Open Access. Powered by Scholars. Published by Universities.®

Medicinal-Pharmaceutical Chemistry Commons

Open Access. Powered by Scholars. Published by Universities.®

Rowan University

2013

Articles 1 - 1 of 1

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

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 ...