Article
New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug).
Molecular pharmacology - 1 Oct 2008
Nawaratne Vindhya, Leach Katie, Suratman Nur, Loiacono Richard E, Felder Christian C, Armbruster Blaine N, Roth Bryan L, Sexton Patrick M, Christopoulos Arthur
Abstract excerpt
The M4 muscarinic acetylcholine (ACh) receptor (mAChR) is a potential therapeutic target but characterized by a lack of subtype-selective ligands. We recently generated "designer receptors exclusively activated by a designer drug" (DREADDs), which contained mutations of two conserved orthosteric-site residues (Y113C/A203G in the M4 mAChR) that caused a loss of ACh activity but a gain in responsiveness to...
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