Design, synthesis, and evaluation of functionalized 5-(4-arylpiperazin-1-yl)-N-quinolinyl-pentanamides as selective dopamine D3 receptor ligands

Dopamine ( 1 ) plays a key role in normal physiological pathways in both the central nervous system and the periphery. The physiological impact of this neurotransmitter is mediated through its interaction with family of G-protein-coupled receptors (GPCRs). These receptors are designated as D 1 , D 2...

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Published inMedicinal chemistry research Vol. 31; no. 5; pp. 749 - 761
Main Authors Blass, Benjamin E., Chen, Peng-Jen, Taylor, Michelle, Griffin, Suzy A., Gordon, John C., Luedtke, Robert R.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.05.2022
Springer Nature B.V
Subjects
Amino acids
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Central nervous system
Dopamine
Dopamine D1 receptors
Dopamine D2 receptors
Dopamine D3 receptors
Dopamine D4 receptors
Dopamine D5 receptors
G protein-coupled receptors
Homology
Inflammatory diseases
Inorganic Chemistry
Ligands
Medicinal Chemistry
Mental disorders
Movement disorders
Neurodegenerative diseases
Neurotransmitters
Original Research
Parkinson's disease
Pharmacology/Toxicology
Physiology
Receptors
Schizophrenia
D
dopamine receptor
Dopamine
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Summary:Dopamine ( 1 ) plays a key role in normal physiological pathways in both the central nervous system and the periphery. The physiological impact of this neurotransmitter is mediated through its interaction with family of G-protein-coupled receptors (GPCRs). These receptors are designated as D 1 , D 2 , D 3 , D 4 , and D 5 and divided into two sub-families, the D 1 -like sub-family (D 1 and D 5 ) and D 2 -like sub-family (D 2 , D 3 and D 4 ) based on pharmacological properties, amino acid homology, and genetic organization. Aberrant D 3 activity has been linked to multiple diseases and conditions such as depression, schizophrenia, substance use disorder, inflammatory diseases, and Parkinson’s disease (PD). As part of our on-going program focused on the identification of novel D 3 ligands, we have identified a novel series of 5-(4-arylpiperazin-1-yl)-N-quinolinyl-pentanamides that are high affinity ligands for this receptor. Graphical Abstract
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-022-02873-3