Ashley N., additional, Jakobs, Franziska M., additional, Hanson, John N., additional, Ricchezza, Joseph, additional, Jordan, Shannon, additional, Nguyen, Norman, additional, Kasarla, Nitish, additional, Wang, Bryant, additional, Garcia, Sergio Sola, additional, Rais, Rana, additional, Slusher, Barbara, additional, Free, R. Benjamin, additional, Sibley, David R., additional, Boateng, Comfort A., additional, and Keck, Thomas M., additional

Published
2024
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7. N-(3-Fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as Selective Dopamine D3 Receptor Ligands: Critical Role of the Carboxamide Linker for D3 Receptor Selectivity

Author

Banala, Ashwini K., Levy, Benjamin A., Khatri, Sameer S., Furman, Cheryse A., Roof, Rebecca A., Mishra, Yogesh, Griffin, Suzy A., Sibley, David R., Luedtke, Robert R., and Newman, Amy Hauck

Abstract

N-(3-Fluoro-4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazine-1-yl)butyl)arylcarboxamides were prepared and evaluated for binding and function at dopamine D3 receptors (D3Rs) and dopamine D2 receptors (D2Rs). In this series, we discovered some of the most D3R selective compounds reported to date (e.g., 8dand 8j, >1000-fold D3R-selective over D2R). In addition, chimeric receptor studies further identified the second extracellular (E2) loop as an important contributor to D3R binding selectivity. Further, compounds lacking the carbonyl group in the amide linker were synthesized, and while these amine-linked analogues bound with similar affinities to the amides at D2R, this modification dramatically reduced binding affinities at D3R by >100-fold (e.g., D3R Kifor 15b= 393 vs for 8j= 2.6 nM), resulting in compounds with significantly reduced D3R selectivity. This study supports a pivotal role for the D3R E2 loop and the carbonyl group in the 4-phenylpiperazine class of compounds and further reveals a point of separation between structure–activity relationships at D3R and D2R.

Published
2024
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