Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands

Peng Jen Chen, Michelle Taylor, Suzy A. Griffin, Armaghan Amani, Hamed Hayatshahi, Kenneth Korzekwa, Min Ye, Robert H. Mach, Jin Liu, Robert R. Luedtke, John C. Gordon, Benjamin E. Blass

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)2690-2694
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume29
Issue number18
DOIs
StatePublished - 15 Sep 2019

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Benzamides
Dopamine D3 Receptors
Pharmacokinetics
Dopamine Receptors
Substance-Related Disorders
Rats
Ligands
Pharmaceutical Preparations
benzamide
Therapeutics

Keywords

  • D
  • D
  • Dopamine receptor
  • Drug addiction
  • G-protein coupled receptor (GPCR)

Cite this

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. / Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands. In: Bioorganic and Medicinal Chemistry Letters. 2019 ; Vol. 29, No. 18. pp. 2690-2694.
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Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands. / 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.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 29, No. 18, 15.09.2019, p. 2690-2694.

Research output: Contribution to journalArticle

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AU - Chen, Peng Jen

AU - Taylor, Michelle

AU - Griffin, Suzy A.

AU - Amani, Armaghan

AU - Hayatshahi, Hamed

AU - Korzekwa, Kenneth

AU - Ye, Min

AU - Mach, Robert H.

AU - Liu, Jin

AU - Luedtke, Robert R.

AU - Gordon, John C.

AU - Blass, Benjamin E.

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