Major General James G. Blunt

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AC-42 is a selective, allosteric agonist of the M1 muscarinic acetylcholine receptor. AC-42 was the first selective M1 agonist to be discovered and its derivatives have been used to study the binding domain of the M1 receptor.[1][2][3]

References

  1. ^ Decker, Michael; Holzgrabe, Ulrike (2012). "M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease". MedChemComm. 3 (7): 752. doi:10.1039/c2md20025b.
  2. ^ Sams, Anette G.; Hentzer, Morten; Mikkelsen, Gitte K.; Larsen, Krestian; Bundgaard, Christoffer; Plath, Niels; Christoffersen, Claus T.; Bang-Andersen, Benny (9 September 2010). "Discovery of N -{1-[3-(3-Oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): An Allosteric Muscarinic M 1 Receptor Agonist with Unprecedented Selectivity and Procognitive Potential". Journal of Medicinal Chemistry. 53 (17): 6386–6397. doi:10.1021/jm100697g. PMID 20684563.
  3. ^ Daval, Sandrine B.; Valant, Céline; Bonnet, Dominique; Kellenberger, Esther; Hibert, Marcel; Galzi, Jean-Luc; Ilien, Brigitte (8 March 2012). "Fluorescent Derivatives of AC-42 To Probe Bitopic Orthosteric/Allosteric Binding Mechanisms on Muscarinic M1 Receptors" (PDF). Journal of Medicinal Chemistry. 55 (5): 2125–2143. doi:10.1021/jm201348t. PMID 22329602.