E
Edwin J. Schweiger
Researcher at General Atomics
Publications - 7
Citations - 648
Edwin J. Schweiger 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 630 citations. Previous affiliations of Edwin J. Schweiger include Merck & Co..
Papers
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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
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.
Nicholas D. P. Cosford,Jeffrey Roger Roppe,Lida Tehrani,Edwin J. Schweiger,T. Jon Seiders,Ashok Chaudary,Sara Rao,Mark A. Varney +7 more
TL;DR: The design, synthesis, and characterization of two potent, non-competitive radioligands, [3H]-methoxymethyl-MTEP and [ 3H]- methoxy-PEPy, that are selective for the mGlu5 receptor are described.
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.
Patent
Heterocyclic compounds and methods of use thereof
Leo Bleicher,Nicholas D. P. Cosford,Rowena V. Cube,Stephen D. Hess,Ian A. McDonald,Benito Munoz,Edwin J. Schweiger,Mark A. Varney,Jean-Michel Vernier +8 more
TL;DR: In this paper, the authors provided novel class of heterocyclic compounds and methods of use thereof and provided methods of modulating metabotropic glutamate receptors using these compounds and also disclosed methods of treating disease using these drugs.
Journal ArticleDOI
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists
Peter C. Chua,Johnny Yasuo Nagasawa,Leo Bleicher,Benito Munoz,Edwin J. Schweiger,Lida Tehrani,Jeffrey Anderson,Merryl Cramer,Janice Chung,Mitchell D. Green,Christopher D. King,Grace Reyes-Manalo,Nicholas D. P. Cosford +12 more
TL;DR: Structure-activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile.