Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands. Issue 18 (15th September 2019)

• Record Type: Journal Article
• Authors: 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.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 18(2019)
• Page Start: 2690
• Page End: 2694
• Publication Date: 2019-09-15
• Subjects: Dopamine receptor -- D3 -- D2 -- G-protein coupled receptor (GPCR) -- Drug addiction; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.07.020
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: As 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.