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Chen PJ , Taylor M , Griffin SA , Amani A , Hayatshahi H , Korzekwa K , Ye M , Mach RH , Liu J , Luedtke RR , Gordon JC , Blass BE
Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands
Bioorg Med Chem Lett. 2019 Sep 15;29(18) :2690-2694
AbstractAs part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D3 ligands. Members of this class are highly selective for D3 versus D2, and we have identified two compounds (13g and 13r) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo efficacy models of substance use disorders.
Notes1464-3405 Chen, Peng-Jen Taylor, Michelle Griffin, Suzy A Amani, Armaghan Hayatshahi, Hamed Korzekwa, Kenneth Ye, Min Mach, Robert H Liu, Jin Luedtke, Robert R Gordon, John C Blass, Benjamin E Journal Article England Bioorg Med Chem Lett. 2019 Sep 15;29(18):2690-2694. doi: 10.1016/j.bmcl.2019.07.020. Epub 2019 Jul 11.