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Xiaohui Jiang
Researcher at General Atomics
Publications - 7
Citations - 634
Xiaohui Jiang is an academic researcher from General Atomics. The author has contributed to research in topics: Metabotropic receptor & MTEP. The author has an hindex of 6, co-authored 7 publications receiving 619 citations.
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Journal ArticleDOI
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity
Nicholas D. P. Cosford,Lida Tehrani,Jeffrey Roger Roppe,Edwin J. Schweiger,Nicholas D. Smith,Jeffrey Anderson,Linda J. Bristow,Jesse Brodkin,Xiaohui Jiang,Ian A. McDonald,Sara Rao,Mark S. Washburn,Mark A. Varney +12 more
TL;DR: Seeking to improve the properties of 2-Methyl-6-(phenylethynyl)pyridine led to the synthesis of compound 9, a highly selective mGlu5 receptor antagonist that is 5-fold more potent than 3 in the rat fear-potentiated startle model of anxiety.
Journal ArticleDOI
Discovery of Novel Heteroarylazoles That Are Metabotropic Glutamate Subtype 5 Receptor Antagonists with Anxiolytic Activity
Jeffrey Roger Roppe,Nicholas D. Smith,Dehua Huang,Lida Tehrani,Bowei Wang,Jeffrey Anderson,Jesse Brodkin,Janice Chung,Xiaohui Jiang,Christopher D. King,Benito Munoz,Mark A. Varney,Petpiboon Peppi Prasit,Nicholas D. P. Cosford +13 more
TL;DR: Compound 47 is active in the rat fear-potentiated startle (FPS) model of anxiety with ED(50) = 5.4 mg/kg (po) when dosed acutely and rapidly tolerate on repeated dosing.
Journal ArticleDOI
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Jeffrey Roger Roppe,Bowei Wang,Dehua Huang,Lida Tehrani,Theodore M. Kamenecka,Edwin J. Schweiger,Jeffery J. Anderson,Jesse Brodkin,Xiaohui Jiang,Merryl Cramer,Janice Chung,Grace Reyes-Manalo,Benito Munoz,Nicholas D. P. Cosford +13 more
TL;DR: The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo receptor occupancy, and is efficacious in the rat fear-potentiated startle model of anxiety following oral dosing.
Journal ArticleDOI
Discovery of novel modulators of metabotropic glutamate receptor subtype-5
Bowei Wang,Jean Michel Vernier,Sara Rao,Janice Chung,Jeffery J. Anderson,Jesse Brodkin,Xiaohui Jiang,Michael F. Gardner,Xiaoqing Yang,Benito Munoz +9 more
TL;DR: A series of potent and selective mGluR5 antagonists were synthesized and evaluated in vitro and in vivo and it was found that a pyridyl functionality is a potential replacement for acetonitrile in the lead structure, with 2-p Pyridyl being most favored.
Journal ArticleDOI
The geminal dimethyl analogue of Flurbiprofen as a novel Aβ42 inhibitor and potential Alzheimer's disease modifying agent
Nicholas Simon Stock,Benito Munoz,Jonathan D.J. Wrigley,Mark S. Shearman,Dirk Beher,James Peachey,Toni L. Williamson,Gretchen Bain,Weichao Chen,Xiaohui Jiang,René St-Jacques,Peppi Prasit +11 more
TL;DR: Methylflurbiprofen 6 exhibited similar in vitro Abeta42 inhibition to its parent NSAID Flurbip rofen and was further evaluated in the Tg2576 mouse model of Alzheimer's disease and an animal model of gastro-intestinal impairment, but proved unviable for further clinical development.