Contrasting Effects of Allosteric and Orthosteric Agonists on M1 Muscarinic Acetylcholine Receptor Internalization and Down-regulation

A new class of subtype-selective muscarinic acetylcholine (mACh) receptor agonist that activates the receptor through interaction at a site distinct from the orthosteric acetylcholine binding site has been reported recently. Here, we have compared the effects of orthosteric (oxotremorine-M, arecolin...

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Veröffentlicht in:	The Journal of pharmacology and experimental therapeutics 2009-12, Vol.331 (3), p.1086-1095
Hauptverfasser:	Thomas, Rachel L., Langmead, Christopher J., Wood, Martyn D., Challiss, R. A. John
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation Allosteric Site Animals Blotting, Western Cellular and Molecular CHO Cells Cricetinae Cricetulus Down-Regulation Ligands Muscarinic Agonists - pharmacology Piperidines - pharmacology Protein Binding Quinolones - pharmacology Radioligand Assay Receptor, Muscarinic M1 - agonists Receptor, Muscarinic M1 - biosynthesis Receptor, Muscarinic M2 - agonists Receptor, Muscarinic M2 - biosynthesis Receptor, Muscarinic M3 - agonists Receptor, Muscarinic M3 - biosynthesis Signal Transduction - drug effects
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