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Your search keyword '"Thomas M. Bridges"' showing total 2 results
Start Over Author "Thomas M. Bridges" Publication Type Academic Journals
2 results on '"Thomas M. Bridges"'

1. Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins.

Author

Thomas M. Bridges, Joy E. Marlo, Colleen M. Niswender, Carrie K. Jones, Satyawan B. Jadhav, Patrick R. Gentry, Hyekyung C. Plumley, C. David Weaver, P. Jeffrey Conn, and Craig W. Lindsley

Subjects
*ALLOSTERIC regulation, *MUSCARINIC receptors, *LIGANDS (Biochemistry), *CHOLINERGIC receptors, *DERIVATIZATION, *DRUG development, *ISATIN
Abstract

This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca2+mobilization assays. Subsequent optimization led to the discovery of VU0238429, which possessed an EC50of approximately 1.16 μM at M5 with >30-fold selectivity versus M1 and M3, with no M2 or M4 potentiator activity. [ABSTRACT FROM AUTHOR]

Published
2009
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