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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Identifying Medication Targets For Psychostimulant Addiction: Unraveling The Dopamine D3 Receptor Hypothesis, Thomas M. Keck, William S. John, Paul W. Czoty, Michael A. Nader, Amy Hauck Newman Mar 2015

Identifying Medication Targets For Psychostimulant Addiction: Unraveling The Dopamine D3 Receptor Hypothesis, Thomas M. Keck, William S. John, Paul W. Czoty, Michael A. Nader, Amy Hauck Newman

Faculty Scholarship for the College of Science & Mathematics

The dopamine D3 receptor (D3R) is a target for developing medications to treat substance use disorders. D3R-selective compounds with high affinity and varying efficacies have been discovered, providing critical research tools for cell-based studies that have been translated to in vivo models of drug abuse. D3R antagonists and partial agonists have shown especially promising results in rodent models of relapse-like behavior, including stress-, drug-, and cue-induced reinstatement of drug seeking. However, to date, translation to human studies has been limited. Herein, we present an overview and illustrate some of the pitfalls and challenges of developing novel D3R-selective compounds toward clinical ...


A Novel Mglur5 Antagonist, Mfz 10-7, Inhibits Cocaine-Taking And Cocaine-Seeking Behavior In Rats, Thomas Keck, Mu-Fa Zou, Gui-Hua Bi, Hai-Ying Zhang, Xiao-Fei Wang, Hong-Ju Yang, Ratika Srivastava, Elliott L. Gardner, Zheng-Xiong Xi, Amy Hauck Newman Sep 2013

A Novel Mglur5 Antagonist, Mfz 10-7, Inhibits Cocaine-Taking And Cocaine-Seeking Behavior In Rats, Thomas Keck, Mu-Fa Zou, Gui-Hua Bi, Hai-Ying Zhang, Xiao-Fei Wang, Hong-Ju Yang, Ratika Srivastava, Elliott L. Gardner, Zheng-Xiong Xi, Amy Hauck Newman

Faculty Scholarship for the College of Science & Mathematics

Pre-clinical studies suggest that negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5), including 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and fenobam are highly effective in attenuating drug-taking and drug-seeking behaviors. However, both MPEP and MTEP have no translational potential for use in humans because of their off-target effects and short half-lives. Here, we report that 3-fluoro-5-[(6-methylpyridin-2-yl)ethynyl]benzonitrile (MFZ 10-7), a novel mGluR5 NAM, is more potent and selective than MPEP, MTEP and fenobam in both in vitro binding and functional assays. Similar to MTEP, intraperitoneal administration of MFZ 10-7 inhibited ...